| 产品标题 |
产品货号 |
产品规格 |
厂家 |
| Stem Cell 3i inhibitor Set | Axon 2129
CAS [N.A.]
MF N.A.MW N.A.
Purity:
99%
Soluble in DMSO
Description
A convenient set of FGFR inhibitor SU 5402 (Axon 1667), MEK inhibitor PD 184352 (Axon 1368) and GSK-3 inhibitor CHIR 99021 (Axon 1386); This conventional 3i inhibitor set, used together to sustain mouse embryonic stem cell (mESC) self-renewal.
Read more: Additional Product Information
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References
Certificates
Categories
Extra info
Q.L. Ying et al. The ground state of embryonic stem cell self-renewal. Nature, 2008, 453, 519-523.
P. Li et al. Germline competent embryonic stem cells derived from rat blastocysts. Cell. 2008, 135, 1299-1310.
H. Kiyonari et al. Three inhibitors of FGF receptor, ERK, and GSK3 establishes germline‐competent embryonic stem cells of C57BL/6N mouse strain with high efficiency and stability. Genesis. 2010, 48, 317-327.
List of publications using PD 184352 (CI 1040) (Axon 1368) purchased from Axon Medchem
List of publications using CHIR 99021 (Axon 1386) purchased from Axon Medchem
Certificate of Analysis
Material Safety Data Sheet
Additional Product Information
Angiogenesis
Cell Signaling & Oncology
CNS
Diabetes & Metabolism
Immunology
Pain & Inflammation
Stem Cell
GSK-3
Wnt-β-Catenin
MAPK
PI3K-Akt-mTOR
Stem Cells
FGFR
MEK
Set of FGFR inhibitor SU5402 (Axon 1667), MEK inhibitor PD184352 (Axon 1368) and GSK-3 inhibitor CHIR99021 (Axon 1386)
Chemical name
N.A.
Parent CAS No.
[N.A.]
Order
Size
Unit Price
Stock
Each 2 mg
€145.00
In Stock | | axonmedchem |
| Stem Cell 2i inhibitor Set | Axon 2128
CAS [N.A.]
MF N.A.MW N.A.
Purity:
99%
Soluble in DMSO
Description
A convenient set of MEK inhibitor PD 0325901 (Axon 1408) and GSK3 inhibitor CHIR 99021 (Axon 1386); highly recommended conventional 2i inhibitor set, used together for dual inhibition of MAPK signaling and GSK-3 in stem cell research, to enable mouse embryonic stem cell (mESC) self-renewal and pluripotency marker expression.
Prime Source Information | | axonmedchem |
| CHIR 99021 - CT 99021 | Axon 1386
CAS [252917-06-9]
MF C22H18Cl2N8MW 465.34
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Very potent and specific glycogen synthase kinase GSK-3 inhibitor; highly recommended tool. * CHIR 99021 and PD 0325901 (Axon 1408) are often used together as 2i in stem cell research (Axon 2128).
CHIR 99021 is also available as the water soluble HCl salt (Axon 2435)
*Promotion | | axonmedchem |
| SB 431542 | Axon 1661
CAS [301836-41-9]
MF C22H16N4O3MW 384.39
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of TGF-β1 superfamily activin receptor-like kinase (ALK), specifically at ALK5 (IC50: 94 nM) and its relatives ALK4 (IC50: 140 nM) and ALK7; SB431542 inhibits endogenous activin and TGF-β signaling, but has no effect on BMP signaling; a useful tool for studing the role of TGF-β, activin and many cellular processes.
*Promotion | | axonmedchem |
| LDN 193189 hydrochloride - DM 3189 hydrochloride | Axon 1509
CAS [1435934-00-1]
MF C25H22N6.2HClMW 479.40
Purity:
99%
Soluble in water and DMSO
Description
A highly potent small molecule BMP inhibitor; inhibiting BMP type I receptors ALK2 (IC50: 5 nM), ALK3 (IC50: 30 nM) and ALK6 (TGFβ1/BMP signaling) and subsequent SMAD phosphorylation; useful tool in stem cell biology. LDN 193189 shows significant in vivo clinical utility, inhibiting FOP and ectopic ossification and a potential agent in the treatment of NSCLC lung tumors.
*Promotion | | axonmedchem |
| Stem Cell LSB inhibitor Set | Axon 5004
CAS [N.A.]
MF #N/AMW #N/A
Purity:
99%
Soluble in DMSO
Description
A convenient set of BMP inhibitor LDN 193189 hydrochloride (Axon 1509) and TGF-β inhibitor SB 431542 (Axon 1661) (termed as LSB by their name abbreviation), for neural differentiation of human pluripotent stem cells (hPSCs). Dual SMAD inhibition by LSB cocktail is an highly efficient protocol for neural induction of hPSCs and more than 80% of hPSCs can be rapidly induced into Pax6+ neural precursor cells by using LDN 193189 (0.1 µM) and SB 431542 (10 µM).
LSB protocol can be further extended; with adding CHIR 99021 (Axon 1386) to form LSC or LSB/CHIR inhibitor set (Axon 5005) for generating subtype specific neural/neuronal cells; or with combining neuronal 3i (CSD) inhibitor set (Axon 5006) of CHIR 99021 (Axon 1386), SU 5402 (Axon 1667) and DAPT (Axon 1484) to form a 5i inhibitor set (Axon 5007, LSB3i), for rapid differentiation of hPSCs into nociceptors.
Read more: Additional Product Information
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References
Certificates
Categories
Extra info
J. Ladewig et al. Small molecules enable highly efficient neuronal conversion of human fibroblasts. Nat Methods. 2012, 9, 575-578.
S.M. Chambers et al. Combined small-molecule inhibition accelerates developmental timing and converts human pluripotent stem cells into nociceptors. Nature Biotechnol. 2012, 30, 715-720.
S.M. Chambers et al. Highly efficient neural conversion of human ES and iPS cells by dual inhibition of SMAD signaling. Nat. Biotechnol. 2009, 27, 275–280.
List of publications using LDN 193189 hydrochloride | | axonmedchem |
| PF 03814735 | Axon 2023
CAS [942487-16-3]
MF C23H25F3N6O2MW 474.48
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent, orally bioavailable, ATP-competitive and reversible inhibitor of aurora kinase A (IC50: 0.8 nM) and aurora kinase B (IC50: 5 nM) with potential antineoplastic activity; PF 03814735 also inhibits Flt1, FAK and TrkA with IC50 values of 10, 22, 30 nM respectively; clinical candidate.
KEYWORDS: PF 03814735 | supplier | Aurora inhibitor | PF03814735 | PF-03814735 | CAS [942487-16-3] | Histone | Survivin | Topo | TPX2 | Aurora kinase | antineoplastic activity | Flt1 | FAK | TrkA | clinical candidate | | axonmedchem |
| DAPT | Axon 1484
CAS [208255-80-5]
MF C23H26F2N2O4MW 432.46
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Inhibitor of γ-secretase.
