Signaling Pathway

c-Met/HGFR

c-Met/HGFR

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c-Met ( hepatocyte growth factor receptor or HGFR) is a protein possesses tyrosine kinase activity. The primary single chain precursor protein is post-translationally cleaved to produce the alpha and beta subunits, which are disulfide linked to form the mature receptor. c-Met is a membrane receptor that is essential for embryonic development and wound healing. Hepatocyte growth factor (HGF) is the only known ligand of the c-Met receptor. c-Met is normally expressed by cells of epithelial origin, while expression of HGF is restricted to cells of mesenchymalorigin. Upon HGF stimulation, c-Met induces several biological responses that collectively give rise to a program known as invasive growth.

c-Met/HGFR Inhibitors & Modulators (32)

Product Name Catalog No. Brief Description
Altiratinib

HY-B0791

Altiratinib(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 a HGF antagonist in vitro.

AMG-208

HY-12035

AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM.

AMG-337

HY-18696

AMG-337 is a potent and highly selective small molecule ATP-competitive MET kinase inhibitor.

BMS 777607

HY-12076

BMS-777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, 40-fold more selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more than 500-fold greater selectivity versus all other receptor and non receptor kinases.

BMS-794833

HY-10497

BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7/15 nM; also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378.

c-Kit-IN-1

HY-15240

c-Kit-IN-1 is a small molecule inhibitor of c-Kit and PDGFR.

c-Met inhibitor 1

HY-15735

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

c-Met inhibitor 2

HY-18711A

c-Met inhibitor 2 is a potent compound that has activity against cancers dependent upon Met activation and also has activity against cancers as a VEGFR inhibitor.

Cabozantinib

HY-13016

Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively.

Crizotinib

HY-50878

Crizotinib is inhibitor of the c-Met kinase and the NPM-ALK.

Crizotinib hydrochloride

HY-50878A

Crizotinib is inhibitor of the c-Met kinase and the NPM-ALK.

E-7050

HY-13068

E7050(Golvatinib) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM.

EMD-1214063

HY-14721

EMD 1214063 is a potent and selective c-Met inhibitor with IC50 of 4 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer.

Foretinib

HY-10338

Foretinib (GSK1363089; XL880; EXEL-2880; GSK089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM.

Glesatinib hydrochloride

HY-19642A

Glesatinib hydrochloride is an inhibitor of the MET and Axl receptor tyrosine kinase pathways, which drive tumour growth when altered.

INCB28060

HY-13404

Description:
IC50 Value: 0.13±0.05 nM( for recombinant human wild-type c-MET) [1]
INCB28060 is a novel orally active inhibitor (IC50: 0.13nM) of c-MET kinase.

JNJ-38877605

HY-50683

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

LY2801653

HY-15514

LY2801653 is a potent, orally bioavailable, small-molecule inhibitor of c-MET kinase(Ki= 2 nM).

LY2801653 dihydrochloride

HY-15514A

LY2801653 2Hcl is a potent, orally bioavailable, small-molecule inhibitor of c-MET kinase(Ki= 2 nM).

MGCD-265 analog

HY-10991

MGCD-265-analog (structurally related to MGCD-265) 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.