c-Met

c-Met is a receptor for HGF (Hepatocyte growth factor) which is essential during many biological processes. The HGF / MET pathway is an excellent target for anti-cancer therapies. Activation of MET results in the recruitment of scaffolding proteins like Gab1 and Grb2, leading to the recruitment of SH2-domain containing signal transducers that in turn activate a number of pathways, like MAPK or PI3K. Branching morphogenesis, the most complex biological response induced by Met requires all signaling pathways and targets including MAPK, Gab1, Grb2, PI3K, Shp2, SH2 (Src-homology-2), Sos (son-of-sevenless), and PLC (phospholipase C).

Inhibitors

Cat.No. Product Name Information Publication Customer Review
S1111 Foretinib (GSK1363089, XL880) XL880 (GSK1363089, EXEL-2880) is an ATP-competitive inhibitor of MET and KDR with IC50 of 0.4 nM and 0.9 nM, respectively. (3)
S1070 PHA-665752 PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM. (5)
S1080 SU11274 SU11274 is a selective Met inhibitor with IC50 of 10 nM. (8)
S1094 PF-04217903 PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM. (1)
S1112 SGX-523 SGX-523 is a selective Met inhibitor with IC50 of 4 nM. (4)
S1561 BMS 777607 BMS-777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively.
S2753 ARQ 197 (Tivantinib) ARQ-197 is a novel and selective human c-Met inhibitor with IC50 of 0.1 μM.
S7067 EMD 1214063 EMD 1214063 is a potent and selective c-Met inhibitor with IC50 of 6 nM.
S2859 Golvatinib (E7050) E7050 is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, respectively.
S2788 INCB28060 INCB28060 is a novel, ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM.
S2774 MK-2461 MK-2461 is a potent inhibitor of c-Met, Ron, Flt1/3, PDGFRβ, Mer and FGFR1/2/3 with IC50 of 2.5 nM, 7 nM, 10 nM/22 nM, 22 nM, 24 nM and 65 nM/39 nM/50 nM, respectively.

c-Met

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