Chemical Structure : PF-04217903
CAS No.: 956905-27-4
货号: PC-42832Not For Human Use, Lab Use Only.
PF-04217903 is a potent, selective, ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM, inhibits HGF-stimulated tyrosine phosphorylation of wild type c-Met with IC50 of 7.3 nM in cell-based assays.
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PF-04217903 is a potent, selective, ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM, inhibits HGF-stimulated tyrosine phosphorylation of wild type c-Met with IC50 of 7.3 nM in cell-based assays.
PF-04217903 shows similar potency for inhibition of c-Met phosphorylation in mIMCD3 mouse epithelial cells (IC50=6.9 nM) and MDCK cell (IC50=9.5 nM).
PF-04217903 also exhibits inhibitory activities against c-Met mutations including V1092I, H1094R, M1250T, R988C, and T11010I (IC50=530 nM), but has little to no activity against mutants Y1230C and Y1235D.
PF-04217903 inhibits tumor cell proliferation, survival, migration/invasion both in vitro and in vivo.
分子量 | 372.3833 | |
分子式 | C19H16N8O | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
1H-Pyrazole-1-ethanol, 4-[1-(6-quinolinylmethyl)-1H-1,2,3-triazolo[4,5-b]pyrazin-6-yl]- |
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4. Yeh I, et al. Nat Commun. 2015 May 27;6:7174.
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