c-Met/HGFR Inhibitor

Ningetinib 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.

LMTK3-IN-1 (compound C28) is an ATP-competitive inhibitor of lemur tyrosine kinase 3 (LMTK3) (K_d=2.5 μM)，that acts by degrading LMTK3 via the ubiquitin-proteasome pathway. LMTK3-IN-1 shows anticancer activity in a variety of cancer cell lines and in vivo BC mouse models. LMTK3-IN-1 induces apoptosis in BC cell lines at 10-20 μM.

Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC₅₀=0.13 nM). Capmatinib hydrochloride 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 hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase.

SAR125844 is a potent, selective, and ATP-competitive MET kinase inhibitor with the value of IC₅₀ is 4.2 nM and K_i is 2.8 nM. SAR125844 has antitumor activity and can be used for the research of cancer.

MK-8033 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 can be used in the research of cancers, such as breast and bladder cancers, non-small cell lung cancers (NSCLCs).

Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC₅₀: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC).

MET kinase-IN-4 is an orally active Met kinase inhibitor. MET kinase-IN-4 has potent Met kinase inhibitory activity with an IC₅₀ value of 1.9 nM. MET kinase-IN-4 can be used for the research of cancer.

Crizotinib-d₅ is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition.

NVP-BVU972 is an selective and potent Met inhibitor, with an IC₅₀ of 14 nM. NVP-BVU972 also exhibits good anti-proliferative activity against Met with drug-resistant mutations and inhibits phosphorylation. NVP-BVU972 can be used in study of cancer.

PF-04217903 mesylate is an orally active, highly selective ATP-competitive c-Met kinase inhibitor with a K_i value of 4.8 nM and a K_d value of 4.5 nM. PF-04217903 mesylate blocks c-Met and HGF signaling pathways, inhibits MET phosphorylation, and blocks downstream MAPK, PI3K/AKT and PLCγ1 pathways. PF-04217903 mesylate suppresses tumor proliferation, survival, migration, invasion, angiogenesis and metastasis, induces apoptosis, and enhances efferocytosis, Annexin A1 expression and resolution of inflammation. PF-04217903 mesylate retains activity against several c-Met mutants (M1131T, V1220I, H1094R). PF-04217903 mesylate increases the incidence of subarachnoid hemorrhage and reduces survival rate without altering aneurysm formation, and also prevents lymph node metastasis induced by VEGF inhibition. PF-04217903 mesylate is applicable to research related to tumors (pancreas, stomach, lung, brain, colon, breast, kidney, melanoma, etc.), intracranial aneurysms and inflammatory diseases (gouty arthritis, neutrophilic pleuritis).

DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC₅₀ of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC₅₀s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo.

EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC.

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

AMG-208 is an orally active c-Met/RON dual selective inhibitor with an IC₅₀ of 9 nM for c-Met. AMG-208 is a CYP3A4 inhibitor with an IC₅₀ of 32 μM. AMG-208 has anti-cancer activity.

Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (K_i=2 nM) with anti-tumor activities. Merestinib dihydrochloride also has potent activity against MST1R (IC₅₀=11 nM), FLT3 (IC₅₀=7 nM), AXL (IC₅₀=2 nM), MERTK (IC₅₀=10 nM), TEK (IC₅₀=63 nM), ROS1, DDR1/2 (IC₅₀=0.1/7 nM) and MKNK1/2 (IC₅₀=7 nM).

Emzeltrectinib is a potent tyrosine kinase inhibitor with antineoplastic activity.

HGF-IN-1 ((the compound on the left in the second line of page 77) is a HGF inhibitor. HGF-IN-1 can be used in cancer research.

AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with K_i values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively.

Afatinib (Standard) is the analytical standard of Afatinib. This product is intended for research and analytical applications. Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.

Zevontabart (MYTX-011 Antibody; Q-397) is a pH-dependent anti-c-MET antibody. Zevontabart regulates the trafficking process of c-MET to reduce receptor recycling, and enhances its own endocytosis and accumulation in c-MET-expressing cells. Zevontabart induces cytotoxicity in solid tumor cells and exerts anti-tumor activity in a non-small cell lung cancer xenograft mouse model. Zevontabart can be used to synthesize ADC, such as: MYTX-011. Zevontabart can be used in studies related to non-small cell lung cancer, with its corresponding isotype control being Human IgG1 kappa, Isotype Control (HY-P99001).