*Promotion | | axonmedchem |
| VU6001221 | Axon 2670
CAS [2002495-17-0]
MF C20H26ClN3O3MW 391.89
Purity:
98%
Soluble in DMSO
Description
VU6001221 is a choline transporter (CHT) inhibitor (IC50 value of 270 nM) with comparable potency for choline uptake inhibition as ML352 (Axon 2587), yet improved PK and CNS penetration. For the first time, VU6001221 allowed evaluation of a CHT inhibitor in a standard preclinical rodent cognition model, namely novel object recognition (NOR).
KEYWORDS: VU6001221 | CHT inhibitor | VU 6001221 | VU-6001221 | CAS [2002495-17-0] | Choline | CHT | Inhibitor | Proteins | | axonmedchem |
| ML352 - VU0476201 | Axon 2587
CAS [1649450-12-3]
MF C21H29N3O4MW 387.47
Purity:
98%
Soluble in 0.1N HCl (aq) and DMSO
Description
Potent and selective inhibitor of the presynaptic choline transporter (CHT; Ki value 92 nM). ML352 exhibited no inhibition of acetylcholinesterase (AChE) or cholineacetyltransferase (ChAT) and also lacked activity at dopamine, serotonin, and norepinephrine transporters, as well as many receptors and ion channels.
KEYWORDS: ML352 | supplier | CHT inhibitor | VU0476201 | ML-352 | VU-0476201 | CAS [1649450-12-3] | Choline transporter | ACh | AChE | neurotransmitter | Alzheimer’s | Parkinson’s | dystonia | schizophrenia | addiction | | axonmedchem |
| TBPB | Axon 2463
CAS [634616-95-8]
MF C25H32N4OMW 404.55
Purity:
100%
Soluble in DMSO
Description
Selective allosteric activator of the M1 muscarinic acetylcholine receptor (EC50 value 20 nM at hM1-WT) devoid of M2-M5 activity. TBPB increases non-amyloidogenic APP processing and produces antipsychotic-like effects in rodent models predictive of antipsychotic-like activity.
References
Certificates
Categories
Extra info
C.K. Jones et al. Novel selective allosteric activator of the M1 muscarinic acetylcholine receptor regulates amyloid processing and produces antipsychotic-like activity in rats. J Neurosci. 2008 Oct 8;28(41):10422-33. doi: 10.1523/JNEUROSCI.1850-08.2008.
M.A. Jacobson et al. The M1 muscarinic receptor allosteric agonists AC-42 and 1-[1'-(2-methylbenzyl)-1,4'-bipiperidin-4-yl]-1,3-dihydro-2H-benzimidazol-2-one bind to a unique site distinct from.... Mol Pharmacol. 2010 Oct;78(4):648-57.
T.M. Bridges et al. Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties. Bioorg Med Chem Lett. 2008 Oct 15;18(20):5439-42.
Certificate of Analysis
Material Safety Data Sheet
CNS
CHRM1
A18
Allosteric activator of the M1 acetylcholine receptor devoid of M2-M5 activity.
Chemical name
1-(1'-(2-methylbenzyl)-1,4'-bipiperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one
Parent CAS No.
[634616-95-8]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| SU11652 | Axon 2767
CAS [326914-10-7]
MF C22H27ClN4O2MW 414.93
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
SU11652 is a sunitinib-like RTK inhibitor of PDGFR-β, VEGFR2, FGFR1 and FLT3, with IC50 values of 3, 27, 170 and 1.5 nM, respectively. Moreover, SU11652 inhibits cKit, acid sphingomyelinase, destabilizes lysosomes, and inhibits multidrug resistance.
KEYWORDS: SU11652 | supplier | RTK inhibitor | SU 11652 | SU-11652 | CAS [326914-10-7] | SCF-PDGF-VEGF | c-KIT | PDGFR | VEGFR | FLT3 | Inhibitor | Receptors | Acid sphingomyelinase | | axonmedchem |
| Apatinib - Apatinib mesylate | YN968D1 | Rivoceranib mesylate | Axon 2849
CAS [1218779-75-9]
MF C25H27N5O4SMW 493.58
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of VEGFR2 tyrosine kinase (IC50 value of 1 nM). Apatinib could also potently suppress the activities of RET, c-KIT and c-Src with IC50 values of 0.13, 0.429 and 0.53 μM, respectively. In vivo, apatinib alone and in combination with chemotherapeutic agents effectively inhibited the growth of several established human tumor xenograft models with little toxicity.
KEYWORDS: Apatinib | supplier | VEGFR2 inhibitor | Apatinib mesylate | YN968D1 | Rivoceranib mesylate | CAS [1218779-75-9] | [811803-05-1] | VEGF | VEGFR | Inhibitor | Receptors | Angiogenesis | | axonmedchem |
| SU 5402 | Axon 1667
CAS [215543-92-3]
MF C17H16N2O3MW 296.32
Purity:
99%
Soluble in 0.1N NaOH(aq) and DMSO
Description
Fibroblast growth factor receptor (FGFR) inhibitor.
A convenient set of FGFR inhibitor SU 5402 (Axon 1667), MEK inhibitor PD 184352 (Axon 1368) and GSK-3 inhibitor CHIR 99021 (Axon 1386) (conventional 3i, Axon 2129), was used together to sustain mouse embryonic stem cell (mESC) self-renewal.
*Promotion | | axonmedchem |
| Nintedanib - BIBF-1120 | Axon 2648
CAS [656247-17-5]
MF C31H33N5O4MW 539.62
Purity:
100%
Soluble in 0.1N HCl(aq) and DMSO
Description
Orally bioavailable, indolinone-derived, receptor tyrosine kinase (RTK) inhibitor with potential antiangiogenic and antineoplastic activities that simultaneously targets VEGFR1-3 (IC50 values 34 nM, 21 nM, and 13 nM, resp.), PDGFRα and β (IC50 values 59 and 65 nM), and FGFR1-3 (IC50 values 69 nM, 37 nM, and 108 nM, resp). In addition, BIBF1120 also inhibits members of the Src family of tyrosine kinases, including Src, Lck, Lyn, and FLT-3 (IC50 values 156 nM, 16 nM, 195 nM, and 26 nM, resp.).
