c-Met/HGFR

Tepotinib (EMD-1214063) is an inhibitor of MET tyrosine kinase with potential antineoplastic activity.

Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity.

L-Ascorbic acid 2-phosphate trisodium (Sodium ascorbyl phosphate) is used in biocatalytic dephosphorylation for electric power generation and electrochemical detection assays.

C-Met inhibitor D9 is a c-Met kinase inhibitor.

SAR125844 is a potent and selective MET kinase inhibitor with a favorable preclinical toxicity profile,(IC50=4.2 nM).

BMS817378 is a potent and selective inhibitor of MET(IC50 : 1.7 nM).

Tepotinib hydrochloride(1 : x) is an orally bioavailable, mesenchymal-epithelial transition (MET) TKI developed mainly for selected NSCLC patients with METex14 skipping mutations.

Capmatinib xHCl (INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor, potently blocking in vitro kinase activity (IC50 = 0.13 nM) as well as constitutive or HGF-stimulated activity in cells (IC50 values range from 0.3 to 1.1 nM).

Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).

Capmatinib 2HCl (INC-280 2HCl) is a novel, ATP-competitive inhibitor of c-MET kinase with an IC50 with 0.13 nM.Capmatinib 2HCl exhibits picomolar enzymatic potency and is highly specific for c-MET with more than 10, 000-fold selectivity over a large panel of human kinases. This inhibitor potently blocks c-MET phosphorylation and activation of its key downstream effectors in c-MET-dependent tumor cell lines. As a result, Capmatinib 2HCl potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis in vitro.

Fosgonimeton acetate is an agonist of hepatocyte growth factor (HGF).

MK-2461 is a novel inhibitor that targets multiple proteins and competitively binds to ATP sites, specifically inhibiting the activated c-Met protein with an average inhibitory concentration (IC50) of 2.5 nM.

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

Capmatinib (INCB28060) is an orally bioavailable inhibitor of the proto-oncogene c-Met (HGFR)with potential antineoplastic activity.

NVP-TAE 226 (TAE226) is an effective FAK inhibitor (IC50: 5.5 nM) and most effective to Pyk2(IC50: 3.5 nM); 10- to 100-fold less effective against IGF-1R, InsR, c-Met, and ALK.

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

MET Tyrosine Kinase Inhibitor PF-04217903 is an orally bioavailabe, small-molecule tyrosine kinase inhibitor with potential antineoplastic activity.

Amuvatinib (MP470) is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity.

Emibetuzumab is a potent humanized bivalent MET antibody (IgG4 type). Emibetuzumab has antitumor activity, inhibition of HGF-dependent and independent MET pathway activation and tumor growth, and can be used to study advanced castration-resistant prostate cancer.

Onartuzumab (MetMAb) is a humanized anti-tyrosine kinase c-MET monovalent monoclonal antibody.Onartuzumab has antitumor activity with inhibitory effects on HGF binding, receptor phosphorylation, and signal transduction.

Rilotumumab (AMG 102) is a monoclonal antibody targeting hepatocyte growth factor that inhibits HGF/ MET-driven signaling. Rilotumumab has antitumor effects and can be used to study castration-resistant prostate cancer (CRPC) and gastric cancer.

Davutamig (REGN-5093) is a humanized IgG4-kappa, anti-MET monoclonal antibody that binds to two distinct, nonoverlapping epitopes on the MET receptor. It functions as an antineoplastic agent [1].

Telisotuzumab(ABT-700) is a humanized recombinant antibody targeting the therapeutic hepatocyte growth factor receptor (MET) with high affinity for c-Met.Telisotuzumab has inhibitory effects on c-Met signaling and antitumor activity.

Hepln-13 is a hepsin inhibitor that acts by hindering prostate cancer bone metastasis.

AMG-208 is a highly selective c-Met inhibitor with IC50 of 9 nM. Phase 1.

MGCD-265 analog (Glesatinib) is an orally bioavailable multitargeted tyrosine kinase inhibitor with potential antineoplastic activity with IC50 of 29 nM and 10 nM for c-Met and VEGFR2, respectively.

Ningetinib Tosylate is an orally bioavailable tyrosine kinase inhibitor with IC50s of <1.0, 1.9 and 6.7 nM for Axl, VEGFR2, and c-Met, respectively.

MK-8033 is a new and selective dual ATP competitive c-Met/Ron inhibitor (IC50: 1 nM Wt c-Met).

1D228, a c-Met/TRK inhibitor with antitumor properties, suppresses cyclin D1 to precipitate G0/G1 arrest, thereby inhibiting proliferation and migration of cancer cells. This compound is applicable in researching gastric, liver, and vascular tumors [1].

