2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. c-Kit

c-Kit

SCFR; CD117

c-Kit

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c-Kit (Mast/stem cell growth factor receptor, SCFR or CD117) is a proteinthat in humans is encoded by the KIT gene. c-Kit (CD117) is an important cell surface marker used to identify certain types of hematopoietic(blood) progenitors in the bone marrow. c-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. c-Kit is a receptor tyrosine kinase type III, which binds to stem cell factor. When c-Kit binds to stem cell factor (SCF) it forms adimer that activates its intrinsic tyrosine kinase activity, that in turn phosphorylates and activates signal transduction molecules that propagate the signal in the cell. Signalling through c-Kit plays a role in cell survival, proliferation, and differentiation.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-10331A
    Regorafenib monohydrate
    		Inhibitor 99.96%
    Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/Flt-1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.
    Regorafenib monohydrate
  • HY-15002
    AST 487
    		Inhibitor 99.42%
    AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.
    AST 487
  • HY-13904
    Flumatinib
    		Inhibitor 99.94%
    Flumatinib (HHGV678) is an orally available, selective inhibitor of Bcr-Abl. Flumatinib inhibits c-Abl, PDGFRβ and c-Kit with IC50s of 1.2 nM, 307.6 nM and 665.5 nM, respectively.
    Flumatinib
  • HY-10206
    Amuvatinib
    		Inhibitor 99.47%
    Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
    Amuvatinib
  • HY-145557
    Bezuclastinib
    		Inhibitor 98.59%
    Bezuclastinib (CGT9486) is an orally active, highly selective tyrosine kinase inhibitor with potent activity against KIT D816V. Bezuclastinib can be used for the research of nonadvanced systemic mastocytosis (NonAdvSM).
    Bezuclastinib
  • HY-P99462
    Barzolvolimab
    		Inhibitor 99.83%
    Barzolvolimab (CDX 0159) is a humanized anti-KIT IgG1 monoclonal antibody. Barzolvolimab specificity and potently inhibits KIT activation by SCF. Barzolvolimab can reduce skin mast cells and disease activity in chronic inducible urticaria.
    Barzolvolimab
  • HY-10209A
    Masitinib mesylate
    		Inhibitor 99.83%
    Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFRα/β (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity.
    Masitinib mesylate
  • HY-10501
    SU14813
    		Inhibitor 99.63%
    SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC50s of 50, 2, 4, 15 nM for VEGFR2/KDR/Flk-1, VEGFR1/Flt-1, PDGFRβ and KIT.
    SU14813
  • HY-101443
    ISCK03
    		Inhibitor 99.50%
    ISCK03 is a SCF/c-Kit and CD117-specific inhibitor. ISCK03 significantly inhibits c-Kit phosphorylation at 10 μM.
    ISCK03
  • HY-10228
    Motesanib
    		Inhibitor 99.96%
    Motesanib (AMG 706) is a potent ATP-competitive inhibitor of VEGFR1/Flt-1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is appr 10-fold more selective for VEGFR than PDGFR and Ret.
    Motesanib
  • HY-13894
    Tyrphostin AG1296
    		Inhibitor 99.69%
    Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.
    Tyrphostin AG1296
  • HY-132166
    M4205
    		Inhibitor 99.47%
    M4205 is a c-KIT inhibitor, with an IC50 of 10 nM for c-KIT V654A. M4205 has high activity on c-KIT mutations in exon 11, 13, 17.
    M4205
  • HY-136256
    Vimseltinib
    		Inhibitor 99.08%
    Vimseltinib (DCC-3014) is a c-FMS (CSF-IR) and c-Kit dual inhibitor extracted from patent WO2014145025A2, Compound Example 10, has IC50s of <0.01 μM and 0.1-1 μM, respectively.
    Vimseltinib
  • HY-10527
    Telatinib
    		Inhibitor 99.60%
    Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2/KDR/Flk-1, VEGFR3/Flt-4, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively.
    Telatinib
  • HY-112802
    AZD3229
    		Inhibitor 99.69%
    AZD3229 is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors. AZD3229 inhibits c-KIT with an IC50 value of 223.3 nM.
    AZD3229
  • HY-10202
    Tandutinib
    		Inhibitor 99.48%
    Tandutinib (MLN518) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib can be used for acute myelogenous leukemia (AML). Tandutinib has the ability to cross the blood-brain barrier.
    Tandutinib
  • HY-10330
    Toceranib
    		Inhibitor
    Toceranib phosphate (SU11654 phosphate) is an orally active receptor tyrosine kinase (RTK) inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit with Kis of 5 and 6 nM for PDGFRβ and VEGFR2/KDR/Flk-1/VEGFR2/KDR/Flk-1, respectively. Toceranib phosphate (SU11654 phosphate) has antitumor and antiangiogenic activity, and used in the treatment of canine mast cell tumors.
    Toceranib
  • HY-109190
    Seralutinib
    		Inhibitor 99.94%
    Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib also targets to CSF1R and c-KIT with IC50s of 8 nM and 14 nM, respectively. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension.
    Seralutinib
  • HY-10204
    OSI-930
    		Inhibitor 98.57%
    OSI-930 is an orally selective inhibitor of Kit, VEGFR2/KDR/Flk-1 and CSF-1R (c-Fms) with IC50s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 has antitumor activity.
    OSI-930
  • HY-13838
    PLX647
    		Inhibitor 99.79%
    PLX647 is an orally active, highly specific dual FMS and KIT kinase inhibitor, with IC50s of 28 and 16 nM, respectively. PLX647 shows selectivity for FMS and KIT over a panel of 400 kinases at a concentration of 1 μM except FLT3 and VEGFR2/KDR/Flk-1 (IC50s=91 and 130 nM, respectively).
    PLX647
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity