c-Met/HGFR Inhibitor

Momordicine I is a cucurbitane-type triterpenoids. Momordicine I suppresses glioma growth by promoting apoptosis and impairing mitochondrial oxidative phosphorylation. Momordicine I inhibits glycolysis, lipid metabolism, induces autophagy in HNC cells to suppress head and neck cancer growth. Momordicine I alleviates isoproterenol-induced cardiomyocyte hypertrophy through suppression of PLA2G6 and DGK-ζ. Momordicine I exerts its cardiovascular benefits by upregulating nitric oxide, inhibiting the activity of angiotensin-converting enzyme (ACE), activating the PI3K/Akt pathway, reducing oxidative stress and inflammation. Momordicine I inhibits AKT1, IL-6, and SRC, suggesting its potential application in type 2 diabetes.

S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC₅₀ values below 20 nM.

c-Met inhibitor 1 is an orally active c-Met inhibitor. c-Met inhibitor 1 can inhibit c-Met phosphorylation with an IC₅₀ of 0.010 μM. c-Met inhibitor 1 has antitumor activity and can be used for the research of tumors such as gastric cancer, pancreatic cancer and malignant glioma.

Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC₅₀s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.

Cabozantinib-d₆ is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC₅₀s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.

ABN401 is an orally active and selective ATP-competitive c-MET inhibitor with an IC₅₀ of 10 nM. ABN401 is cytotoxic to MET-addicted cancer cells with the IC₅₀ of 2-43 nM. ABN401 has bioavailability in rats and dogs of 42.1-56.2% and 27.4-37.7%, respectively. ABN401 has antitumor activity.

BPI-9016M is a potent, orally active, and selective dual c-Met and AXL tyrosine kinases inhibitor. BPI-9016M suppresses tumor cell growth, migration and invasion of lung adenocarcinoma.

SCR-1481B1 (Metatinib anhydrous; c-Met inhibitor 2) is an inhibitor of the N-terminal fragment of Gasdermin D (GSDMD), with an IC₅₀ of 1.04 μM and a K_a of 0.42 μM in mice. SCR-1481B1 effectively blocks GSDMD-NT oligomerization and pore formation, inhibits GSDMD-mediated pyroptosis (Pyroptosis), preserves mitochondrial integrity, and reduces proinflammatory cytokine secretion. SCR-1481B1 also inhibits angiogenesis, exerts GSDMD-independent antitumor effects, and enhances the infiltration of antitumor immune cells. SCR-1481B1 is also an inhibitor targeting to c-MET and VEGFR2, can be used in studies related to melanoma and sepsis.

Cabozantinib-d₄ is deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.

Tepotinib (Standard) is the analytical standard of Tepotinib. This product is intended for research and analytical applications. Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC₅₀ of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation. Tepotinib has antitumor effects.

Roquefortine C is a mycotoxin that can be isolated from Penicillium species. Roquefortine C is an agonist of P-gp and an inhibitor of P450 3A and P450 1A. Roquefortine C can inhibit Gram-positive bacteria and also has certain neurotoxicity. Additionally, Roquefortine C can exert antitumor activity.

SFN68 is a humanized IgG1 neutralizing monoclonal antibody targeting HGF. SFN68 significantly inhibits HGF/c-Met interaction, c-Met activation, and, cell scattering and proliferation mediated by HGF. SFN68 can be used for cancers research.

JNJ-38877605-d1 (compound DO-2) is a highly selective MNNG HOS transforming (MET) inhibitor. JNJ-38877605-d1 is thought to diminish the formation of the Aldehyde Oxidase 1 inactive metabolite M3.

Glesatinib (MGCD265) is an orally active, potent MET/SMO dual inhibitor. Glesatinib, a tyrosine kinase inhibitor, antagonizes P-glycoprotein (P-gp) mediated multidrug resistance (MDR) in non-small cell lung cancer (NSCLC).

JNJ-38877618 is a potent, highly selective, orally bioavailable Met kinase inhibitor with IC₅₀s of 2 and 3 nM for wild type and mutant Met, respectively.

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

MK-8033 hydrochloride is an orally active ATP competitive c-Met/Ron dual inhibitor (IC₅₀s: 1 nM (c-Met),7 nM (Ron)), with preferential binding to the activated kinase conformation. MK-8033 hydrochloride can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs).

MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC₅₀ of 7.4 nM. MET kinase-IN-2 has antitumor activity.

Vabametkib is a MET TKI inhibitor. Vabametkib can be used in research on non-small cell lung cancer (NSCLC).

(rel)-Tivantinib is a potent and highly selective inhibitor of the receptor tyrosine kinase c-MET. (rel)-Tivantinib has two novel targets, GSK3α and GSK3β, which play an important role in the cellular mechanism of non-small cell lung cancer (NSCLC).