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Tyrosine Kinase/Adaptors c-Kit

c-Kit

Proto-oncogene c-KIT is the gene encoding the receptor tyrosine kinase protein known as tyrosine-protein kinase KIT, CD117 (cluster of differentiation 117) or mast/stem cell growth factor receptor (SCFR). Multiple transcript variants encoding different isoforms have been found for this gene.KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT is a receptor tyrosine kinase type III, which binds to stem cell factor (a substance that causes certain types of cells to grow), also known as "steel factor" or "c-kit ligand".
Cat No. product name
T0093 Sorafenib tosylateHOT Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).
T0097L Pazopanib Pazopanib, a small molecule inhibitor, inhibits multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits VEGFR-1...
T0374L Sunitinib Sunitinib, a multi-targeted RTK inhibitor, is targeting PDGFRβ and VEGFR2 (Flk-1) with IC50 of 2 nM and 80 nM and also inhibits c-Kit.
T1448 DasatinibHOT Dasatinib is a potent inhibitor of the Bcr-Abl and Src family (IC50s: 0.6, 0.8, 79 and 37 nM for Abl, Src, c-Kit, and c-KitD816V, respectively).
T1448L Dasatinib monohydrate Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promot...
T1621 Imatinib MesylateHOT Imatinib mesylate is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respecti...
T1667 Tandutinib Tandutinib (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R ...
T1792 RegorafenibHOT Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor (IC50s: 1.5/2.5/4.2/7/13/22 nM for RET/C-RAF/VEGFR2/c-Kit/VEGFR1/PDGFRβ).
T1797 XL184 Cabozantinib S-malate is the s-malate salt form of cabozantinib, an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential ...
T1830 BX795 BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respec...
T1836 AZD2932 AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3, and c-Kit.
T1925 PLX647 PLX647 is a highly selective dual FMS/KIT kinase inhibitor (IC50: 28/16 nM).
T2070 CEP-32496 CEP-32496 is a highly potent inhibitor of BRAF.
T2115 Pexidartinib Pexidartinib is a capsule formulation containing a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic ...
T2288L Motesanib Diphosphate Motesanib Diphosphate is the orally bioavailable diphosphate salt of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity.
T7499 TAK-779 TAK-779 is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).
T2372 PonatinibHOT Ponatinib is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively).
T2446 KI8751 KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.
T2500 Cediranib Cediranib (AZD2171) is a highly potent (IC50 < 1 nmol/L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro, also inhibits Flt1/4 (IC50: 5 nM...
T2514 Linifanib Linifanib (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR (IC50: 4 nM), CSF-1R (IC50: 3 nM), Flt-1/3 (IC50: 3/4 nM) and PDGFRβ (IC50...
T2516 Amuvatinib Amuvatinib is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity.
T2586 CabozantinibHOT Cabozantinib (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50s: 0.035, 1.3, 4.6, 7 and 11.3 nM).
T2609 Masitinib Masitinib is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has...
T2668 JNK-IN-8 JNK-IN-8 is an irreversible JNK1/2/4 inhibitor (IC50: 4.7/18.7/1 nM). The selectivity is higher 10-fold than MNK2, Fms and no inhibition of Met, c-Kit, PDGFRβ ...
T3452 ISCK03 ISCK03 is a selective SCF/c-Kit inhibitor.
T4053 AST 487 AST 487 is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.
T4332 c-Kit-IN-1 DCC-2618 is an effective inhibitor of c-Met and c-Kit (IC50s<200 nM).
T6078 SaracatinibHOT Saracatinib (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to Lck, Fyn, Lyn, Blk, Fgr and c-Yes.
T6091 CP-673451 CP-673451 is a specific inhibitor of PDGFRα/β (IC50: 10/1 nM) with antiangiogenic and antitumor activity and the selectivity is higher 450-fold than other ang...
T6097 GNF-5837 GNF-5837 is a specific, and orally bioavailable pan-TRK inhibitor for TrkA/TrkB (IC50: 8/12 nM).
T6137 KRN-633 KRN-633 is an effective VEGFR inhibitor. The IC50s of KRN-633 for VEGFR1, VEGFR2, and VEGFR3 is 170, 160 and 125 nM, respectively.
T6166 Telatinib Telatinib is an effective inhibitor of VEGFR2/3, c-Kit, and PDGFRα. The IC50s of Telatinib forVEGFR2/3, c-Kit and PDGFRα are 6 nM/4 nM, 1 nM, and 15 nM, respe...
T6193 Dovitinib 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...
T6196 PP1 PP1, a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.
T6230 ImatinibHOT matinib is an inhibitor of the receptor tyrosine kinases c-Abl, Bcr-Abl, PDGFR, and c-Kit (IC50: 600/100/100 nM).
T6289 Dovitinib Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit, IC50: 1/2 nM), also effective to class IV (FGFR1/3) and class V ...
T6479 Dovitinib 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 p...
T6711 Tyrphostin AG 1296 Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR.
T4320 Flumatinib Flumatinib is an orally bioavailable tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity.
T5109 Avapritinib Avapritinib is a dual inhibitor of the mutant KIT receptor (KIT D816V, IC50: 0.27 nM) and PDGFRα (PDGFRα D842V, IC50: 0.24 nM).
T0093L SorafenibHOT Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-4/B-Raf).
T1452 AxitinibHOT Axitinib is an orally bioavailable tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.7, 1.6 nM for VEGFR1, VEGFR2, VEGFR3, c-kit, and PDGFRβ, respec...
T5164 Cabozantinib hydrochloride (849217-68-1(free base)) Cabozantinib (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 nM).
T5409 AZD3229 AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors. It demonstrates potent single-digit nM growth inhibition acro...
TQ0080 SU14813 maleate SU14813 maleate is an inhibitor of multi-targeted receptor tyrosine kinases (IC50s: 2, 50, 4, 15 nM for VEGFR1, VEGFR2, PDGFRβ, and KIT).
TQ0235 AC710 AC710 is a potent PDGFR inhibitor (Kds: 0.6, 1, 1.57, 1.3, 1 nM for FLT3, KIT, CSF1R, PDGFRα and PDGFRβ).
T7861 Flumatinib mesylate Flumatinib mesylate is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants.
T2288 Motesanib Motesanib is an orally bioavailable receptor tyrosine kinase inhibitor with potential antineoplastic activity. AMG 706 selectively targets and inhibits vascular...
T6930 Pazopanib 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, ...
T4409 Gilteritinib Gilteritinib is a potent inhibitor at the FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In pr...
Sorafenib tosylate HOT
T0093CAS 475207-59-1
Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).
Pazopanib
T0097LCAS 444731-52-6
Pazopanib, a small molecule inhibitor, inhibits multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits VEGFR-1...
Sunitinib
T0374LCAS 557795-19-4
Sunitinib, a multi-targeted RTK inhibitor, is targeting PDGFRβ and VEGFR2 (Flk-1) with IC50 of 2 nM and 80 nM and also inhibits c-Kit.
Dasatinib HOT
T1448CAS 302962-49-8
Dasatinib is a potent inhibitor of the Bcr-Abl and Src family (IC50s: 0.6, 0.8, 79 and 37 nM for Abl, Src, c-Kit, and c-KitD816V, respectively).
Dasatinib monohydrate
T1448LCAS 863127-77-9
Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promot...
Imatinib Mesylate HOT
T1621CAS 220127-57-1
Imatinib mesylate is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respecti...
Tandutinib
T1667CAS 387867-13-2
Tandutinib (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R ...
Regorafenib HOT
T1792CAS 755037-03-7
Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor (IC50s: 1.5/2.5/4.2/7/13/22 nM for RET/C-RAF/VEGFR2/c-Kit/VEGFR1/PDGFRβ).
XL184
T1797CAS 1140909-48-3
Cabozantinib S-malate is the s-malate salt form of cabozantinib, an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential ...
BX795
T1830CAS 702675-74-9
BX795 is an effective and selective PDK1 inhibitor (IC50: 6 nM), and its selectivity is 140- and 1600-fold for PDK1 over PKA and PKC in cell-free assays, respec...
AZD2932
T1836CAS 883986-34-3
AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3, and c-Kit.
PLX647
T1925CAS 873786-09-5
PLX647 is a highly selective dual FMS/KIT kinase inhibitor (IC50: 28/16 nM).
CEP-32496
T2070CAS 1188910-76-0
CEP-32496 is a highly potent inhibitor of BRAF.
Pexidartinib
T2115CAS 1029044-16-3
Pexidartinib is a capsule formulation containing a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic ...
Motesanib Diphosphate
T2288LCAS 857876-30-3
Motesanib Diphosphate is the orally bioavailable diphosphate salt of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity.
TAK-779
T7499CAS 229005-80-5
TAK-779 is an antagonist of chemokine receptor 5 (CCR5), CCR2b, and CXC chemokine receptor 3 (CXCR3).
Ponatinib HOT
T2372CAS 943319-70-8
Ponatinib is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively).
KI8751
T2446CAS 228559-41-9
KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.
Cediranib
T2500CAS 288383-20-0
Cediranib (AZD2171) is a highly potent (IC50 < 1 nmol/L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro, also inhibits Flt1/4 (IC50: 5 nM...
Linifanib
T2514CAS 796967-16-3
Linifanib (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR (IC50: 4 nM), CSF-1R (IC50: 3 nM), Flt-1/3 (IC50: 3/4 nM) and PDGFRβ (IC50...
Amuvatinib
T2516CAS 850879-09-3
Amuvatinib is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity.
