c-met (mouse)

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

Crizotinib (PF-02341066) is an ATP-competitive small-molecule tyrosine kinase inhibitor of c-MET (IC50: 8 nM) and ALK (IC50: 20 nM) receptors.

KRC-00715 is an orally effective inhibitor of c-Met, exhibiting high selectivity with an IC50 of 9.0 nM. This compound specifically inhibits the growth of gastric cancer cell lines with high c-Met expression by inducing G1/S phase block, and reduces the activity of downstream signals, including Akt, Erk, and c-Met itself. In the gastric cancer cell line Hs746T, KRC-00715 demonstrates cytotoxicity with an IC50 of 39 nM and selectively inhibits the proliferation of cell lines that overexpress c-Met. Additionally, KRC-00715 decreases tumor size in Hs746T xenograft mouse models.

PROTACc-Met degrader-1 (Compound Met-DD4) is an orally effective PROTAC degrader targeting c-Met with a DC50 of 6.21 nM. It inhibits the proliferation of c-Met-addicted MKN-45 cells with an IC50 of 4.37 nM and causes cell cycle arrest in the G0/G1 phase. In a xenograft mouse model using MKN-45 cells, PROTACc-Met degrader-1 demonstrates antitumor activity.

Arylsulfonamide 64B (HIF inhibitor 64B), an inhibitor of the hypoxia-induced factor (HIF), not only suppresses hypoxia/HIF-induced expression of c-Met and CXCR4 but also decreases primary tumor growth and metastasis in a uveal melanoma mouse model [1].

PARP1/c-Met-IN-1 (Compound 16) serves as a selective dual inhibitor targeting both PARP1 and c-Met, demonstrating IC50 values of 3.3 nM and 32.2 nM, respectively. This compound effectively induces apoptosis and causes cell cycle arrest at the G2/M phase in MDA-MB-231 cells. Furthermore, PARP1/c-Met-IN-1 displays notable antitumor activity in mouse models [1].

AG01 is a monoclonal antibody targeting the anti-granular protein precursor (GP88). It inhibits the proliferation and migration of triple-negative breast cancer (TNBC) cells, reducing the expression of phosphorylated protein kinases such as p-Src, p-AKT, and p-ERK, as well as oncogenic proteins like Axl, c-MET, HIF-1α, and VEGF. In TNBC xenograft mouse models, AG01 suppresses tumor growth and the expression of Ki67 in vivo. AG01 is useful for research involving cancers like TNBC.