KEYWORDS: Nintedanib | supplier | RTK inhibitor | Angiokinase inhibitor | BIBF-1120 | BIBF1120 | Intedanib | CAS [656247-17-5] - [656247-18-6] | PDGF-FGF-VEGF | PDGFR | FGFR | VEGFR | Receptor tyrosine kinase | Src | Lck | Lyn | FLT-3 | antiangiogenic | antineoplastic | antitumor | | axonmedchem |
| AST 1306 tosylate | Axon 1986
CAS [1050500-29-2]
MF C24H18ClFN4O2.C7H8O3SMW 621.08
Purity:
98%
Soluble in DMSO
Description
A selective, irreversible ErbB2 and EGFR inhibitor whose growth-inhibitory effects are more potent in ErbB2-overexpressing cells; AST1306 potently inhibits wild-type EGFR and ErbB2, as well as EGFR mutant T790M/L858R, in both cell-free and intact cell assays; IC50 values to be 0.5, 3.0, 0.8 and 12 nM for EGFR, ErbB2, ErbB4 and EGFR mutant T790M/L858R, respectively
References
Certificates
Categories
Extra info
H Xie et al. AST1306, A Novel Irreversible Inhibitor of the Epidermal Growth Factor Receptor 1 and 2, Exhibits Antitumor Activity Both In Vitro and In Vivo. PLoS ONE 2011, 6(7), e21487.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
EGFR
ErbB2-HER2
JAK-STAT
RTK class I; EC 2.7.10.1
ErbB2 and EGFR inhibitor
Chemical name
N-(4-(3-chloro-4-(3-fluorobenzyloxy)phenylamino)quinazolin-6-yl)acrylamide 4-methylbenzenesulfonate
Parent CAS No.
[897383-62-9]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| ZM 323881 hydrochloride | Axon 1978
CAS [193000-39-4]
MF C22H18FN3O2.HClMW 411.86
Purity:
99%
Soluble in DMSO
Description
Potent and selective inhibitor of VEGFR2 (IC50: 2 nM for VEGFR2 vs >50 mM for VEGFR1 respectively)
KEYWORDS: ZM 323881 hydrochloride | supplier VEGFR2 inhibitor | ZM323881 HCl | CAS [193000-39-4] | [193001-14-8] | VEGF | VEGFR | RTK | receptor tyrosine kinase | vascular endothelial growth factor | cancer | arthritis | diabetes | | axonmedchem |
| Golvatinib - E 7050 | Axon 1959
CAS [928037-13-2]
MF C33H37F2N7O4MW 633.69
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent and orally available inhibitor of c-MET (HGFR) (IC50: 14 nM) and VEGFR2 (IC50: 16 nM); Golvatinib inhibits the activities of both c-Met and VEGFR2, which may inhibit tumor cell growth and survival of tumor cells that overexpress these receptor tyrosine kinases
References
Certificates
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Extra info
T Nakagawa et al. E7050: A dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models. Cancer Science 2010, 101(1), 210-215.
W Wang et al. Met kinase inhibitor E7050 reverses three different mechanisms of hepatocyte growth factor-induced tyrosine kinase inhibitor resistance in EGFR mutant lung cancer. Clin Cancer Res. 2012, 18(6):1663-1671.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
c-MET
VEGFR
RTK class IV and X; EC 2.7.10.1
Potent and orally available inhibitor of c-MET (HGFR) and VEGFR2
Chemical name
N-(2-fluoro-4-(2-(4-(4-methylpiperazin-1-yl)piperidine-1-carboxamido)pyridin-4-yloxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Parent CAS No.
[928037-13-2]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |
| NSC 228155 | Axon 2955
CAS [113104-25-9]
MF C11H6N4O4SMW 290.25
Purity:
98%
Soluble in DMSO
Recently added | | axonmedchem |
| AZD 3759 | Axon 2563
CAS [1626387-80-1]
MF C22H23ClFN5O3MW 459.90
Purity:
98%
Optical purity:
Optically pure
Soluble in 0.1N HCl(aq) and DMSO
Description
Potent, orally active, brain-penetrant, EGFR tyrosine kinase inhibitor (IC50 value 7.2 nM for inhibition of cellular phosphorylation on L858R cell lines), that shows tumor regression in the mouse model with brain metastasis. At 1 µM, AZD 3759 showed less than 50% inhibition against 115 out of a panel of 124 recombinant protein and lipid kinases, and was neither a direct inhibitor nor a time-dependent inhibitor for a series of Cytochrome isoforms, suggesting a low enzyme induction liability.
KEYWORDS: AZD 3759 | supplier | EGFR inhibitor | AZD3759 | CAS [1626387-80-1] | [1626387-81-2] | EGF | EGFR | Inhibitor | orally active | brain-penetrant | RTK | CNS | tumor regression | metastases | clinical trial | central nervous system | | axonmedchem |
| AZD 9291 - Osimertinib | Axon 2342
CAS [1421373-65-0]
MF C28H33N7O2MW 499.61
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
A potent oral, third-generation EGFR TKI, that irreversibly and selectively targets both sensitizing and resistant T790M+ mutant EGFR while harboring less activity toward wild-type EGFR (IC50 values 1 nM,12 nM, 5 nM, and 184 nM against L858R/T790M-, L858R-, L861Q-mutant, and WT EGFR, respectively).
KEYWORDS: AZD 9291 | supplier | EGFR inhibitor | Osimertinib | AZD9291 | CAS [1421373-65-0] | EGF | EGFR | Non-small cell lung cancer | NSCLC | ERBB | HER | T790M | TKI | cancer | oncology | | axonmedchem |
| E 3810 dihydrochloride - AL 3810 dihydrochloride | Lucitanib | Axon 1942
CAS [N.A.]
MF C26H25N3O4.2HClMW 516.42
Purity:
99%
Soluble in water and DMSO
Description
First-in-class dual VEGFR/FGFR tyrosine kinase inhibitor; E-3810 potently and selectively inhibited VEGFR1, -2, and -3 and FGFR-1 and -2 kinases in the nanomolar range; a potent antiangiogenic small molecule with a favorable pharmacokinetic profile and broad spectrum antitumor activity
References
Certificates
Categories
Extra info
E Bello et al. E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011, 71(4), 1396-1405.
JC Soria et al. First-in-man study of E-3810, a novel VEGFR and FGFR inhibitor, in patients with advanced solid tumors. Ann. Oncol. 2011, 22, 40.
Y Zhou et al. AL3810, a multi-tyrosine kinase inhibitor, exhibits potent anti-angiogenic and anti-tumour activity via targeting VEGFR, FGFR and PDGFR. J. Cell Mol. Med. 2012, 16(10), 2321-2330.
G Damia et al. Is PDGFR an important target for E-3810? J. Cell Mol. Med. 2012, 16(11), 2838-2839. [Letter to the Editor]
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
VEGFR
RTK class IV and V; EC 2.7.10.1
FGFR
Dual VEGFR/FGFR tyrosine kinase inhibitor
Chemical name
6-(7-((1-aminocyclopropyl)methoxy)-6-methoxyquinolin-4-yloxy)-N-methyl-1-naphthamide dihydrochloride
Parent CAS No.