RPI-1 is a competitive, potent ATP-dependent Ret kinase inhibitor.

Lmtk3-in-1 is a potent ATP-competitive lemur tyrosine kinase 3 (LMTK3) (Kd=2.5 μM) inhibitor that degrades LMTK3 through the ubiquitin proteasome pathway. LMTK3-IN-1 has shown anticancer activity in a variety of cancer cell lines and in vivo BC mouse models. LMTK3-IN-1 (10-20 μM) can induce the apoptosis of BC cell line.

c-Met-IN-19 (Compound 21j) is a potent c-Met inhibitor with an IC50 of 1.99 nM and demonstrates cytotoxic effects on various cancer cell lines, including A549, HT-29, SGC-7901, and MDA-MB-231, with IC50 values of 0.25, 0.36, 0.98, and 0.76 μM, respectively [1].

C-Met-IN-18, an ATP-competitive type-III inhibitor, targets both wild-type (WT) and D1228V mutant c-MET with IC50 values of 0.013 µM and 0.20 µM, respectively. It is utilized in research pertaining to c-MET-driven cancers [1].

MET/PDGFRA-IN-1 (compound 8c) serves as an inhibitor of MET and PDGFRA proteins, displaying an IC50 of 36 μM against MET. It impedes MET phosphorylation, thereby promoting apoptosis, and curtails the proliferation of various MET-positive cell lines, with IC50 values of 15.3 μM for AsPc-1, 19.0 μM for EBC-1, 22.0 μM for MKN-45, 25.6 μM for Mia-Paca-2, 21.0 μM for HT-29, and 31.5 μM for K562 [1].

c-met-IN-1 is a potent and selective c-Met inhibitor (IC50: 1.1 nM) with antitumor activity.

Glesatinib is an orally active and potent dual inhibitor of MET/SMO. Glesatinib is also a tyrosine kinase inhibitor. It antagonizes P-glycoprotein mediated multidrug resistance (MDR) in NSCLC.

CSF1R-IN-2 is an oral-active SRC, MET and c-FMS inhibitor (IC50s: 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively).

RIPK3-IN-1 is a selective and potent RIPK3 inhibitor (IC50: 9.1 nM) that inhibits the activities of c-Met kinase, RIPK1 and RIPK2.RIPK3-IN-1 has potential tumorigenic activity and can be used to study apoptosis.

SU11274 (Met Kinase Inhibitor)(IC50=10 nM) is a specific Met inhibitor. It shows no significant effects on PGDFRβ, EGFR or Tie2.

S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3, blocking cellular phosphorylation of MET, AXL, and FGFRs.

SGI-7079 is a new selective Axl inhibitor. SGI-7079 can be a dose-dependent manner inhibited growth of tumors. It is also a potential therapeutic target for EGFR inhibitor resistance.

Tivantinib (ARQ 197) is an orally bioavailable small molecule inhibitor of c-Met with potential antineoplastic activity.

Ensartinib hydrochloride (X-396 dihydrochloride) is a potent new-generation ALK inhibitor with high activity against CNS metastases and a broad range of known crizotinib-resistant ALK mutations. It potently inhibits both wild-type ALK and ALK variants (C1156Y, F1174, G1202R, L1196M, S1206R, and T1151 mutants) with in vitro IC50s of <4 nM.

c-Met inhibitor 1 is a c-Met receptor signaling pathway inhibitor, used for the treatment of cancer including glioblastoma, gastric, and pancreatic cancer.

Dihexa (Hexanoyl-Tyr-Ile-Ahx-NH2) is an activator of the hepatocyte growth factor/c-Met (HGF/c-Met) system,it binds to HGF (Kd = 65 pM),and an analog of the peptide angiotensin IV.

Tyrosine kinase inhibitor is a tyrosine kinase inhibitor used in combination with fragmenting aromatic nitrogen compounds as antiproliferative agents.

EGFR-IN-8, a dual inhibitor targeting both EGFR and c-Met, shows potential as a promising candidate for further development in treating EGFR TKI-resistant NSCLC.

Antitumor Agent-111 (Compound 46), a c-Met kinase inhibitor (IC50 = 46 nM), exhibits both antitumor and antiproliferative effects. It impedes the cell cycle at the G0/G1 phase and induces apoptosis [1].

BMS 777607 (BMS 817378) is a Met-related inhibitor for c-Met/Axl/Ron/Tyro3 (IC50: 3.9/1.1/1.8/4.3 nM). BMS-777607 has been investigated for the basic science of Malignant Solid Tumour.

PF-04217903 phenolsulfonate is a potent ATP-competitive inhibitor of c-Met kinase (Ki of 4.8 nM for human c-Met).