Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
Water DMSO Alcohol
S1068 Crizotinib (PF-02341066) <1 mg/mL 9 mg/mL <1 mg/mL
S1119 Cabozantinib (XL184, BMS-907351) <1 mg/mL 100 mg/mL <1 mg/mL
S1111 Foretinib (GSK1363089) <1 mg/mL 100 mg/mL <1 mg/mL
S1070 PHA-665752 <1 mg/mL 128 mg/mL <1 mg/mL
S1080 SU11274 <1 mg/mL 92 mg/mL 2 mg/mL
S9308 Pulsatilla saponin D -1 mg/mL 100 mg/mL -1 mg/mL
S7674 Savolitinib(AZD6094, HMPL-504) <1 mg/mL 16 mg/mL <1 mg/mL
S1112 SGX-523 <1 mg/mL 3 mg/mL <1 mg/mL
S1561 BMS-777607 <1 mg/mL 47 mg/mL <1 mg/mL
S2753 Tivantinib (ARQ 197) <1 mg/mL 73 mg/mL <1 mg/mL
S1114 JNJ-38877605 <1 mg/mL 37 mg/mL <1 mg/mL
S1094 PF-04217903 <1 mg/mL 5 mg/mL <1 mg/mL
S1361 MGCD-265 analog <1 mg/mL 104 mg/mL <1 mg/mL
S2788 Capmatinib (INCB28060) <1 mg/mL 2 mg/mL <1 mg/mL
S1124 BMS-754807 <1 mg/mL 92 mg/mL 92 mg/mL
S2201 BMS-794833 <1 mg/mL 94 mg/mL <1 mg/mL
S1316 AMG-208 <1 mg/mL 0.25 mg/mL <1 mg/mL
S2774 MK-2461 <1 mg/mL 99 mg/mL <1 mg/mL
S2859 Golvatinib (E7050) <1 mg/mL 20 mg/mL <1 mg/mL
S2747 AMG-458 <1 mg/mL 21 mg/mL <1 mg/mL
S2761 NVP-BVU972 <1 mg/mL 68 mg/mL 68 mg/mL
S7067 Tepotinib (EMD 1214063) <1 mg/mL 5 mg/mL <1 mg/mL
S8167 AMG 337 <1 mg/mL 95 mg/mL 95 mg/mL
S7014 Merestinib (LY2801653) <1 mg/mL 100 mg/mL 100 mg/mL
S8404 S49076 <1 mg/mL 87 mg/mL <1 mg/mL
S3759 Norcantharidin -1 mg/mL 33 mg/mL -1 mg/mL
S7669 NPS-1034 <1 mg/mL 100 mg/mL 4 mg/mL
Catalog No. Information Product Use Citations Product Validations

Crizotinib (PF-02341066)

Crizotinib (PF-02341066) is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively.


Cabozantinib (XL184, BMS-907351)

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 in cell-free assays, respectively.


Foretinib (GSK1363089)

Foretinib (GSK1363089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2.



PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM in cell-free assays, >50-fold selectivity for c-Met than RTKs or STKs.



SU11274 is a selective Met inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2.


Pulsatilla saponin D

Pulsatilla saponin D, isolated from the root of Pulsatilla koreana, targets c-Met and exerts antiangiogenic and antitumor activities.


Savolitinib(AZD6094, HMPL-504)

Savolitinib (volitinib, AZD6094, HMPL-504) is a novel, potent, and selective MET inhibitor currently in clinical development in various indications, including PRCC. The IC50 values of this compound for c-Met and p-Met are 5 nM and 3 nM, respectively. It shows exquisite selectivity for c-Met over 274 kinase.



SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α. Phase 1.



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 in cell-free assays, 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. Phase 1/2.


Tivantinib (ARQ 197)

Tivantinib (ARQ 197) is the first non-ATP-competitive c-Met inhibitor with Ki of 0.355 μM in a cell-free assay, little activity to Ron, and no inhibition to EGFR, InsR, PDGFRα or FGFR1/4. Phase 3.



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. Phase 1.



PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM in A549 cell line, susceptible to oncogenic mutations (no activity to Y1230C mutant). Phase 1.


MGCD-265 analog

MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.


Capmatinib (INCB28060)

Capmatinib (INCB28060) is a novel, ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM in a cell-free assay, inactive against RONβ, as well as EGFR and HER-3. Phase 1.



BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2.



BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1.



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



MK-2461 is a potent, multi-targeted inhibitor for c-Met(WT/mutants) with IC50 of 0.4-2.5 nM, less potent to Ron, Flt1; 8- to 30-fold greater selectivity of c-Met targets versus FGFR1, FGFR2, FGFR3, PDGFRβ, KDR, Flt3, Flt4, TrkA, and TrkB. Phase 1/2. .


Golvatinib (E7050)

Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2.



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



NVP-BVU972 is a selective and potent Met inhibitor with IC50 of 14 nM.


Tepotinib (EMD 1214063)

Tepotinib (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. Phase 1.


AMG 337

AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the MET receptor with an IC50 of 1 nM.


Merestinib (LY2801653)

LY2801653 is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min.



S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L.



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



NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.

Tags: c-Met inhibition | c-Met cancer | c-Met pathway | c-Met activation | c-Met phosphorylation | c-Met inhibitor clinical trial | c-Met assay | c-Met inhibitor therapy | c-Met inhibitor review