[1058137-23-7]
Order
Size
Unit Price
Stock
2 mg
€95.00
In Stock | | axonmedchem |
| SU 6668 - TSU 68 | Orantinib | Axon 1891
CAS [252916-29-3]
MF C18H18N2O3MW 310.35
Purity:
98%
Soluble in 0.1N NaOH(aq) and DMSO
Description
An ATP-competitive, orally bioavailable receptor tyrosine kinase (RTK) inhibitor targeting PDGFR, VEGF and FGFR (IC50 values are 0.06, 2.43, 3.04 and >100 μM at PDGFRβ, VEGFR2, FGFR1 and EGFR respectively)
References
Certificates
Categories
Extra info
L Sun et al. Design, synthesis, and evaluations of substituted 3-[(3- or 4-carboxyethylpyrrol-2-yl)methylidenyl]indolin-2-ones as inhibitors of VEGF, FGF, and PDGF receptor tyrosine kinases. J Med Chem. 1999, 42(25), 5120-5130.
AD Laird et al. SU6668 is a potent antiangiogenic and antitumor agent that induces regression of established tumors. Cancer Res. 2000, 60(15), 4152-4160.
M Toi et al. A multicenter phase II study of TSU-68, an oral multiple tyrosine kinase inhibitor, in combination with docetaxel in metastatic breast cancer patients with anthracycline resistance. Breast Cancer. 2014, 21(1), 20-27.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
VEGFR
PDGFR
RTK class III, IV and V; EC 2.7.10.1
FGFR
Inhibitor of RTK targeting PDGFR, VEGF and FGFR
Chemical name
3-(2,4-dimethyl-5-((2-oxoindolin-3-ylidene)methyl)-1H-pyrrol-3-yl)propanoic acid
Parent CAS No.
[252916-29-3]
Order
Size
Unit Price
Stock
10 mg
€105.00
In Stock | | axonmedchem |
| Brivanib alaninate - BMS 582664 | Axon 1864
CAS [649735-63-7]
MF C22H24FN5O4MW 441.46
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Brivalib alaninate (BMS 582664) is the orally active prodrug of BMS 540215 (Axon 1850). Brivanib alaninate hydrolyzes in vivo quickly to BMS 540215, which is a potent and ATP-competitive VEGFR inhibitor with IC50 of 25, 380 and 10 nM for VEGFR2, -1 and -3 respectively; also showed good selectivity for FGFR-1, -2, and -3 with IC50 of 148, 125 and 68 nM
References
Certificates
Categories
Extra info
ZW Cai et al. Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular (...). J. Med. Chem. 2008, 51(6), 1976-1980.
H Huynh et al. Brivanib Alaninate, a Dual Inhibitor of Vascular Endothelial Growth Factor Receptor and Fibroblast Growth Factor Receptor Tyrosine Kinases, Induces Growth Inhibition in Mouse Models (...). Clin. Cancer Res. 2008, 14, 6146.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
VEGFR
RTK class IV; EC 2.7.10.1
Prodrug of BMS 540215; Inhibitor of VEGF
Chemical name
(S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[1,2-f][1,2,4]triazin-6-yloxy)propan-2-yl) 2-aminopropanoate
Parent CAS No.
[649735-63-7]
Order
Size
Unit Price
Stock
2 mg
€105.00
In Stock | | axonmedchem |
| BMS 540215 - Brivanib | Axon 1850
CAS [649735-46-6]
MF C19H19FN4O3MW 370.38
Purity:
98%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent and ATP-competitive inhibitor of VEGF; it inhibits VEGFR2, -1 and -3 with IC50 of 25, 380 and 10 nM respectively; also showed good selectivity for FGFR-1, -2, and -3 with IC50 of 148, 125 and 68 nM. BMS 540215 is the active component of its prodrug, Brivalib alaninate (BMS 582664, Axon 1864), which hydrolyzes to BMS 540215 in vivo quickly
References
Certificates
Categories
Extra info
RS Bhide et al. Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor. J. Med. Chem. 2006, 49(7), 2143-2146.
ZW Cai et al. Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular (...). J. Med. Chem. 2008, 51(6), 1976-1980.
H Huynh et al. Brivanib Alaninate, a Dual Inhibitor of Vascular Endothelial Growth Factor Receptor and Fibroblast Growth Factor Receptor Tyrosine Kinases, Induces Growth Inhibition in Mouse Models (...). Clin. Cancer Res. 2008, 14, 6146.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
VEGFR
RTK class IV; EC 2.7.10.1
Inhibitor of VEGFR (subtype 2 and 3 selective)
Chemical name
(R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[1,2-f][1,2,4]triazin-6-yloxy)propan-2-ol
Parent CAS No.
[649735-46-6]
Order
Size
Unit Price
Stock
5 mg
€110.00
In Stock | | axonmedchem |
| Cabozantinib S-malate - XL 184 | Axon 1819
CAS [1140909-48-3]
MF C28H24FN3O5.C4H6O5MW 635.59
Purity:
99%
Soluble in DMSO
Description
A orally available and potent inhibitor of multiple receptor tyrosine kinases (RTK), specifically MET and VEGFR2. It also inhibits KIT, FLT3, Tie-2, RET and AXL
References
Certificates
Categories
Extra info
M Yakes et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol. Cancer Ther. 2011, 10(12), 2298-2308.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
Axl
c-MET
FLT3
VEGFR
c-KIT
RTK class IV and X; EC 2.7.10.1
Inhibitor of multiple receptor tyrosine kinases, specifically MET and VEGFR2
Chemical name
N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide (S)-2-hydroxysuccinate
Parent CAS No.
[849217-68-1]
Order
Size
Unit Price
Stock
10 mg
€85.00
In Stock | | axonmedchem |
| AMG 706 - Motesanib diphosphate | Axon 1768
CAS [857876-30-3]
MF C22H23N5O.2H3O4PMW 569.44
Purity:
99%
Soluble in water
Description
A potent and orally bioavailable multiple receptor tyrosine kinase inhibitor, targeting VEGFR/PDGFR/c-KIT (IC50: 2, 3, 6, 84, 8 and 59 nm for VEGFR1, VEGFR2, VEGFR3, PDGFR, KIT and Ret receptors respectively); potently inhibits angiogenesis and induces regression in tumor xenografts.
References
Certificates
Categories
Extra info
A Polverino et al. AMG 706, an Oral, Multikinase Inhibitor that Selectively Targets Vascular Endothelial Growth Factor, Platelet-Derived Growth Factor, and Kit Receptors, Potently Inhibits Angiogenesis (...). Cancer Res. 2006, 66, 8715.
A Coxon et al. Broad Antitumor Activity in Breast Cancer Xenografts by Motesanib, a Highly Selective, Oral Inhibitor of Vascular Endothelial Growth Factor, Platelet-Derived Growth Factor, and Kit Receptors. Clin. Cancer Res. 2009, 15, 110.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
VEGFR
PDGFR
c-KIT
RTK class III and IV; EC 2.7.10.1
Multiple receptor tyrosine kinase inhibitor
Chemical name
N-(3,3-dimethylindolin-6-yl)-2-(pyridin-4-ylmethylamino)nicotinamide bis(phosphate)
Parent CAS No.
