human c-met

PF-04217903 methanesulfonate is a potent ATP-competitive inhibitor of c-Met kinase (Ki of 4.8 nM for human c-Met).

PF-04217903 phenolsulfonate is a potent, ATP-competitive inhibitor of c-Met kinase with a Ki of 4.8 nM for human c-Met.

AMG-458 is a potent c-Met inhibitor with Ki of 1.2 nM, ~350-fold selectivity for c-Met than VEGFR2 in cells.

Norcantharidin (Norcantharadine) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.

Capmatinib 2HCl (INC-280 2HCl) is a novel, ATP-competitive inhibitor of c-MET kinase with an IC50 with 0.13 nM.Capmatinib 2HCl exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10, 000-fold selectivity over a large panel of human kinases. This inhibitor potently blocks c-MET phosphorylation and activation of its key downstream effectors in c-MET-dependent tumor cell lines. As a result, Capmatinib 2HCl potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis in vitro.

(±)-Norcantharidin (Endothall anhydride) is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers.

Anticanceragent 276 (Compound 5) is a multitarget anticancer compound. It exhibits potent antitumor activity against human cancer cells, with IC50 values of 6.90 μM for HEPG2 cells and 4.48 μM for MCF7 cells. Anticanceragent 276 interacts strongly and stably with multiple targets, including topoisomerase II, VEGFR2, c-Met, EGFR, and ERα.

1. Herbacetin induces apoptosis in HepG2 cells, by ROS and PI3K/Akt pathway. 2. Herbacetin suppresses the HGF-induced motility of human breast cancer MDA-MB-231 cells by inhibiting c-Met and Akt phosphorylation.

KRC-108 is a multiple kinase inhibitor. KRC-108 is a potent inhibitor of Ron, Flt3 and TrkA as well as c-Met. KRC-108 inhibited oncogenic c-Met M1250T and Y1230D more strongly than wild type c-Met. The anti-proliferative activity of KRC-108 was measured by performing a cytotoxicity assay on a panel of cancer cell lines. The GI(50) values (i.e., 50% inhibition of cell growth) for KRC-108 ranged from 0.01 to 4.22 μM for these cancer cell lines. KRC-108 was also effective for the inhibition of tumor growth in human HT29 colorectal cancer and NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice. This molecule should serve as a useful lead for inhibitors targeting kinases and may lead to new therapeutics for the treatment of cancer. (source: Invest New Drugs. 2012 Apr;30(2):518-23. doi: 10.1007/s10637-010-9584-2. Epub 2010 Nov 16. ).

Ficlatuzumab is a humanized monoclonal antibody that specifically targets and neutralizes the biological activity of human hepatocyte growth factor (HGF), by inhibiting HGF, Ficlatuzumab effectively blocks c-Met receptor-mediated downstream signaling pathways responsible for cancer cell proliferation, migration, and invasion, demonstrating applicable use for the treatment of squamous cell carcinoma.

SYN1143 (AMG-1) is a potent inhibitor of human RON and c-Met.In vitro kinase assays showed that compound I is a potent inhibitor of human RON and c-Met with IC50s of 9 and 4 nmol/L, respectively.

Anti-HGFR/c-Met Antibody is a human-derived antibody expressed in CHO cells, targeting HGFR/c-Met. It possesses a huIgG1 heavy chain and a huλ light chain, with an estimated molecular weight (MW) of 150 kDa. For isotype control, refer to Human IgG1 kappa, Isotype Control.