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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".

  • Edicotinib
    T151991142363-52-7
    Edicotinib (JNJ-527) is a brain penetrant and orally active inhibitor of the colony-stimulating factor-1 receptor (IC50: 3.2 nM). It shows less inhibitory effects on KIT and FLT3 (IC50: 20 nM and 190 nM). It has the potential for Alzheimer's disease and rheumatoid arthritis treatment.
    • $64
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  • Regorafenib
    T1792755037-03-7
    Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ and is orally active. Regorafenib has antitumor and anti-angiogenic activity.
    • $30
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  • Sorafenib
    T0093L284461-73-0
    Sorafenib (Bay 43-9006) is a multikinase inhibitor that inhibits Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. Sorafenib has antitumor activity and can induce autophagy and apoptosis as well as agonistic iron death.
    • $34
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  • Pexidartinib
    T21151029044-16-3
    Pexidartinib (PLX-3397) is a capsule formulation containing a small-molecule receptor tyrosine kinase (RTK) inhibitor of KIT, CSF1R and FLT3 with potential antineoplastic activity.
    • $40
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  • Avapritinib
    T51091703793-34-3
    Avapritinib (BLU-285) is a dual inhibitor of the mutant KIT receptor (KIT D816V, IC50: 0.27 nM) and PDGFRα (PDGFRα D842V, IC50: 0.24 nM).
    • $80
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  • Gilteritinib
    T44091254053-43-4
    Gilteritinib (ASP2215) 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 preClinicalal studies, gilteritinib showed strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 Clinicalal trials for acute myeloid leukemia.
    • $34
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  • Lenvatinib
    T0520417716-92-8
    Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4/5.2 nM). Lenvatinib has strong anti-tumor activity.
    • $40
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  • Cabozantinib
    T2586849217-68-1
    Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity.
    • $39
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    TargetMol | Citations Cited
  • Pazopanib
    T0097L444731-52-6
    Pazopanib (GW786034), a small molecule inhibitor, inhibits multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits VEGFR-1, -2 and -3, c-kit and PDGF-R, which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated.
    • $42
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  • Imatinib impurities3
    T67847404844-11-7
    Imatinib impurities3 is a protein kinases inhibitor with IC50 values of 6.95uM, 0.245uM, 0.139uM for ABL1 wt, KIT wt, PDGFRR wt, respectively.
    • $50
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  • c-Kit-IN-3
    T106512363169-01-9In house
    c-Kit-IN-3 is a selective inhibitor of c-KIT kinase with IC50s of 4 nM and 8 nM for c-Kit (wt) and c-Kit (T670I).
    • $79
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  • Cabozantinib hydrochloride
    T51641817759-42-4
    Cabozantinib hydrochloride (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).
    • $37
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  • N-Desethylsunitinib hydrochloride
    T12145L1261432-05-6
    N-Desethylsunitinib hydrochloride is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ, and KIT inhibitor.
    • $133
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  • PP1
    T6196172889-26-8
    PP1 (AGL 1872), a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.
    • $34
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  • Imatinib Mesylate
    T1621220127-57-1
    Imatinib Mesylate (STI-571) 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, respectively).
    • $54
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  • Axitinib
    T1452319460-85-0
    Axitinib (AG-013736) 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, respectively.
    • $33
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  • Dasatinib monohydrate
    T1448L863127-77-9
    Dasatinib monohydrate (BMS-354825 Monohydrate) is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib monohydrate binds to and inhibits the growth-promoting activities of these kinases. Apparently, because of its less stringent binding affinity for the BCR-ABL kinase, Dasatinib monohydrate has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations.
    • $33
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  • Dasatinib
    T1448302962-49-8
    Dasatinib (BMS-354825) is a tyrosine kinase inhibitor that inhibits Src and Bcr-Abl (Ki=16/30 pM) and is orally active and ATP-competitive. Dasatinib has antitumor activity and is used in the treatment of leukemia and lymphoma.
    • $37
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  • Imatinib
    T6230152459-95-5
    Imatinib (STI571) is a multi-targeted receptor tyrosine kinase inhibitor that selectively inhibits the kinase activities of BCR/ABL, v-Abl, PDGFR, and c-kit with oral activity. Imatinib has antitumor activity for the treatment of chronic granulocytic leukemia.
    • $36
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  • JNK-IN-8
    T26681410880-22-6
    JNK-IN-8 (JNK Inhibitor XVI) 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 in A375 cell line.
    • $39
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  • Sunitinib
    T0374L557795-19-4
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM). Sunitinib has antitumor activity and can be used for the treatment of kidney cancer and gastrointestinal tumors.
    • $53
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  • Ponatinib
    T2372943319-70-8
    Ponatinib (AP24534) 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).
    • $50
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  • Motesanib Diphosphate
    T2288L857876-30-3
    Motesanib Diphosphate (AMG 706) is the orally bioavailable diphosphate salt of a multiple-receptor tyrosine kinase inhibitor with potential antineoplastic activity.
    • $36
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  • JNJ-38158471
    T22349951151-97-6
    JNJ-38158471 (CS-2660), a highly selective, orally available, well tolerated VEGFR2 inhibitor with IC50 of 40 nM, inhibits closely related tyrosine kinases such as Ret and Kit with IC50 of 180 nM and 500 nM.
