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-168579
    c-Kit-IN-6
    Inhibitor
    c-Kit-IN-6 (Compound 101) is an inhibitor of c-Kit with an IC50 value ranging between 100 nM and 1 μM. Additionally, c-Kit-IN-6 can inhibit the proliferation of GIST430 and BaF3 mutant cells.
    c-Kit-IN-6
  • HY-170228
    c-Kit-IN-9
    Inhibitor
    Kit-IN-9 (Compound D9) is an inhibitor of c-Kit. c-Kit-IN-9 inhibits the inflammatory responses in J774A.1, RAW264.7, MPMs cells and lung tissues by blocking the activation of the NF-κB pathway induced by LPS (HY-D1056). Meanwhile, c-Kit-IN-9 exhibits good anti-inflammatory activities in acute lung injury and sepsis mouse models. c-Kit-IN-9 can be used in the research of acute lung injury and related inflammatory diseases.
    c-Kit-IN-9
  • HY-146697
    IHMT-TRK-284
    Inhibitor
    IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC50 values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies.
    IHMT-TRK-284
  • HY-10638
    AP23464
    Inhibitor
    AP23464 is an ATP-based inhibitor for Kit, that inhibits the phosphorylation of Kit wildtype and mutants, with IC50 of 5-85 nM. AP23464 inhibits the proliferation of Kit mutated cells (IC50 is 3-20 nM), arrests the cell cycle at G0/G1 phase, and induces apoptosis in Kit mutated cells.
    AP23464
  • HY-13645
    Henatinib
    Inhibitor
    Henatinib is an orally active small-molecule multikinase inhibitor that has demonstrated broad and potent antitumor activities. Henatinib inhibits the activity of VEGFR-2, c-kit, PDGFR with IC50 values of 0.6 nM, 3.3 nM and 41.5 nM, respectively. Henatinib significantly inhibits VEGFR-2 phosphorylation and its downstream signal pathway in human umbilical vein endothelial cells (HUVECs).
    Henatinib
  • HY-W709612
    Regorafenib N-oxide and N-desmethyl (M5)-d3-1
    Regorafenib N-oxide and N-desmethyl (M5)-d3-1 (N-Desmethyl regorafenib N-oxide-d3-1) is the deuterium labeled Regorafenib N-oxide and N-desmethyl (M5) (HY-108226). Regorafenib N-oxide and N-desmethyl (M5) (N-Desmethyl regorafenib N-oxide) is an active metabolite of Sorafenib (HY-10201) and can be metabolized by CYP3A4.
    Regorafenib N-oxide and N-desmethyl (M5)-d<sub>3</sub>-1
  • HY-12009R
    Pazopanib Hydrochloride (Standard)
    Inhibitor
    Pazopanib (Hydrochloride) (Standard) is the analytical standard of Pazopanib (Hydrochloride). This product is intended for research and analytical applications. Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
    Pazopanib Hydrochloride (Standard)
  • HY-10209AR
    Masitinib mesylate (Standard)
    Inhibitor
    Masitinib (mesylate) (Standard) is the analytical standard of Masitinib (mesylate). This product is intended for research and analytical applications. 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 (Standard)
  • HY-50905R
    Dovitinib (Standard)
    Inhibitor
    Dovitinib (Standard) is the analytical standard of Dovitinib. This product is intended for research and analytical applications. Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity.
    Dovitinib (Standard)
  • HY-10206R
    Amuvatinib (Standard)
    Inhibitor
    Amuvatinib (Standard) is the analytical standard of Amuvatinib. This product is intended for research and analytical applications. 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 (Standard)
  • HY-108226
    Regorafenib N-oxide and N-desmethyl (M5)
    Inhibitor
    Regorafenib N-oxide and N-desmethyl (M5) (N-Desmethyl regorafenib N-oxide) is an active metabolite of Sorafenib (HY-10201) and can be metabolized by CYP3A4.
    Regorafenib N-oxide and N-desmethyl (M5)
  • HY-107458
    AP23848
    Inhibitor
    AP23848 is an ATP-dependent kinase inhibitor that effectively and selectively targets the Kit activation loop mutation both in vitro and in vivo, showing anti-tumor activity. AP23848 can inhibit the phosphorylation of the activated Kit mutation and tumor growth in mice, making it suitable for targeting diseases with the D816V mutation, such as systemic mastocytosis (SM) and acute myeloid leukemia (AML) research.
    AP23848
  • HY-10331R
    Regorafenib (Standard)
    Inhibitor
    Regorafenib (Standard) is the analytical standard of Regorafenib. This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) 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 VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity.
    Regorafenib (Standard)
  • HY-16749R
    Pexidartinib (Standard)
    Inhibitor
    Pexidartinib (Standard) is the analytical standard of Pexidartinib. This product is intended for research and analytical applications. Pexidartinib (PLX-3397) is a potent, orally active, selective, and ATP-competitive colony stimulating factor 1 receptor (CSF1R or M-CSFR) and c-Kit inhibitor, with IC50s of 20 and 10 nM, respectively. Pexidartinib (PLX-3397) exhibits 10- to 100-fold selectivity for c-Kit and CSF1R over other related kinases. Pexidartinib (PLX-3397) induces cell apoptosis and has anti-tumor activity.
    Pexidartinib (Standard)
  • HY-10202AR
    Tandutinib hydrochloride (Standard)
    Inhibitor
    Tandutinib (hydrochloride) (Standard) is the analytical standard of Tandutinib (hydrochloride). This product is intended for research and analytical applications. Tandutinib hydrochloride (MLN518 hydrochloride) 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 hydrochloride can be used for acute myelogenous leukemia (AML). Tandutinib hydrochloride has the ability to cross the blood-brain barrier.
    Tandutinib hydrochloride (Standard)
  • HY-W754911
    Avapritinib-d3
    Inhibitor
    Avapritinib-d3 (BLU-285-d3) is deuterium labeled Avapritinib. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2.
    Avapritinib-d<sub>3</sub>
  • HY-10208S2
    Pazopanib-d3
    Inhibitor
    Pazopanib-d3 (GW786034-d3) is deuterium labeled Pazopanib. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
    Pazopanib-d<sub>3</sub>
  • HY-169517
    Protein kinase inhibitor 10
    Inhibitor
    Protein kinase inhibitor 10 is a protein kinase inhibitor with IC50 values of 28.9, 13.6, and 2.41 μM for TAM receptor, FAK, and KIT, respectively. Protein kinase inhibitor 10 can inhibit abnormal and excessive cell proliferation, showing promise for research in cancer therapy.
    Protein kinase inhibitor 10
  • HY-13894R
    Tyrphostin AG1296 (Standard)
    Inhibitor
    Tyrphostin AG1296 (Standard) is the analytical standard of Tyrphostin AG1296. This product is intended for research and analytical applications. 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 (Standard)
  • HY-15463S3
    Imatinib-13C,d3
    Inhibitor
    Imatinib-13C,d3 (STI571-13C,d3) is 13C 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-<sup>13</sup>C,d<sub>3</sub>
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity