c-Met

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c-Met Inhibitors (21)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1068 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.
  • Nature, 2012, 487(7408):505-9
  • Cell, 2012, 151(5):937-50
  • Nat Med, 2012, 18(6):883-91
S1119 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.
  • Cancer Discov, 2014, 4(7):816-27
  • Nat Commun, 2014, 5:3116
  • Mol Cancer Ther, 2014, 10.1158/1535-7163.MCT-14-0274
S1111 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.
  • Nat Genet, 2012, 44(8):852-60
  • Leukemia, 2014, 28(3):629-41
  • Cancer Res, 2011, 71(15):5255-64
S1070 PHA-665752 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.
  • Nat Genet, 2012, 44(8):852-60
  • Cancer Discov, 2013, 3(12):1404-15
  • Cell Res, 2015, 10.1038/cr.2015.16
S1080 SU11274 SU11274 is a selective Met inhibitor with IC50 of 10 nM in cell-free assays, no effects on PGDFRβ, EGFR or Tie2.
  • Nat Med, 2012, 18(7):1118-22
  • Clin Cancer Res, 2014, 20(22):5796-807
  • Oncogene, 2013, 32(10):1252-65
S7669 NPS-1034 NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.
S1112 SGX-523 SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α. Phase 1.
  • Am J Respir Crit Care Med, 2016, 10.1164/rccm.201509-1878OC
  • J Hepatol, 2014, 60(1):143-51
  • Proc Natl Acad Sci USA, 2012, 109(31):E2127-33
S1561 BMS-777607 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.
  • J Clin Invest, 2014, 124(11):4737-52
  • J Pathol, 2015, 237(1):14-24
  • Mol Cancer Ther, 2014, 13(1):37-48
S7067 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.
  • Cell Res, 2015, 10.1038/cr.2015.16
S2201 BMS-794833 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.
S2761 NVP-BVU972 NVP-BVU972 is a selective and potent Met inhibitor with IC50 of 14 nM.
S2774 MK-2461 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. .
S2788 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.
  • Dev Cell, 2014, 29(4):421-36
S1316 AMG-208 AMG 208 is a highly selective c-Met inhibitor with IC50 of 9 nM. Phase 1.
S2747 AMG-458 AMG 458 is a potent c-Met inhibitor with Ki of 1.2 nM, ~350-fold selectivity for c-Met than VEGFR2 in cells.
S1361 MGCD-265 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.
  • Cancer Lett, 2013, 340(1):43-50
  • Int J Clin Exp Pathol, 2013, 6(10):2082-91
S2859 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.
S1114 JNJ-38877605 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.
  • Nature, 2015, 10.1038/nature14407
  • Gut, 2014, 10.1136/gutjnl-2013-305257
  • PLoS Biol, 2011, 9(9):e1001162
S1124 BMS-754807 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.
  • Cancer Res, 2014, 74(20):5866-77
  • Clin Cancer Res, 2013, 19(11):2984-94
  • Mol Cell Biol, 2015, 35(7):1182-96
S1094 PF-04217903 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.
  • Clin Cancer Res, 2014, 20(17):4559-73
  • Clin Cancer Res, 2015, 21(1):166-74
  • Clin Cancer Res, 2015, 1(7):1752-63
S2753 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.
  • Oncotarget, 2015, 6(5):3211-24
  • J Exp Clin Cancer Res, 2015, 34:118
  • Cell Signal, 2013, 25(12):2652-60

Hover Mouse over '+' to display IC50

Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
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 127 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
S7669 NPS-1034 <1 mg/mL 100 mg/mL 4 mg/mL
S1112 SGX-523 <1 mg/mL 2 mg/mL <1 mg/mL
S1561 BMS-777607 <1 mg/mL 47 mg/mL <1 mg/mL
S7067 Tepotinib (EMD 1214063) <1 mg/mL 5 mg/mL <1 mg/mL
S2201 BMS-794833 <1 mg/mL 94 mg/mL <1 mg/mL
S2761 NVP-BVU972 <1 mg/mL 68 mg/mL 68 mg/mL
S2774 MK-2461 <1 mg/mL 99 mg/mL <1 mg/mL
S2788 Capmatinib (INCB28060) <1 mg/mL 2 mg/mL <1 mg/mL
S1316 AMG-208 <1 mg/mL 0.25 mg/mL <1 mg/mL
S2747 AMG-458 <1 mg/mL 21 mg/mL <1 mg/mL
S1361 MGCD-265 <1 mg/mL 104 mg/mL <1 mg/mL
S2859 Golvatinib (E7050) <1 mg/mL 20 mg/mL <1 mg/mL
S1114 JNJ-38877605 <1 mg/mL 37 mg/mL <1 mg/mL
S1124 BMS-754807 <1 mg/mL 92 mg/mL 92 mg/mL
S1094 PF-04217903 <1 mg/mL 5 mg/mL <1 mg/mL
S2753 Tivantinib (ARQ 197) <1 mg/mL 73 mg/mL <1 mg/mL
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