    • $101
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  • Ki20227
    T4315623142-96-1
    Ki-20227 is a specific c-Fms tyrosine kinase(CSF1R) inhibitor (IC50: 2 nM). It also has certain inhibitory against VEGFR2(IC50: 12 nM) and c-Kit/PDGFRβ(IC50: 451/217 nM), respectively.
    • $39
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  • KG5
    T41003877874-85-6
    KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities.
    • $48
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  • Labuxtinib
    T798511426449-01-5
    Labutinib is a selective inhibitor of the c-kit tyrosine kinase [1].
    • $198
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  • SU14813
    T7945627908-92-3
    SU14813 is a multi-receptor tyrosine kinase inhibitor with potent antiangiogenesis and antitumor activity (IC50s of 50, 2, 4, 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT).
    • $47
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  • M4205
    T96892590556-80-0
    M4205 is an inhibitor of c-Kit exhibiting high activity on c-Kit mutations in exons 11, 13, 17.
    • $98
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  • Multi-kinase inhibitor 1
    T4191778274-97-8
    Multi-kinase inhibitor 1 (Multi-kinase inhibitor I) is a Multi-kinase inhibitor.
    • $33
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  • Sunitinib Malate
    T0374341031-54-7
    Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.
    • $37
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  • Masitinib mesylate
    T85441048007-93-7
    Masitinib mesylate (AB-1010 mesylate) is a selective and orally bioavailable c-Kit inhibitor (IC50 of 200 nM,540/800 nM,510 nM for human recombinant c-Kit;PDGFRα/β;LynB,respectively).
    • $30
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  • GNF-5837
    T60971033769-28-6
    GNF-5837 is a specific, and orally bioavailable pan-TRK inhibitor for TrkA/TrkB (IC50: 8/12 nM).
    • $43
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    TargetMol | Citations Cited
  • AC710
    TQ02351351522-04-7
    AC710 is a potent PDGFR inhibitor (Kds: 0.6, 1, 1.57, 1.3, 1 nM for FLT3, KIT, CSF1R, PDGFRα and PDGFRβ).
    • $30
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  • SU14813 maleate
    TQ0080849643-15-8
    SU14813 maleate is an inhibitor of multi-targeted receptor tyrosine kinases (IC50s: 2, 50, 4, 15 nM for VEGFR1, VEGFR2, PDGFRβ, and KIT).
    • $53
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  • Vimseltinib
    T106521628606-05-2
    Vimseltinib (DCC-3014) is a c-FMS (CSF-IR) and c-Kit dual inhibitor (IC50s: <0.01 μM and 0.1-1 μM).
    • $96
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  • Regorafenib monohydrate
    T1792L1019206-88-2
    Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.
    • $30
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  • Sorafenib tosylate
    T0093475207-59-1
    Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).
    • $37
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  • AST 487
    T4053630124-46-8
    AST 487 (NVP-AST 487) is a RET kinase inhibitor, inhibiting RET autophosphorylation and activation of downstream effectors. It also can inhibit Flt-3.
    • $31
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  • Linifanib
    T2514796967-16-3
    Linifanib (AL-39324) (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: 66 nM). Linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3).
    • $43
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  • Anti-Mouse CD117 Antibody
    T80558
    Anti-Mouse CD117 Antibody, a rat-derived IgG2b isotype, acts as an inhibitor specific to the mouse CD117 antigen.
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  • AZD3229
    T54092248003-60-1
    AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors. It demonstrates potent single-digit nM growth inhibition across a broad cell panel.
    • $62
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  • Dasatinib hydrochloride
    T22303854001-07-3
    Dasatinib hydrochloride (BMS-354825 HCl) (BMS-354825) hydrochloride is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib hydrochloride hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib hydrochloride hydrochloride also induces Apoptosis and Autophagy.
    • $38
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  • c-Kit-IN-5-1
    T222561003311-62-3
    c-Kit-IN-5-1 (AMG-25) is a novel selective and potent c-Kit inhibitor.
    • $1,480
    Backorder
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  • PD180970
    T23128287204-45-9
    PD180970 is an inhibitor of Bcr-Abl with IC50s of 5 nM, 0.8 nM and 50 nM for the autophosphorylation of p210Bcr-Abl, Src and Kit. PD180970 can be used in studies about chronic myelogenous leukemia.
    • $53
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  • OSI-930
    T2624728033-96-3
    OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.
    • $47
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  • Masitinib
    T2609790299-79-5
    Masitinib (AB1010) 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 been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet and has been available for veterinaries since 2011.
    • $31
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  • N-Desmethyl imatinib
    T11641404844-02-6
    N-Desmethyl imatinib (Imatinib metabolite N-Desmethyl imatinib) is a metabolite of Imatinib, which is a multi-target inhibitor of c-Kit, v-Abl, and PDGFR.
    • $84
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  • Dovitinib lactate
    T7104692737-80-7
    Dovitinib lactate (TKI-258 lactate)(TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) (IC50 :5 nM).
    • $47
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  • BX795
    T1830702675-74-9
    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, respectively. Meanwhile, the selectivity for PDK1 is 100-fold than GSK3β.
    • $54
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