|Description||PF-04217903 methanesulfonate is a selective ATP-competitive c-Met inhibitor and is susceptible to oncogenic mutations (no activity to Y1230C mutant). It showed more than 1000-fold greater selectivity against c-Met kinase over 150 other kinases. It displays similar potency to inhibit the activity of c-Met-H1094R, c-Met-R988C, and c-Met-T1010I, but has no inhibitory activity against c-Met-Y1230C. It showed antitumor activity in tumor models where c-Met is activated by mechanisms including c-Met gene amplification, HGF/c-Met autocrine loop formation or c-Met overexpression. It suppressed proliferation of c-Met-amplified GTL-16 and H1993cells. It induced apoptosis in GTL-16 cells. It inhibited the phosphorylation of c-Met and suppressed tumor growth.|
|Synonyms||PF-04217903 methanesulfonate; PF 04217903 methanesulfonate; PF04217903 methanesulfonate|
NVP-BVU972 potently inhibits MET kinase but displays low inhibition against other kinases including the most closely related kinase RON with IC50 values of more...
PF-04136309 is an orally available human chemokine receptor 2 (CCR2) antagonist with potential immunomodulating and antineoplastic activities. Upon oral adminis...
LY2801653 is an orally available, small molecule inhibitor of the proto-oncogene c-Met with potential antineoplastic activity.
Tepotinib, also known as EMD 1214063 and MSC2156119, is an inhibitor of MET tyrosine kinase with potential antineoplastic activity. MET tyrosine kinase inhibito...
BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7 nM/15 nM.
The hydrochloride salt form of Glesatinib, an inhibitor of tyrosine kinase, could be effectively targeting tumors that are driving to grow through MET and AXL r...
LY2801653 is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a dissociation constant (K(i)) of 2 nM, a pharmacodynamic residence time ...
SGX523 is a novel, ATP-competitive kinase inhibitor remarkable for its exquisite selectivity for MET. SGX523 potently inhibited MET with an IC50 of 4 nmol/L an...