PF-04217903 mesylate

Description: PF-04217903 mesylate, the methanesulfonate salt of PF-04217903, is a novel, potent, orally bioavailabe, selective, and ATP-competitive small-molecule tyrosine kinase inhibitor of c-Met with IC50 of 4.8 nM in A549 cell line and with anticancer activity, it is susceptible to oncogenic mutations (with no activity to Y1230C mutant). PF-04217903 selectively binds to and inhibits c-Met, disrupting the c-Met signaling pathway, which may result in the inhibition of tumor cell growth, migration and invasion of tumor cells, and the induction of death in tumor cells expressing c-Met.

References: Biochemistry. 2009; 48(23):5339-49; Cancer Res. 2010; 70(24):10090-100; Eur J Cancer. 2011; 47(8):1231-43.

Related CAS: 956905-27-4 (free base)

Chemical Name: 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1, 2, 3]triazolo[4, 5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol mesylate

InChi Key: HBEMHKVWZJTVOC-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H16N8O.CH4O3S/c28-7-6-26-12-15(9-22-26)17-10-21-18-19(23-17)27(25-24-18)11-13-3-4-16-14(8-13)2-1-5-20-16; 1-5(2, 3)4/h1-5, 8-10, 12, 28H, 6-7, 11H2; 1H3, (H, 2, 3, 4)

SMILES Code: OCCN1N=CC(C2=CN=C3C(N(CC4=CC=C5N=CC=CC5=C4)N=N3)=N2)=C1.OS(=O)(C)=O