c-Met/HGFR Inhibitor

Caveolin-1 (82-101) amide (human, mouse, rat) (Caveolin-1 scaffolding domain peptide) is a peptide that reverses aging-associated deleterious changes in multiple organs. Caveolin-1 (82-101) amide (human, mouse, rat) inhibits tyrosine kinases.

Elzovantinib (TPX-0022) is an oral-active inhibitor of SRC, MET and c-FMS, with IC₅₀ values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.

CEP-40783 is a potent, selective and orally available inhibitor of AXL and c-Met with IC₅₀ values of 7 nM and 12 nM, respectively.

(E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells.

Bafisontamab (EMB-01) is a bispecific antibody targeting EGFR and cMET with antitumor activity.

NPS-1034 is a dual inhibitor of AXL and MET with IC₅₀s of 10.3 and 48 nM, respectively.

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

Norleual TFA, an angiotensin (Ang) IV analog, is a hepatocyte growth factor (HGF)/c-Met inhibitor with an IC₅₀ of 3 pM. Norleual TFA is an AT4 receptor antagonist and exhibits potent antiangiogenic activities.

Canlitinib is a tyrosine kinase inhibitor, extracted from patent WO2018072614 (IV-2). Canlitinib has the potential for cancer study.

Tyrosine kinase inhibitor is a potent tyrosine kinase inhibitor.

Davutamig (REGN-5093) is a human IgG4-kappa, anti-MET bispecific antibody. Davutamig binds 2 distinct epitopes of MET, blocking ligand binding and inducing MET internalization and degradation. Davutamig is applicable to the research of advanced non-small cell lung cancer with MET gene abnormalities.

AMG-337 is a potent, orally active, selective MET kinase inhibitor with IC₅₀ values of 1, 1, 4.7, 5, 21.5, 1077 and >4000 nM of WT MET, H1094R MET, M1250T MET, HGF-stimulated pMET (PC3 cells) MET, V1092I MET, Y1230H MET, and D1228H MET, respectively. AMG 337 inhibits the phosphorylation of MET and downstream effectors in MET-amplified cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis.

Capmatinib (INC280; INCB28060) dihydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC₅₀=0.13 nM). Capmatinib dihydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase.

MGCD-265 analog is a potent and oral active inhibitor of c-Met and VEGFR2 tyrosine kinases, with IC₅₀s of 29 nM and 10 nM, respectively. MGCD-265 analog has significant antitumor activity.

Cabozantinib (Standard) is the analytical standard of Cabozantinib. This product is intended for research and analytical applications. Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC₅₀ values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC₅₀=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.

X-376 is a potent and highly specific ALK tyrosine kinase inhibitor (TKI) (IC₅₀=0.61 nM). X-376 is a less potent inhibitor of MET (IC₅₀=0.69 nM). X-376 displays potent anti-tumor activity.

Zurletrectinib is a brain-penetrant, orally active TRK inhibitor (TRKA IC₅₀ = 0.81 nM; TRKB IC₅₀ = 0.145 nM; TRKC IC₅₀ = 0.184 nM). Zurletrectinib exhibits stronger activity as a consequence of its augmented binding affinity for TRK kinases. Zurletrectinib exhibits higher activity against most TRK inhibitor resistance mutations (13 out of 18 mutations). Zurletrectinib can be used for the study of glioma.

Pamufetinib (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.

MK-2461 is an ATP-competitive, selective and orally active wild-type and mutant c-Met inhibitor (IC₅₀s: 0.4-2.5 nM). MK-2461 also inhibits Ron (IC₅₀ of 7 nM) and Flt1 (IC₅₀ of 10 nM), MK-2461 shows selective for c-MET over other kinases (lC₅₀s = 22-7800 nM). MK-2461 can be used for the study of cancer, such as gastric cancer.

7-Methoxy-1-tetralone is a potent antitumor agent. 7-Methoxy-1-tetralone inhibits cancer cell proliferation and migration, and induces hepatocellular carcinoma cell (HCC) apoptosis. 7-Methoxy-1-tetralone decreased the protein levels of NF-κB, matrix metallopeptidase 2 (MMP2)/MMP9, and p-AKT. 7-Methoxy-1-tetralone showed antitumor activity in nude mice and had no effect on body weight and liver, spleen and organ index.