[453562-69-1]
Order
Size
Unit Price
Stock
5 mg
€105.00
In Stock | | axonmedchem |
| RET Inhibitor 2667 | Axon 2667
CAS [1980023-80-0]
MF C26H25FN10OMW 512.54
Purity:
99%
Optical purity:
Optically pure
Soluble in DMSO
Description
Potent RET inhibitor (IC50 value <10 nM) with activity against wild-type RET and its mutants.
KEYWORDS: RET inhibitor 2667 | supplier | RET inhibitor | CAS [1980023-80-0] | RTK | GDNF | RET | Receptor tyrosine kinase | oncology | breast cancer | proliferation | | axonmedchem |
| EGFR Inhibitor [879127-07-8] - EGFR Inhibitor 324674 | Axon 1760
CAS [879127-07-8]
MF C21H18F3N5OMW 413.40
Purity:
99%
Soluble in DMSO
Description
A potent, cell permeable, irreversible and highly selective EGFR tyrosine kinase inhibitor with IC50 value in the nM range
References
Certificates
Categories
Extra info
Q Zhang et al. Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library. J. Am. Chem. Soc. 2006, 128(7), 2182-2183.
K Okamoto et al. Role of survivin in EGFR inhibitor-induced apoptosis in non-small cell lung cancers positive for EGFR mutations. Cancer Res. 2010, 70(24), 10402-10410.
Z Yu et al. Novel irreversible EGFR tyrosine kinase inhibitor 324674 sensitizes human colon carcinoma HT29 and SW480 cells to apoptosis by blocking the EGFR pathway. Biochem. Biophys. Res. Commun. 2011, 411(4), 751-756.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
EGFR
JAK-STAT
RTK class I; EC 2.7.10.1
Highly selective EGFR tyrosine kinase inhibitor
Chemical name
N-(3-(6-(3-(trifluoromethyl)phenylamino)pyrimidin-4-ylamino)phenyl)cyclopropanecarboxamide
Parent CAS No.
[879127-07-8]
Order
Size
Unit Price
Stock
5 mg
€125.00
In Stock | | axonmedchem |
| Poziotinib - HM781-36B | Axon 2920
CAS [1092364-38-9]
MF C23H21Cl2FN4O3MW 491.34
Purity:
99%
Soluble in DMSO
Description
Poziotinib is an irreversible pan-HER inhibitor with IC50 values of 0.0032 µM, 0.0053 µM and 0.0235 µM for HER1, HER2 and HER4, respectively. Poziotinib inhibited phosphorylation of HER family and downstream signaling molecules, and induced apoptosis and G1 arrest. Moreover, poziotinib demonstrated potent antitumor activity in HER2 amplified gastric cancer cells, HER2-amplified breast cancer cells, and erlotinib-resistant NSCLC.
KEYWORDS: Poziotinib | supplier | HER inhibitor | HM781-36B | CAS [1092364-38-9] | CAS[1429757-68-5] | Non Selective (Phosphorylation Substrates) | EGFR | ErbB2-HER2 | ErbB4-HER4 | Inhibitor | Receptors | Gastric cancer | NSCLC | Breast cancer | | axonmedchem |
| Tivozanib - AV 951 | KRN 951 | Axon 1717
CAS [475108-18-0]
MF C22H19ClN4O5MW 454.86
Purity:
98%
Moderately soluble in DMSO
Description
A highly potent and orally available tyrosine kinase inhibitor (TKI), targeting VEGFR1, 2 and 3, c-KIT and PDGFR (IC50: 0.21, 0.16, 0.24, 1.63 and 1.72 nM, respectively)
References
Certificates
Categories
Extra info
K Nakamura et al. KRN951, a Highly Potent Inhibitor of Vascular Endothelial Growth Factor Receptor Tyrosine Kinases, Has Antitumor Activities and Affects Functional Vascular Properties. Cancer Res. 2006, 66(18), 9134-9142.
Eri Taguchi et al. Anti-tumor activity and tumor vessel normalization by the vascular endothelial growth factor receptor tyrosine kinase inhibitor KRN951 in a rat peritoneal disseminated tumor model. Cancer Sci. 2008, 99(3), 623.
C Campas et al. Tivozanib. Drugs Fut. 2009, 34(10), 793.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
VEGFR
RTK class IV; EC 2.7.10.1
VEGFR1, 2, and 3 tyrosine kinase inhibitor
Chemical name
1-(2-chloro-4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-3-(5-methylisoxazol-3-yl)urea
Parent CAS No.
[475108-18-0]
Order
Size
Unit Price
Stock
5 mg
€99.00
In Stock | | axonmedchem |
| Pelitinib - EKB 569 | Axon 1665
CAS [257933-82-7 ]
MF C24H23ClFN5O2MW 467.92
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
An irreversible inhibitor of EGFR tyrosine kinase with potential antineoplastic activity. Pelitinib irreversibly binds covalently to EGFR ErbB-1, -2 and -4, thereby inhibiting receptor phosphorylation and signal transduction and resulting in apoptosis and suppression of proliferation in tumor cells that overexpress these receptors
References
Certificates
Categories
Extra info
M Nunes et al. Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an EGFR inhibitor, EKB-569, (...). Mol. Cancer Ther. 2004, 3,21.
C Erlichman et al. Phase I study of EKB-569, an irreversible inhibitor of the epidermal growth factor receptor, in patients with advanced solid tumors. J. Clin. Oncol. 2006, 24(15), 2252-2260.
A Ocaña and E Amir. Irreversible pan-ErbB tyrosine kinase inhibitors and breast cancer: current status and future directions. Cancer Treat Rev. 2009, 5(8), 685-691.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
EGFR
JAK-STAT
RTK class I; EC 2.7.10.1
EGFR tyrosine kinase inhibitor
Chemical name
(E)-N-(4-(3-chloro-4-fluorophenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-4-(dimethylamino)but-2-enamide
Parent CAS No.
[257933-82-7 ]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| Regorafenib - BAY 73-4506 | Stivarga | Axon 1678
CAS [755037-03-7]
MF C21H15ClF4N4O3MW 482.82
Purity:
98%
Soluble in DMSO
Description
An oral multi-kinase inhibitor which targets angiogenic, stromal and oncogenic receptor tyrosine kinases (RTK). Regorafenib shows anti-angiogenic activity due to its dual targeted VEGFR2-TIE2 tyrosine kinase inhibition
References
Certificates
Categories
Extra info
SM Wilhelm et al. Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int. J. Cancer. 2011, 129(1), 245-55.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
VEGFR
MAPK
c-KIT
RTK class III and IV; EC 2.7.10.1
RAF
Multi-kinase RTK inhibitor
Chemical name
4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide
Parent CAS No.
