| 产品详情 |
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| Product Name | PLX647 |
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| Description | Purity >98%. PLX647 is a dual inhibitor of the receptor tyrosine kinases FMS and KIT (IC50 s = 28 and 16 nM, respectively). It is selective for FMS and KIT but does inhibit FLT3 and KDR (IC50 s = 91 and 130 nM, respectively) in a panel of 400 kinases at a concentration of 1 µM. PLX647 inhibits proliferation of Ba/F3 cells expressing constitutively active FMS or KIT (IC50 s = 92 and 180 nM, respectively) as well as ligand-dependent growth of M-NFS-60 and M-07e cells that express endogenous FMS and KIT, respectively (IC50 s = 380 and 230 nM, respectively). It has no effect on HEK293T or HepG2 cells that lack FMS and KIT (IC50 = >50 µM) or Ba/F3 cells overexpressing KDR (IC50 = >5 µM). PLX647 also inhibits differentiation of human osteoclast precursor cells (IC50 = 170 nM). In vivo, PLX647 (40 mg/kg) reduces TNF-Alpha and IL-6 release in a rat model of LPS-induced cytokine release. It reduces mast cell degranulation in a mouse model of passive cutaneous anaphylaxis (PCA) and inhibits bone destruction and delays disease progression in a mouse model of collagen-induced arthritis (CIA). PLX647 also reverse bone osteolysis and allodynia in a syngeneic rat model of cancer-induced bone pain. |
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| Size | n/a |
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| Concentration | n/a |
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| Applications | n/a |
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| Other Names | 5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-2-pyridinamine |
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| Gene, Accession, CAS # | CAS: 873786-09-5 |
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| Catalog # | LS-H9460 |
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| Order / More Info | PLX647 from LIFESPAN BIOSCIENCES INC. |
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| Product Specific References | n/a |
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