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

c-Kit

SCFR; CD117

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-10981S
    Lenvatinib-d4
    Inhibitor 99.59%
    Lenvatinib-d4 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities[1][2].
    Lenvatinib-d<sub>4</sub>
  • HY-12960
    SKLB4771
    Inhibitor 98.08%
    SKLB4771 is a potent and selective Flt3 inhibitor with an IC50 value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue.
    SKLB4771
  • HY-10527C
    Telatinib mesylate
    Inhibitor 99.74%
    Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2/KDR/Flk-1, VEGFR3/Flt-4, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively.
    Telatinib mesylate
  • HY-112802A
    AZD3229 Tosylate
    Inhibitor 99.80%
    AZD3229 Tosylate is a potent pan-KIT mutant inhibitor for the treatment of gastrointestinal stromal tumors.
    AZD3229 Tosylate
  • HY-15198
    KG5
    Inhibitor 99.79%
    KG5 is an orally active dual PDGFRβ and B-Raf allosteric inhibitor. KG5 also inhibits Flt3, KIT and c-Raf. KG5 has anticancer, antiangiogenic activities.
    KG5
  • HY-12009S
    Pazopanib-13C,d3 hydrochloride
    Pazopanib-13C,d3 (hydrochloride) is the deuterium and 13C labeled Pazopanib hydrochloride[1]. Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1/Flt-1, VEGFR2/KDR/Flk-1, VEGFR3/Flt-4, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively[2][3].
    Pazopanib-<sup>13</sup>C,d<sub>3</sub> hydrochloride
  • HY-156619
    Labuxtinib
    Inhibitor 99.76%
    Labuxtinib is c-kit tyrosine kinase inhibitor.
    Labuxtinib
  • HY-10230S
    Midostaurin-d5
    Inhibitor ≥98.0%
    Midostaurin-d5 is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, VEGFR2/KDR/Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/Flt-1/2 with IC50s ranging from 22-500 nM[1].
    Midostaurin-d<sub>5</sub>
  • HY-18317
    JNJ-38158471
    Inhibitor
    JNJ-38158471 is a well tolerated, orally available, highly selective VEGFR-2 inhibitor, with an IC50 of 40 nM. JNJ-38158471 also inhibits Ret and Kit with IC50s of 180 and 500 nM, respectively.
    JNJ-38158471
  • HY-15814
    HG-7-85-01
    Inhibitor 99.94%
    HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, VEGFR2/KDR/Flk-1 and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression.
    HG-7-85-01
  • HY-15463S2
    Imatinib-d3 hydrochloride
    Imatinib-d3 (hydrochloride) is the deuterium labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
    Imatinib-d<sub>3</sub> hydrochloride
  • HY-10208S
    Pazopanib-d6
    Inhibitor ≥98.0%
    Pazopanib-d6 is the deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1/Flt-1, VEGFR2/KDR/Flk-1, VEGFR3/Flt-4, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
    Pazopanib-d<sub>6</sub>
  • HY-16961A
    Sitravatinib malate
    Inhibitor
    Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3/Flt-4, VEGFR2/KDR/Flk-1, VEGFR1/Flt-1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
    Sitravatinib malate
  • HY-B0062
    Dovitinib lactate hydrate
    Inhibitor
    Dovitinib lactate hydrate (TKI258 lactate hydrate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/Flt-1/2/3 and PDGFRα, respectively.
    Dovitinib lactate hydrate
  • HY-13016A
    Cabozantinib hydrochloride
    Inhibitor
    Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2/KDR/Flk-1 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis.
    Cabozantinib hydrochloride
  • HY-10331B
    Regorafenib mesylate
    Inhibitor
    Regorafenib (BAY 73-4506) mesylate 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 mesylate shows very robust antitumor and antiangiogenic activity.
    Regorafenib mesylate
  • HY-101034
    CHMFL-ABL/KIT-155
    Inhibitor
    CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) is a highly potent and orally active type II ABL/c-KIT dual kinase inhibitor (IC50s of 46 nM and 75 nM, respectively), and it also presents significant inhibitory activities to BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM) and PDGFRβ (IC50=80 nM) kinases. CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) arrests cell cycle progression and induces apoptosis.
    CHMFL-ABL/KIT-155
  • HY-152839A
    Elenestinib phosphate
    Inhibitor
    Elenestinib phosphate (BLU-263 phosphate) is a potent and orally active tyrosine kinase inhibitor. Elenestinib phosphate has the potential for the research of systemic mastocytosis (SM).
    Elenestinib phosphate
  • HY-128589
    CHMFL-KIT-033
    Inhibitor
    CHMFL-KIT-033 is a potent and selective inhibitor of c-KIT T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC50 of 0.045 μM.
    CHMFL-KIT-033
  • HY-10206A
    Amuvatinib hydrochloride
    Inhibitor
    Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.
    Amuvatinib hydrochloride
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity