c-met

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].

c-Met-IN-17 is a potent inhibitor of c-Met kinase with an IC50 of 0.031 μM, making it relevant for anticancer research. [1]

c-Met-IN-19 (Compound 21j) is a potent c-Met inhibitor with an IC50 of 1.99 nM, demonstrating 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 inhibitor D9 is a c-Met kinase inhibitor.

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.

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.

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

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

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.

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

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.

SYN1143 (AMG-1) is a potent inhibitor of human RON and c-Met.In vitro kinase assays showed that compound I is a potent inhibitor of human RON and c-Met with IC50s of 9 and 4 nmol L, respectively.

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.

KRC-00715 is an orally effective inhibitor of c-Met, exhibiting high selectivity with an IC50 of 9.0 nM. This compound specifically inhibits the growth of gastric cancer cell lines with high c-Met expression by inducing G1 S phase block, and reduces the activity of downstream signals, including Akt, Erk, and c-Met itself. In the gastric cancer cell line Hs746T, KRC-00715 demonstrates cytotoxicity with an IC50 of 39 nM and selectively inhibits the proliferation of cell lines that overexpress c-Met. Additionally, KRC-00715 decreases tumor size in Hs746T xenograft mouse models.

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.

BMS-777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3.

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

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).

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).

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

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.

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.

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.