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Home >> Signaling Pathways >> Tyrosine Kinase >> c-Kit

c-Kit(肥大/干细胞生长因子受体)

C-kit is a type of receptor tyrosine kinase and a type of tumor marker, also called CD117 and stem cell factor receptor.

  1. Cat.No. 产品名称 Information
  2. GC69050 Elenestinib Elenestinib (BLU-263 ) 是一种有效的口服活性酪氨酸激酶 (b>tyrosine kinase) 抑制剂。Elenestinib 具有研究系统性肥大细胞增多症（SM）的潜力。
  3. GC68727 Barzolvolimab Barzolvolimab (CDX 0159) 是一种人源化抗 KIT IgG1 单克隆抗体。Barzolvolimab 特异性并有效抑制 KIT 的激活。Barzolvolimab 可以减少慢性诱导性荨麻疹的皮肤肥大细胞和疾病活动。
  4. GC25313 CS-2660 (JNJ-38158471) CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. CS-2660 (JNJ-38158471) also inhibits closely related tyrosine kinases such as RET (c-RET) and Kit (c-Kit) with IC50 of 180 nM and 500 nM，while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3.
  5. GC65948 c-Kit-IN-5-1 AMG-25 is a novel potent and selective c-Kit inhibitor.
  6. GC64810 Bezuclastinib Bezuclastinib (CGT9486; PLX 9486) 是一种有效的 c-kit 和c-kit D816V 抑制剂，0.0001
  7. GC62314 M4205 M4205 是一种 c-KIT 抑制剂，对 c-KIT V654A 作用的 IC50 值为 10 nM。M4205 对外显子 11, 13, 17 突变型 c-KIT 具有很高的活性。
  8. GC62145 Chiauranib Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy.
  9. GC60930 Imatinib D4 ImatinibD4(STI571D4)是Imatinib(STI571)的氘代物。Imatinib是一种口服生物可用的酪氨酸激酶抑制剂，可选择性抑制BCR/ABL，v-Abl，PDGFR，c-kit激酶活性。
  10. GC39612 Imatinib D8 Imatinib D8 (STI571 D8) 是 Imatinib (STI571) 的氘代物。Imatinib 是一种口服生物可用的酪氨酸激酶抑制剂，可选择性抑制 BCR/ABL，v-Abl，PDGFR，c-kit 激酶活性。
  11. GC38853 Tandutinib hydrochloride An antagonist of PDGFRβ, FLT3, and c-Kit
  12. GC38757 c-Kit-IN-3 hydrochloride c-Kit-IN-3 hydrochloride (Compound 18) 是一种有效的 c-KIT 激酶抑制剂，对 BaF3-tel-c-KIT (IC50 为 4 nM) 和广泛的耐药性突变体 (对 BaF3-tel-c-KIT-T670I 的 IC50 为 8 nM)，具有很高的生物利用度。
  13. GC38756 c-Kit-IN-3 D-tartrate c-Kit-IN-3 (D-tartrate) (Compound 18) 是一种有效的 c-KIT kinase 激酶抑制剂，对 BaF3-tel-c-KIT (IC50 为 4 nM) 和广泛的耐药性突变体 (对 BaF3-tel-c-KIT-T670I 的IC50为 8 nM)，具有很高的生物利用度。
  14. GC38595 c-Kit-IN-3 c-Kit-IN-3 (Compound 18) 是一种有效的 c-KIT 激酶抑制剂，IC50 为 4 nM。c-Kit-IN-3 在生化分析中显示出对 c-KIT 激酶和多种耐药突变体的强大效价，并具有很高的生物利用度。
  15. GC37808 Toceranib phosphate A multi-targeted receptor tyrosine kinase inhibitor
  16. GC37538 Ripretinib A KIT and PDGFRα inhibitor
  17. GC36546 Masitinib mesylate An inhibitor of c-Kit
  18. GC36438 Lenvatinib mesylate An inhibitor of VEGFR2 and VEGFR3
  19. GC35705 c-Kit-IN-2 c-Kit-IN-2 是一种 c-KIT 抑制剂，IC50 值为 82 nM，对三种 GIST 细胞系 GIST882、GIST430 和 GIST48 均有较好的抗增殖活性，GI50 值分别为 3、1 和 2 nM。
  20. GC35685 CHMFL-KIT-033 CHMFL-KIT-033 是一种有效、可选择性的 c-KIT T670I 突变型的抑制剂, IC50 值为 0.045 μM。用于胃肠道间质瘤 (GISTs) 的治疗。
  21. GC35682 CHMFL-ABL/KIT-155 CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34) 是一种高效的，具有口服活性的 type II ABL/c-KIT 双激酶抑制剂 (IC50 分别为 46 nM 和 75 nM)，对 BLK (IC50=81 nM), CSF1R (IC50=227 nM), DDR1 (IC50=116 nM), DDR2 (IC50=325 nM), LCK (IC50=12 nM), PDGFRβ (IC50=80 nM) 激酶也具有明显的抑制活性。CHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155) 阻止细胞周期进展和诱导细胞凋亡。
  22. GC34708 Pexidartinib hydrochloride A multi-targeted receptor tyrosine kinase inhibitor
  23. GC33362 Amuvatinib hydrochloride (MP470 hydrochloride) A multi-targeted RTK inhibitor
  24. GC33246 AZD3229 Tosylate An inhibitor of c-Kit-driven cell proliferation
  25. GC33027 AZD3229 An inhibitor of c-Kit-driven cell proliferation
  26. GC32867 Flumatinib (HHGV678) A Bcr-Abl inhibitor
  27. GC19332 Sitravatinib A multi-kinase inhibitor
  28. GC19074 Avapritinib A dual inhibitor of KIT and PDGFRα mutant kinases
  29. GC18167 AC710 A PDGFR family kinase inhibitor
  30. GC13961 ISCK03 An inhibitor of SCF/c-kit signaling
  31. GC12222 Pexidartinib (PLX3397) A multi-targeted receptor tyrosine kinase inhibitor
  32. GC17959 AZD2932 A multi-kinase inhibitor
  33. GC15075 PLX647 A dual inhibitor of FMS and KIT
  34. GC10314 Imatinib (STI571) 伊马替尼 (STI571) (STI571) 是一种口服生物可利用的酪氨酸激酶抑制剂，可选择性抑制 BCR/ABL、v-Abl、PDGFR 和 c-kit 激酶活性。伊马替尼 (STI571) (STI571) 通过在 ATP 结合位点附近结合而起作用，将其锁定在封闭或自我抑制的构象中，从而半竞争性地抑制蛋白质的酶活性。伊马替尼 (STI571) 也是 SARS-CoV 和 MERS-CoV 的抑制剂。
  35. GC14292 Apatinib Mesylate