Cabozantinib HOT
T2586CAS 849217-68-1
Cabozantinib (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50s: 0.035, 1.3, 4.6, 7 and 11.3 nM).
Masitinib
T2609CAS 790299-79-5
Masitinib is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has...
JNK-IN-8
T2668CAS 1410880-22-6
JNK-IN-8 is an irreversible JNK1/2/4 inhibitor (IC50: 4.7/18.7/1 nM). The selectivity is higher 10-fold than MNK2, Fms and no inhibition of Met, c-Kit, PDGFRβ ...
ISCK03
T3452CAS 945526-43-2
ISCK03 is a selective SCF/c-Kit inhibitor.
AST 487
T4053CAS 630124-46-8
AST 487 is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.
c-Kit-IN-1
T4332CAS 1225278-16-9
DCC-2618 is an effective inhibitor of c-Met and c-Kit (IC50s<200 nM).
Saracatinib HOT
T6078CAS 379231-04-6
Saracatinib (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to Lck, Fyn, Lyn, Blk, Fgr and c-Yes.
CP-673451
T6091CAS 343787-29-1
CP-673451 is a specific inhibitor of PDGFRα/β (IC50: 10/1 nM) with antiangiogenic and antitumor activity and the selectivity is higher 450-fold than other ang...
GNF-5837
T6097CAS 1033769-28-6
GNF-5837 is a specific, and orally bioavailable pan-TRK inhibitor for TrkA/TrkB (IC50: 8/12 nM).
KRN-633
T6137CAS 286370-15-8
KRN-633 is an effective VEGFR inhibitor. The IC50s of KRN-633 for VEGFR1, VEGFR2, and VEGFR3 is 170, 160 and 125 nM, respectively.
Telatinib
T6166CAS 332012-40-5
Telatinib is an effective inhibitor of VEGFR2/3, c-Kit, and PDGFRα. The IC50s of Telatinib forVEGFR2/3, c-Kit and PDGFRα are 6 nM/4 nM, 1 nM, and 15 nM, respe...
Dovitinib Dilactic Acid
T6193CAS 852433-84-2
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...
PP1
T6196CAS 172889-26-8
PP1, a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.
Imatinib HOT
T6230CAS 152459-95-5
matinib is an inhibitor of the receptor tyrosine kinases c-Abl, Bcr-Abl, PDGFR, and c-Kit (IC50: 600/100/100 nM).
Dovitinib
T6289CAS 405169-16-6
Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit, IC50: 1/2 nM), also effective to class IV (FGFR1/3) and class V ...
Dovitinib Lactate
T6479CAS 915769-50-5
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 p...
Tyrphostin AG 1296
T6711CAS 146535-11-7
Tyrphostin AG 1296 is an inhibitor of PDGFR with IC50 of 0.3-0.5 μM, no activity to EGFR.
Flumatinib
T4320CAS 895519-90-1
Flumatinib is an orally bioavailable tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity.
Avapritinib
T5109CAS 1703793-34-3
Avapritinib is a dual inhibitor of the mutant KIT receptor (KIT D816V, IC50: 0.27 nM) and PDGFRα (PDGFRα D842V, IC50: 0.24 nM).
Sorafenib HOT
T0093LCAS 284461-73-0
Sorafenib is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-4/B-Raf).
Axitinib HOT
T1452CAS 319460-85-0
Axitinib is an orally bioavailable tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.7, 1.6 nM for VEGFR1, VEGFR2, VEGFR3, c-kit, and PDGFRβ, respec...
Cabozantinib hydrochloride (849217-68-1(free base))
T5164CAS T5164
Cabozantinib (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 nM).
AZD3229
T5409CAS 2248003-60-1
AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors. It demonstrates potent single-digit nM growth inhibition acro...
SU14813 maleate
TQ0080CAS 849643-15-8
SU14813 maleate is an inhibitor of multi-targeted receptor tyrosine kinases (IC50s: 2, 50, 4, 15 nM for VEGFR1, VEGFR2, PDGFRβ, and KIT).
AC710
TQ0235CAS 1351522-04-7
AC710 is a potent PDGFR inhibitor (Kds: 0.6, 1, 1.57, 1.3, 1 nM for FLT3, KIT, CSF1R, PDGFRα and PDGFRβ).
Flumatinib mesylate
T7861CAS 895519-91-2
Flumatinib mesylate is a selective inhibitor of c-Abl, PDGFRβ and c-Kit, effectively overcomes drug resistance of certain KIT mutants.
Motesanib
T2288CAS 453562-69-1
Motesanib is an orally bioavailable receptor tyrosine kinase inhibitor with potential antineoplastic activity. AMG 706 selectively targets and inhibits vascular...
Pazopanib HCl
T6930CAS 635702-64-6
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, ...
Gilteritinib
T4409CAS 1254053-43-4
Gilteritinib is a potent inhibitor at the FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In pr...