c-Kit

c-Kit Inhibitors (23)

water-soluble

Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1064 Masitinib (AB1010) Masitinib is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms. Phase 3.
  • Mol Syst Biol, 2015, 11(1):789
  • Biomaterials, 2013, 34(38):9737-46
  • Biosens Bioelectron, 2015, 77:149-156
S1244 Amuvatinib (MP-470) Amuvatinib (MP-470) is a potent and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively. Phase 2.
  • Nat Genet, 2012, 44(8):852-60
  • Cancer Res, 2014, 74(20):5878-90
  • Oncogene, 2014, 33(10):1316-24
S1220 OSI-930 OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1.
  • Mol Syst Biol, 2015, 11(1):789
  • Biochem Pharmacol, 2012, 84(6):766-74
  • BMC Microbiol, 2013, 13(1):249
S1021 Dasatinib Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively.
  • Cell Stem Cell, 2012, 10(2):210-7
  • Cancer Discov, 2016, 6(7):727-39
  • Cancer Discov, 2011, 1(7):608-25
S1026 Imatinib Mesylate (STI571) Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively.
  • Cancer Cell, 2014, 26(6):840-50
  • Cell Stem Cell, 2012, 10(2):210-7
  • Sci Transl Med, 2014, 6(261):261ra152
S1042 Sunitinib Malate Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit.
  • Nature, 2011, 478(7369):349-55
  • Sci Transl Med, 2015, 7(284):284ra57
  • Cell Res, 2011, 21(7):1080-7
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
S1005 Axitinib Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.
  • Cancer Discov, 2012, 2(4):344-55
  • Development, 2013, 140(20):4214-25
  • Glia, 2012, 60(6):936-47
S1035 Pazopanib HCl (GW786034 HCl) Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.
  • Cancer Discov, 2013, 3(6):636-47
  • J Virol, 2011, 85(5):2296-303
  • J Cell Physiol, 2016, 231(10):2286-302
S1018 Dovitinib (TKI-258, CHIR-258) Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4.
  • Cancer Res, 2013, 73(16):5195-205
  • Haematologica, 2011, 96(6):922-6
  • Expert Opin Inv Drugs, 2014, 23(4):469-87
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1101 Vatalanib (PTK787) 2HCl Vatalanib (PTK787) 2HCl is an inhibitor of VEGFR2/KDR with IC50 of 37 nM in a cell-free assay, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 3.
  • Nat Biotechnol, 2013, 31(10):898-907
  • J Clin Invest, 2011, 121(8):3005-23
  • Cell Res, 2011, 21(7):1080-7
S1207 Tivozanib (AV-951) Tivozanib (AV-951) is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R. Phase 3.
  • J Med Chem, 2015,
  • J Chem Inf Model, 2014, 54(3):881-93
  • Cytometry A, 2014, 85(6):537-47
S1032 Motesanib Diphosphate (AMG-706) Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3.
  • Cardiovasc Res, 2011, 91(3):402-11
  • Mol Cell Endocrinol, 2013, 377(1-2):1-6
  • Int J Cardiol, 2015, 183C:221-231
S1363 Ki8751 Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR.
  • Mol Cell Proteomics, 2012, 11(9):745-57
  • Sci Rep, 2015, 5:7890
  • Cellular Signalling, 2016, 19;28(6):652-662
S2231 Telatinib Telatinib is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively. Phase 2.
  • Biochem Pharmacol, 2014, 89(1):52-61
S3012 Pazopanib Pazopanib is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.
  • Cancer Discov, 2013, 3(6):636-47
  • Clin Cancer Res, 2014, 19(9):2368-80
  • J Virol, 2011, 85(5):2296-303
S2769 Dovitinib (TKI-258) Dilactic Acid Dovitinib Dilactic acid (TKI258 Dilactic acid) is the Dilactic acid of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
  • Cancer Lett, 2016, 380(1):163-173
  • Expert Opin Inv Drugs, 2014, 23(4):469-87
  • Br J Cancer, 2011, 104(1):75-82
S8024 Tyrphostin AG 1296 Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR.
  • Onco Targets Ther, 2014, 7:425-32
S7765 Dovitinib (TKI258) Lactate Dovitinib (TKI258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
  • Genome Biol, 2014, 15(8):428
S7782 Dasatinib Monohydrate Dasatinib Monohydrate is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
  • Nature, 2016, 534(7607):341-6
  • Cell Stem Cell, 2012, 10(2):210-7
  • Cancer Discov, 2011, 1(7):608-25
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S7781 Sunitinib Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.
  • Nature, 2011, 478(7369):349-55
  • Sci Transl Med, 2015, 7(284):284ra57
  • Mol Syst Biol, 2015, 11(1):789
S7003 AZD2932 AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.
S7818 Pexidartinib (PLX3397) Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. Phase 3.
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All c-Kit Products

Hover Mouse over '+' to display IC50

Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1064 Masitinib (AB1010) <1 mg/mL 100 mg/mL 4 mg/mL
S1244 Amuvatinib (MP-470) <1 mg/mL 32 mg/mL <1 mg/mL
S1220 OSI-930 <1 mg/mL 89 mg/mL 3 mg/mL
S1021 Dasatinib <1 mg/mL 98 mg/mL <1 mg/mL
S1026 Imatinib Mesylate (STI571) 118 mg/mL 118 mg/mL <1 mg/mL
S1042 Sunitinib Malate <1 mg/mL 15 mg/mL <1 mg/mL
S1119 Cabozantinib (XL184, BMS-907351) <1 mg/mL 100 mg/mL <1 mg/mL
S1005 Axitinib <1 mg/mL 35 mg/mL <1 mg/mL
S1035 Pazopanib HCl (GW786034 HCl) <1 mg/mL 17 mg/mL <1 mg/mL
S1018 Dovitinib (TKI-258, CHIR-258) <1 mg/mL 30 mg/mL <1 mg/mL
S1101 Vatalanib (PTK787) 2HCl 10 mg/mL 85 mg/mL 6 mg/mL
S1207 Tivozanib (AV-951) <1 mg/mL 20 mg/mL <1 mg/mL
S1032 Motesanib Diphosphate (AMG-706) 19 mg/mL 100 mg/mL <1 mg/mL
S1363 Ki8751 <1 mg/mL 47 mg/mL <1 mg/mL
S2231 Telatinib <1 mg/mL 82 mg/mL 1 mg/mL
S3012 Pazopanib <1 mg/mL 87 mg/mL <1 mg/mL
S2769 Dovitinib (TKI-258) Dilactic Acid 70 mg/mL 90 mg/mL <1 mg/mL
S8024 Tyrphostin AG 1296 <1 mg/mL 6 mg/mL <1 mg/mL
S7765 Dovitinib (TKI258) Lactate 66 mg/mL 100 mg/mL 1 mg/mL
S7782 Dasatinib Monohydrate <1 mg/mL 21 mg/mL <1 mg/mL
S7781 Sunitinib <1 mg/mL 25 mg/mL <1 mg/mL
S7003 AZD2932 <1 mg/mL 89 mg/mL 5 mg/mL
S7818 Pexidartinib (PLX3397) <1 mg/mL 83 mg/mL <1 mg/mL
Tags: c-Kit mutation | c-Kit receptor | c-Kit expression | c-Kit cancer | c-Kit signaling | c-Kit mutation analysis | c-Kit tyrosine kinase receptor | c-Kit proto-oncogene | c-Kit activation | c-Kit phosphorylation | c-Kit kinase activity | c-Kit inhibitor review
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