[755037-03-7]
Order
Size
Unit Price
Stock
5 mg
€75.00
In Stock | | axonmedchem |
| CP 547632 | Axon 1662
CAS [252003-65-9]
MF C20H24BrF2N5O3SMW 532.40
Purity:
98%
Soluble in DMSO
Description
A potent and oral tyrosine kinase inhibitor (TKI), targeting VEGFR2 and basic FGF kinases (IC50 to be 11 and 9 nM respectively); selective relative to EGFR, PDGF-ß, and other related TKs; inhibits VEGF-stimulated autophosphorylation of VEGFR2 in a whole cell assay with an IC50 value of 6 nM
References
Certificates
Categories
Extra info
JS Beebe et al. Pharmacological Characterization of CP-547,632, a Novel Vascular Endothelial Growth Factor Receptor-2 Tyrosine Kinase Inhibitor for Cancer Therapy. Cancer Res. 2003, 63, 7301-7309.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
VEGFR
RTK class IV; EC 2.7.10.1
VEGFR2 tyrosine kinase inhibitor
Chemical name
3-(4-bromo-2,6-difluorobenzyloxy)-5-(3-(4-(pyrrolidin-1-yl)butyl)ureido)isothiazole-4-carboxamide
Parent CAS No.
[252003-65-9]
Order
Size
Unit Price
Stock
2 mg
€105.00
In Stock | | axonmedchem |
| AEE 788 - NVP-AEE 788 | Axon 1653
CAS [497839-62-0]
MF C27H32N6MW 440.58
Purity:
98%
Optical purity:
>98% ee
Soluble in 0.1N HCl(aq) and DMSO
Description
A dual family EGFR/ErbB2 and VEGFR kinase inhibitor with antitumor and antiangiogenic activity
References
Certificates
Categories
Extra info
P Traxier, PR Allegrini, R Brandt et al. AEE788: A dual family EGFR/ErbB2 and VEGFR kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res. 2004, 64, 4931-4941.
D Meco et al. Dual Inhibitor AEE788 Reduces Tumor Growth in Preclinical Models of Medulloblastoma. Transl. Oncol. 2010, 3(5), 326-335.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
EGFR
VEGFR
ErbB2-HER2
JAK-STAT
RTK class I and IV; EC 2.7.10.1
EGFR, ErbB2 and VEGFR tyrosine kinase inhibitor
Chemical name
(R)-6-(4-((4-ethylpiperazin-1-yl)methyl)phenyl)-N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
Parent CAS No.
[497839-62-0]
Order
Size
Unit Price
Stock
5 mg
€95.00
In Stock | | axonmedchem |
| ABT 869 - Linifanib | Axon 1638
CAS [796967-16-3]
MF C21H18FN5OMW 375.40
Purity:
99%
Soluble in DMSO
Description
A multi-targeted receptor tyrosine kinase (RTK) inhibitor, targeting VEGRFs, PDGFRs, Fms-like tyrosine kinase-3 and c-KIT. In cellular assays ABT869 inhibits RTK phosphorylation (IC50 = 2, 4, and 7 nM for PDGFR-β, KDR, and CSF-1R, respectively) and VEGF-stimulated proliferation (IC50 = 0.2 nM for human endothelial cells)
References
Certificates
Categories
Extra info
DH Albert et al. Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol. Cancer Ther. 2006, 5, 995-1006.
J Zhou et al. ABT-869, a promising multi-targeted tyrosine kinase inhibitor: from bench to bedside. J. Hematol. Oncol. 2009, 2, 33.
AK Ikeda et al. ABT-869 inhibits the proliferation of Ewing Sarcoma cells and suppresses platelet-derived growth factor receptor beta and c-KIT signaling pathways. Mol. Cancer Ther. 2010, 9(3), 653-60.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
FLT3
VEGFR
PDGFR
c-KIT
RTK class III and IV; EC 2.7.10.1
PDGFR, c-KIT and VEGFR tyrosine kinase inhibitor
Chemical name
1-(4-(3-amino-1H-indazol-4-yl)phenyl)-3-(2-fluoro-5-methylphenyl)urea
Parent CAS No.
[796967-16-3]
Order
Size
Unit Price
Stock
5 mg
€85.00
In Stock | | axonmedchem |
| Vatalanib - PTK 787 | Axon 1637
CAS [212141-54-3]
MF C20H15ClN4MW 346.81
Purity:
98%
Soluble in DMSO
Description
A potent and selective inhibitor of tyrosine kinases, targeting VEGFR, with IC50 to be 77 nM (VEGFR1), 37 nM (VEGFR2), 580 nM (PDGFR-β), 730 nM (c-KIT), 660 nM (FLT-4) and 1.4 µM (c-FMS) respectively; not active against EGFR, SRC-ABL and PKC etc
References
Certificates
Categories
Extra info
JM Wood et al. PTK787/ZK 222584, a Novel and Potent Inhibitor of Vascular Endothelial Growth Factor Receptor Tyrosine Kinases (...). Cancer Res. 2000, 60, 2178-2189.
EN Scott et al. Vatalanib: the clinical development of a tyrosine kinase inhibitor of angiogenesis in solid tumours. Expert Opin Investig Drugs 2007, 16(3), 367–379.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
VEGFR
RTK class IV; EC 2.7.10.1
VEGFR tyrosine kinase inhibitor
Chemical name
N-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine
Parent CAS No.
[212141-54-3]
Order
Size
Unit Price
Stock
10 mg
€75.00
In Stock | | axonmedchem |
| OSI 420 - Erlotinib, 6-O-Desmethyl- | Axon 1632
CAS [183321-86-0]
MF C21H21N3O4MW 379.41
Purity:
98%
Soluble in DMSO
Description
An active O-desmethyl metabolite of Erlotinib (Axon 1128), which inhibits EGFR tyrosine kinase; precursor of [11C]-labelled Erlotinib for PET study
References
Certificates
Categories
Extra info
A Broniscer et al. Plasma and cerebrospinal fluid pharmacokinetics of erlotinib and its active metabolite OSI-420. Clin. Cancer Res. 2007, 13(5), 1511-1515.
Y Togashi et al. Cerebrospinal Fluid Concentration of Erlotinib and its Active Metabolite OSI-420 in Patients with Central Nervous System Metastases of Non-small Cell Lung Cancer. J. Thoracic Oncol. 2010, 5(7), 950-955.
I. Bahce et al. Development of [(11)C]erlotinib positron emission tomography for in vivo evaluation of EGF receptor mutational status. Clin. Cancer Res. 2013, 19, 183-193.
NF Smith et al. Modulation of erlotinib pharmacokinetics in mice by a novel cytochromeP450 3A4 inhibitor, BAS 100. Br. J. Cancer 2008, 98, 1630–1632.
