产品名称 PND 1186 - SR 2516 | VS 4718
产品货号 Axon 2459 CAS [1061353-68-1] MF C25H26F3N5O3MW 501.50 Purity: 100% Soluble in DMSO Description Orally active dual FAK/PYK2 inhibitor (IC50 value 1.5 nM and ~100 nM in vitro and in vivo, respectively) that blocks FAK and p130Cas (130 kDa Crk-associated substrate) tyrosine phosphorylation, promotes caspase-3 activation, and selectively triggered cell apoptosis in tumor cells in 3D environments. PND1186 inhibitory effects differ from Dasatinib (Axon 1392; as it does not affect c-Src activity), and prevents spontaneous breast to lung metastasis in pre-clinical models. PND-1186 inhibits cell growth in multiple myeloma (MM) cells both in vitro and in vivo by inhibition of PYK2 (IC50 and EC50 values 85 nM and 20 nM, respectively). References Certificates Categories Extra info I. Tanjoni et al. PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environments. Cancer Biol Ther. 2010 May 15;9(10):764-77.   C. Walsh et al. Oral delivery of PND-1186 FAK inhibitor decreases tumor growth and spontaneous breast to lung metastasis in pre-clinical models. Cancer Biol Ther. 2010 May 15;9(10):778-90.   Y. Zhang et al. Pyk2 promotes tumor progression in multiple myeloma. Blood. 2014 Oct 23;124(17):2675-86. Certificate of Analysis Material Safety Data Sheet Apoptosis Cell Cycle Regulation Cell Signaling & Oncology FAK PYK2 Wnt-β-Catenin MAPK EC 2.7.10.2 Orally active dual FAK/PYK2 inhibitor triggering cell apoptosis in tumor cells Chemical name 2-(2-(2-methoxy-4-morpholinophenylamino)-5-(trifluoromethyl)pyridin-4-ylamino)-N-methylbenzamide Parent CAS No. [1061353-68-1] Order Size Unit Price Stock 5 mg €105.00 In Stock
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PND 1186 - SR 2516 | VS 4718

Based on 8 reference(s) in Google Scholar 9 10 8

Axon 2459

CAS [1061353-68-1]

MF C25H26F3N5O3
MW 501.50

  • Purity: 100%
  • Soluble in DMSO

PND 1186

Description

Orally active dual FAK/PYK2 inhibitor (IC50 value 1.5 nM and ~100 nM in vitro and in vivo, respectively) that blocks FAK and p130Cas (130 kDa Crk-associated substrate) tyrosine phosphorylation, promotes caspase-3 activation, and selectively triggered cell apoptosis in tumor cells in 3D environments. PND1186 inhibitory effects differ from Dasatinib (Axon 1392; as it does not affect c-Src activity), and prevents spontaneous breast to lung metastasis in pre-clinical models. PND-1186 inhibits cell growth in multiple myeloma (MM) cells both in vitro and in vivo by inhibition of PYK2 (IC50 and EC50 values 85 nM and 20 nM, respectively).

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