c-MET

SU11274 is a Met tyrosine kinase inhibitor.

AMG-458 is a potent inhibitor of c-Met with an IC50 value of 60nM and displays selectivity against VEGFR2.

TAS-115 is a potent VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively.

SRI 31215 (TFA), a triplex inhibitor of matriptase, hepsin and hepatocyte growth factor activator (HGFA) with IC50s of 0.69 μM, 0.65 μM, 0.3 μM, blocks pro-HGF activation and thus mimics the activity of HAI-1/2.

MK8033 Hcl is a novel and specific dual ATP competitive c-Met/Ron inhibitor (IC50=1 nM Wt c-Met) under investigation as a treatment for cancer.

SYN1143 is a potent, selective and orally active dual inhibitor of c-Met/RON, with IC50s of 4 and 9 nM, respectively.

BAY-474 is a tyrosine-protein kinase c-Met inhibitor. BAY-474 acts as an epigenetics probe.

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

XL092 is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values in cell-based assays of 15, 1.6, 3.4, and 7.2 nM respectively.

PRO-6E is a PROTAC that targets Cereblon to induce degradation of the MET protein. It achieves up to 81.9% degradation of MET at 1 μM in MKN-45 cells, effectively inhibiting tumor growth both in vitro and in vivo. Additionally, PRO-6E promotes apoptosis and cell cycle arrest, making it a valuable tool for research on MET-related oncogenic processes.

SJF-8240 (PROTAC 7) is a proteolysis-targeting chimera (PROTAC) designed to selectively degrade the receptor tyrosine kinase c-Met. It induces polyubiquitination and subsequent proteasomal degradation of c-Met, leading to effective inhibition of downstream signaling. SJF-8240 exhibits potent antiproliferative activity in GTL16 gastric cancer cells, with an IC₅₀ of 66.7 nM, making it a promising tool for targeted cancer therapy and c-Met–driven tumor research.

DFX117 is a selective, orally active inhibitor targeting PI3Kα and c-Met tyrosine kinase. This compound effectively inhibits the PI3K/Akt/mTOR pathway, demonstrating significant antiproliferative activity against cancer cell lines such as NCI-H1975, NCI-H1993, and HCC827, with IC50 values ranging from 0.02 to 0.08 µM. DFX117 induces cell cycle arrest at the G0/G1 phase and promotes apoptosis in A549 and NCI-H1975 cells. Additionally, DFX117 exhibits notable antitumor efficacy in murine models, making it a valuable tool for cancer research.

Capmatinib hydrochloride is a selective c-MET kinase inhibitor that competitively targets ATP (IC50 = 0.13 nM). It effectively inhibits the phosphorylation of c-MET and its downstream signaling pathways, including ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride demonstrates potent antitumor activity by inhibiting c-MET-dependent tumor cell proliferation and migration, as well as inducing apoptosis. This compound is primarily metabolized by CYP3A4 and aldehyde oxidase, making it relevant for studies in cancer research and therapeutic development.

ABN401 is a selective ATP-competitive inhibitor of c-MET, exhibiting an IC50 of 10 nM. This compound demonstrates cytotoxic effects on MET-addicted cancer cells, with IC50 values ranging from 2 to 43 nM. ABN401 has shown oral bioavailability in preclinical models, with 42.1% to 56.2% in rats and 27.4% to 37.7% in dogs, and possesses significant antitumor activity, making it a valuable tool for cancer research and therapeutic development.

EGFR/c-Met-IN-1 is a dual inhibitor targeting both EGFR and c-Met, with IC50 values of 68.1 nM for EGFRL858R and 0.26 nM for c-Met. This compound induces apoptosis and causes cell cycle arrest in A549-P cells by downregulating the phosphorylation of EGFR, c-Met, and downstream AKT pathways. EGFR/c-Met-IN-1 demonstrates significant tumor growth inhibition in vitro and in vivo, making it a valuable reagent for cancer research focused on targeting these pathways.

EGFR-IN-8 is a dual inhibitor of the epidermal growth factor receptor (EGFR) and c-Met, demonstrating potential efficacy against EGFR TKI-resistant non-small cell lung cancer (NSCLC). This compound offers a novel approach for effectively targeting resistance mechanisms in NSCLC, providing a valuable tool for oncological research and drug development. Its unique pharmacological profile positions it as a promising candidate for further investigation in cancer therapy.

Zevontabart (MYTX-011 Antibody) is a pH-dependent antibody-drug conjugate (ADC) targeting c-MET. It interferes with the trafficking of c-MET, leading to reduced receptor recycling and enhanced endocytosis in c-MET-expressing cells. Zevontabart demonstrates significant cytotoxicity against solid tumor cells and exhibits anti-tumor efficacy in non-small cell lung cancer xenograft models. This reagent is valuable for research in non-small cell lung cancer and related studies.