AA Memon et al. Positron Emission Tomography (PET) Imaging with [11C]-Labeled Erlotinib: A Micro-PET Study on Mice with Lung Tumor Xenografts. Cancer Res. 2009, 69(3), 873-878.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
EGFR
JAK-STAT
RTK class I; EC 2.7.10.1
EGFR tyrosine kinase inhibitor
Chemical name
2-(4-(3-ethynylphenylamino)-7-(2-methoxyethoxy)quinazolin-6-yloxy)ethanol
Parent CAS No.
[183321-86-0]
Order
Size
Unit Price
Stock
2 mg
€90.00
In Stock | | axonmedchem |
| OSI 930 | Axon 1547
CAS [728033-96-3]
MF C22H16F3N3O2SMW 443.44
Purity:
99%
Soluble in DMSO
Description
A potent and orally active inhibitor of tyrosine kinases, targeting c-KIT and VEGFR2; OSI-930 is designed to target both cancer cell proliferation and blood vessel growth (angiogenesis) in selected tumors
References
Certificates
Categories
Extra info
AJ Garton et al. OSI-930: A Novel Selective Inhibitor of Kit and Kinase Insert Domain Receptor Tyrosine Kinases with Antitumor Activity in Mouse Xenograft Models. Cancer Res 2006, 66(2), 1015-1024.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
VEGFR
c-KIT
RTK class III and IV; EC 2.7.10.1
c-Kit and VEGFR2 tyrosine kinase inhibitor
Chemical name
3-(quinolin-4-ylmethylamino)-N-(4-(trifluoromethoxy)phenyl)thiophene-2-carboxamide
Parent CAS No.
[728033-96-3]
Order
Size
Unit Price
Stock
5 mg
€90.00
In Stock | | axonmedchem |
| BIBW 2992 - Afatinib | Axon 1544
CAS [850140-72-6]
MF C24H25ClFN5O3MW 485.94
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
Second generation tyrosine kinase inhibitor (TKI) that irreversibly inhibits human epidermal receptor 2 (Her2 or ErbB 2) and EGFR (HER1) kinases. An investigational drug for breast cancer as well as other EGFR and Her2 driven cancers such as NSCLC and Head-and-Neck
KEYWORDS: BIBW 2992 | supplier | EGFR/HER2 inhibitor | 850140-72-6 | 439081-18-2 | Afatinib | BIBW2992 | BIBW-2992 | EGFR | ErbB2-HER2 | TKI | breast cancer | epidermal | growft factor | | axonmedchem |
| Neratinib - HKI 272 | Axon 1526
CAS [698387-09-6]
MF C30H29ClN6O3MW 557.04
Purity:
98%
Soluble in 0.1N HCl(aq) and DMSO
Description
An irreversible tyrosine kinase inhibitor with activity against HER2 and EGFR kinases; a therapeutic agent under investigation for the treatment breast cancer and other solid tumors.
KEYWORDS: Neratinib | supplier | EGFR/HER2 inhibitor | HKI 272 | HKI272 | CAS [698387-09-6] | EGFR | ErbB2-HER2 | RTK | breast cancer | solid tumors | NSCLC | growth factor receptor | | axonmedchem |
| Cediranib - AZD 2171 | Axon 1461
CAS [288383-20-0]
MF C25H27FN4O3MW 450.51
Purity:
99%
Soluble in DMSO
Description
highly potent and orally available tyrosine kinase inhibitor (TKI), targeting VEGF receptor; thereby blocking VEGF-signaling, angiogenesis, and tumor cell growth
References
Certificates
Categories
Extra info
SR Wedge et al. AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer. Cancer Res. 2005, 65 (10), 4389–400.
G Goss et al. A phase I and pharmacokinetic study of daily oral cediranib, an inhibitor of vascular endothelial growth factor tyrosine kinases, in combination with cisplatin and gemcitabine. Eur. J. Cancer 2008, 45, 782.
P Nikolinakos & JV Heymach. The tyrosine kinase inhibitor cediranib for non-small cell lung cancer and other thoracic malignancies. J. Thorac. Oncol. 2008, 3 (6 Suppl 2): S131–4.
CA Heckman et al. The tyrosine kinase inhibitor cediranib blocks ligand-induced vascular endothelial growth factor receptor-3 activity and lymphangiogenesis. Cancer Res. 2008, 68(12), 4754-4762.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
VEGFR
RTK class IV; EC 2.7.10.1
VEGFR tyrosine kinase inhibitor
Chemical name
4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-6-methoxy-7-(3-pyrrolidin-1-yl-propoxy)-quinazoline
Parent CAS No.
[288383-20-0]
Order
Size
Unit Price
Stock
5 mg
€70.00
In Stock | | axonmedchem |
| WZ 4002 | Axon 1506
CAS [1213269-23-8]
MF C25H27ClN6O3MW 494.97
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
A mutant-selective EGFR kinase inhibitor against EGFR T790M; a potential agent for some drug-resistant non-small cell lung cancers
References
Certificates
Categories
Extra info
W Zhou et al. Novel mutant-selective EGFR kinase inhibitors against EGFR T790M. Nature 2009, 462, 1070-1074.
Y Sakuma et al. WZ4002, a third-generation EGFR inhibitor, can overcome anoikis resistance in EGFR-mutant lung adenocarcinomas more efficiently than Src inhibitors. Laboratory Investigation 2012, 92, 371-383.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
EGFR
JAK-STAT
RTK class I; EC 2.7.10.1
EGFR kinase inhibitor (T790M specific)
Chemical name
N-(3-(5-chloro-2-(2-methoxy-4-(4-methylpiperazine-1-yl)phenylamino)pyrimidin-4yloxy)phenyl)acrylam
Parent CAS No.
[1213269-23-8]
Order
Size
Unit Price
Stock
5 mg
€70.00
In Stock | | axonmedchem |
| CI 1033 - Canertinib dihydrochloride | Axon 1433
CAS [289499-45-2]
MF C24H25ClFN5O3.2HClMW 558.86
Purity:
99%
Soluble in water and DMSO
Description
An orally bioavailable tyrosine kinase inhibitor, targeting EGFR, irreversibly inhibiting their signal transduction functions and resulting in tumor cell apoptosis and suppression of tumor cell proliferation; water-soluble form
References
Certificates
Categories
Extra info
PA. Jänne et al. Multicenter, Randomized, Phase II Trial of CI-1033, an Irreversible Pan-ERBB Inhibitor, for Previously Treated Advanced Non–Small-Cell Lung Cancer. J. Clinic. Oncology, 2007, 25(25), 3936-3944.
E Calvo et al. Administration of CI-1033, an Irreversible Pan-erbB Tyrosine Kinase Inhibitor, Is Feasible on a 7-Day On, 7-Day Off Schedule. A Phase I Pharmacokinetic and Food Effect Study. Clinical Cancer Research 2004, 10, 7112-7120.
