c-Met/HGFR

Tyrosine kinase-IN-6 is a potent inhibitor of RON splice variants, demonstrating significant anticancer and antineoplastic effects [1].

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

Glesatinib is an orally active and potent dual inhibitor of MET/SMO.

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

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

DS-1205: AXL kinase inhibitor (IC50=1.3 nM), also targets MER, MET, TRKA (IC50s: 63, 104, 407 nM), hinders cell migration and tumor growth.

X-376 (Ensartinib) is an orally available small molecule inhibitor of the receptor tyrosine kinase ALK with potential antineoplastic activity.

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

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.

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

c-Kit-IN-1 (DCC-2618) is an effective inhibitor of c-Met and c-Kit (IC50s<200 nM).

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.

Umikibart is a humanized IgG4κ antibody targeting HGF, with the corresponding isotype control being HumanIgG4(S228P) kappa, Isotype Control.

c-Met-IN-26 (compound 1-170) is an effective inhibitor of c-Met, exhibiting an IC50 of 1.6 nM.

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

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

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,

Davutamig (REGN-5093) is a humanized IgG4-kappa, anti-MET monoclonal antibody that binds to two distinct, nonoverlapping epitopes on the MET receptor.

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