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| Product Name: | PLX647 | | Synonyms: | PLX647;PLC647;5-(1H-Pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-2-pyridinamine;[5-[(1H-Pyrrolo[2,3-b]pyridin-3-yl)methyl]pyridin-2-yl](4-trifluoromethylbenzyl)amine;2-Pyridinamine, 5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethyl)-N-[[4-(trifluoromethyl)phenyl]methyl]-;PLX 647;PLX-647;CS-1696;5-({1H-pyrrolo[2,3-b]pyridin-3-yl}methyl)-N-{[4-(trifluoromethyl)phenyl]methyl}pyridin-2-amine | | CAS: | 873786-09-5 | | MF: | C21H17F3N4 | | MW: | 382.38 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 873786-09-5.mol |  |
| | PLX647 Chemical Properties |
| density | 1.358±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: soluble20mg/mL, clear | | form | powder | | pka | 13.73±0.40(Predicted) | | color | white to beige |
| | PLX647 Usage And Synthesis |
| Description | PLX647 is a dual inhibitor of the receptor tyrosine kinases FMS and KIT (IC50s = 28 and 16 nM, respectively). It is selective for FMS and KIT but does inhibit FLT3 and KDR (IC50s = 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 (IC50s = 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 (IC50s = 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-α 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 reverses bone osteolysis and allodynia in a syngeneic rat model of cancer-induced bone pain. | | Uses | PLX647 is a novel tyrosine kinase (TK) inhibitor, which selectively targets c-Kit and c-Fms. | | references | [1]. zhang c, ibrahim pn, zhang j, et al. design and pharmacology of a highly specific dual fms and kit kinase inhibitor. proc natl acad sci u s a, 2013, 110(14): 5689-5694. |
| | PLX647 Preparation Products And Raw materials |
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