c-Met/HGFR

Amivantamab (JNJ-61186372) is a humanized antibody that recognizes epidermal growth factor receptor (EGFR) and MET proto-oncogene (MET), with anticancer and anti-tumor activities, preventing ligand binding to EGFR and MET and receptor dimerization that inhibits downstream signal transduction. Amivantamab can induce Fc-dependent endocytosis of macrophages and antibody-dependent cytotoxicity of natural killer cells, and can be used to study metastatic non-small cell lung cancer.

Tepotinib (EMD-1214063) is a c-MET tyrosine kinase inhibitor (IC50=3 nM) that is selective, orally active, and ATP-competitive. Tepotinib has antitumor effect and is used in the treatment of non-small cell lung cancer.

1. Herbacetin induces apoptosis in HepG2 cells, by ROS and PI3K Akt pathway. 2. Herbacetin suppresses the HGF-induced motility of human breast cancer MDA-MB-231 cells by inhibiting c-Met and Akt phosphorylation.

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.

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

Bozitinib (PLB-1001) (PLB-1001) is a highly selective inhibitor of the c-MET kinase with blood-brain barrier permeability. Bozitinib binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily.

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.

Merestinib (LY2801653) is an orally available, small molecule inhibitor of the proto-oncogene c-Met (Ki: 2 nM) with potential antineoplastic activity. Merestinib electively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing the constitutively activated c-Met protein.

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

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

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.

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.

Crizotinib hydrochloride (PF-02341066 hydrochloride) is a novel inhibitor of anaplastic lymphoma kinase and c-Met, with IC50 values of 20 nM and 8 nM, respectively.

URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19 42 14 150 nM, for MLK1 MLK2 MLK3 DLK), and also inhibits LRRK2 activity (IC50: 11 nM).

Foretinib (GSK1363089) is a broad-spectrum tyrosine kinase inhibitor with IC50s of 0.4 nM and 0.9 nM for Met and KDR.

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.

Savolitinib (Volitinib) (AZD-6094) is an effective, selective, and orally bioavailable c-Met inhibitor (IC50s: 5 nM 3 nM for c-Met p-Met).

BMS-794833 is a potent ATP competitive inhibitor of Met VEGFR2; a prodrug of BMS-817378.

Ningetinib (CT-053) (CT053PTSA) 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.

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

BMS-2 is a Met Flt-3 VEGFR2 tyrosine kinase inhibitor.

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).

BMS 777607 (BMS 817378) is a Met-related inhibitor targeting c-Met, Axl, Ron, and Tyro3 with IC50 values of 3.9 nM, 1.1 nM, 1.8 nM, and 4.3 nM, respectively. BMS-777607 has been investigated in basic science research for malignant solid tumors.

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

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

SGX-523 is a selective Met inhibitor (IC50: 4 nM), no inhibitory to Abl, BRAFV599E, p38α, and c-Raf.

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

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).

PHA-665752 is an effective, specific and ATP-competitive c-Met inhibitor (IC50: 9 nM), >50-fold selectivity for c-Met than STKs or RTKs.

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.

Altiratinib (DCC-2701)(DCC-2701) is a novel c-MET TIE-2 VEGFR inhibitor; effectively reduce tumor burden in vivo and block c-MET pTyr(1349)-mediated signaling, cell growth and migration as compared with an HGF antagonist in vitro.

Dual IGF-1R InsR Inhibitor BMS-754807 is an oral small molecule inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases with potential antineoplastic activity.

Terevalefim (ANG-3777) is an hepatocyte growth factor (HGF) mimetic. Terevalefim selectively activates the c-Met receptor.

NVP-TAE 226 (TAE226) is a potent FAK inhibitor (IC50: 5.5 nM), exhibiting even greater efficacy against Pyk2 (IC50: 3.5 nM), and is 10- to 100-fold less effective against IGF-1R, InsR, c-Met, and ALK.

JNJ-38877605 is an ATP-competitive c-Met inhibitor (IC50: 4 nM), 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.

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.

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.

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

Cabozantinib S-malate (XL184) is the s-malate salt form of cabozantinib, an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity.

SRI 31215 TFA, a small molecule that acts as a triplex inhibitor of matriptase, hepsin and HGFA and mimics the activity of HAI-1 2, endogenous inhibitors of HGF activation with IC50s of 0.69 μM, 0.65 μM, 0.3 μM,

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

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.

JNJ-38877618 (OMO-1) is an effective and highly selective inhibitor of Met kinase (IC50s: 2 and 3 nM for wild type and mutant Met, respectively).

SCR-1481B1 (c-Met inhibitor 2) has activity against cancers dependent on Met activation and also has activity against cancers as a VEGFR inhibitor

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

XL092 (JUN04542) is an Axl Mer cMet KDR inhibitor for the treatment of Axl and Mer receptor tyrosine kinase- dependent disorders.