LV Sequist. Second-Generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non-Small Cell Lung Cancer. The Oncologist, 2007, 12(3), 325-330.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Apoptosis
Cell Signaling & Oncology
EGFR
JAK-STAT
RTK class I; EC 2.7.10.1
EGFR tyrosine kinase inhibitor
Chemical name
N-[4-(3-Chloro-4-fluoro-phenylamino)-7-(3-morpholin-4-yl-propoxy)-quinazolin-6-yl]-acrylamide dihydrochloride
Parent CAS No.
[267243-28-7]
Order
Size
Unit Price
Stock
5 mg
€60.00
In Stock | | axonmedchem |
| GW 786034 - Pazopanib hydrochloride | Axon 1420
CAS [635702-64-6]
MF C21H23N7O2S.HClMW 473.98
Purity:
98%
Soluble in DMSO
Description
A potent and selective inhibitor of tyrosine kinases, targeting VEGFR/c-KIT/PDGFR, blocking angiogenesis; as an oral antineoplastic agent
References
Certificates
Categories
Extra info
G Sonpavde et al. Pazopanib, a potent orally administered small-molecule multitargeted tyrosine kinase inhibitor for renal cell carcinoma. Exp. Opin. Invest. Drugs. 2008, 17(2), 253-261.
G Sonpavde and TE Hutson. Pazopanib: a novel multitargeted tyrosine kinase inhibitor. Curr. Oncol. Rep. 2007, 9(2), 115-9.
K Podar et al. The small-molecule VEGF receptor inhibitor pazopanib (GW786034B) targets both tumor and endothelial cells in multiple myeloma. Proc. Natl. Acad. Sci. USA. 2006, 103(51), 19478-19483.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
VEGFR
PDGFR
c-KIT
RTK class III and IV; EC 2.7.10.1
PDGFR, c-KIT and VEGFR tyrosine kinase inhibitor
Chemical name
5-{4-[(2,3-Dimethyl-2H-indazol-6-yl)-methyl-amino]-pyrimidin-2-ylamino}-2-methyl-benzenesulfonamide hydrochloride
Parent CAS No.
[444731-52-6]
Order
Size
Unit Price
Stock
5 mg
€70.00
In Stock | | axonmedchem |
| AG 013736 - Axitinib | Axon 1414
CAS [319460-85-0]
MF C22H18N4OSMW 386.47
Purity:
99%
Soluble in DMSO
Description
A tyrosine kinase inhibitor (TKI), targeting VEGFR/PDGFR/c-KIT; orally bioavailable drug exerting an anti-angiogenic effect.
KEYWORDS: AG 013736 | supplier | VEGFR inhibitor | Axitinib | AG013736 | AG-013736 | AG-13736 | CAS [319460-85-0] | SCF | PDGF | VEGF | c-KIT | PDGFR | VEGFR | Tyrosine kinase inhibitor | TKI | RTK | orally bioavailable | anti-angiogenic | | axonmedchem |
| Sunitinib malate - SU 11248 | Sutent | Axon 1398
CAS [341031-54-7]
MF C22H27FN4O2.C5H8O4MW 530.59
Purity:
99%
Soluble in DMSO
Description
Small molecule multi-targeted receptor tyrosine kinase (RTK) inhibitor. Sunitinib inhibits cellular signaling by targeting multiple RTKs, including PDGF-R/VEGF-R.
KEYWORDS: Sunitinib malate | supplier | PDGFR inhibitor | SU 11248 | Sutent | SU11248 | SU-11248 | CAS [341031-54-7] | [557795-19-4] | SCF | PDGF | VEGF | c-KIT | PDGFR | VEGFR | RTK | receptor tyrosine kinase | | axonmedchem |
| Vandetanib - ZD 6474 | Axon 1411
CAS [443913-73-3]
MF C22H24BrFN4O2MW 475.35
Purity:
99%
Soluble in 0.1N HCl(aq) and DMSO
Description
An orally bioavailable tyrosine kinase inhibitor (TKI), targeting VEGFR, EGFR, and RET; a potential medication for non-small-cell lung cancer.
References
Certificates
Categories
Extra info
RS Herbst et al. Vandetanib (ZD6474): an orally available receptor tyrosine kinase inhibitor that selectively targets pathways critical for tumor growth and angiogenesis. Expert Opin. Investig. Drugs. 2007, 16, 239-249.
SR Wedge et al. ZD6474 inhibits vascular endothelial growth factor signaling, angiogenesis, and tumor growth following oral administration. Cancer Res. 2002, 62, 4645-4655.
D. Vitagliano et al. The tyrosine kinase inhibitor ZD6474 blocks proliferation of RET mutant medullary thyroid carcinoma cells. Endocr Relat Cancer. 2010 Nov 30;18(1):1-11.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
EGFR
VEGFR
JAK-STAT
RTK class I and IV; EC 2.7.10.1
VEGFR and EGFR tyrosine kinase inhibitor
Chemical name
(4-Bromo-2-fluoro-phenyl)-[6-methoxy-7-(1-methyl-piperidin-4-ylmethoxy)-quinazolin-4-yl]-amine
Parent CAS No.
[443913-73-3]
Order
Size
Unit Price
Stock
5 mg
€55.00
In Stock | | axonmedchem |
| EAI045 | Axon 2680
CAS [1942114-09-1]
MF C19H14FN3O3SMW 383.40
Purity:
99%
Soluble in DMSO
Description
EAI045 is an allosteric inhibitor that targets drug-resistant L858R/T790M-mutant EGFR tyrosine kinase (IC50 value of 3 nM), and spares the wild-type receptor (~1000-fold selectivity versus wild-type EGFR at 1 mM ATP).
KEYWORDS: EAI045 | supplier | Allosteric EGFR L858R/T790M inhibitor | EAI 045 | EAI-045 | CAS [1942114-09-1] | EGF | EGFR | Inhibitor | Receptors | | axonmedchem |
| Lapatinib ditosylate - GW 572016 | Axon 1395
CAS [388082-77-7]
MF C29H26ClFN4O4S.2C7H8O3SMW 925.46
Purity:
99%
Soluble in DMSO
Description
An ATP-competitive epidermal growth factor receptor (EGFR) and HER2/neu (ErbB-2) dual tyrosine kinase inhibitor
References
Certificates
Categories
Extra info
HA Burris. Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib. Oncologist 2004, 9 Suppl 3: 10–5.
MH Nelson, CR Dolder. Lapatinib: a novel dual tyrosine kinase inhibitor with activity in solid tumors. Ann Pharmacother 2006, 40(2), 261–9.
Certificate of Analysis
Material Safety Data Sheet
Angiogenesis
Cell Signaling & Oncology
EGFR
ErbB2-HER2
JAK-STAT
RTK class I; EC 2.7.10.1
EGFR and ErbB-2/HER2 tyrosine kinase inhibitor
Chemical name
N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]-2-furyl]
quinazolin-4-amine ditosylate
Parent CAS No.
[231277-92-2]
Order
Size
Unit Price
Stock
10 mg
€95.00
In Stock | | axonmedchem |