    A selective VEGFR2 inhibitor
  36. GC15254 Tandutinib (MLN518) An antagonist of PDGFRβ, FLT3, and c-Kit
  37. GC13914 Flumatinib mesylate A Bcr-Abl inhibitor
  38. GC11763 Telatinib (BAY 57-9352) A multi-kinase inhibitor
  39. GC12730 Pazopanib Hydrochloride A multi-kinase inhibitor
  40. GC11336 Motesanib Diphosphate (AMG-706) A multikinase inhibitor
  41. GC15454 Lenvatinib (E7080)

    An inhibitor of VEGFR2 and VEGFR3
  42. GC14957 OSI-930 A dual inhibitor of Kit and VEGFR2
  43. GC15779 Cabozantinib (XL184, BMS-907351) A VEGFR2 inhibitor
  44. GC13547 Dovitinib (TKI-258, CHIR-258) A multi-kinase inhibitor
  45. GC11759 Imatinib Mesylate (STI571) An inhibitor of c-Abl, Bcr-Abl, PDGFR, and c-Kit
  46. GC17958 Linifanib (ABT-869) A dual VEGFR and PDGFR family kinase inhibitor
  47. GC13410 Masitinib (AB1010) An inhibitor of c-Kit
  48. GC10719 Toceranib A multi-targeted receptor tyrosine kinase inhibitor
  49. GC14315 SU14813 maleate A dual VEGFR and PDGFR family kinase inhibitor
  50. GC14733 SU14813 A dual VEGFR and PDGFR family kinase inhibitor
  51. GC13012 Motesanib Motesanib (AMG 706) 是一种有效的 ATP 竞争性 VEGFR1/2/3 抑制剂，IC50 分别为 2 nM/3 nM/6 nM，对 Kit 具有相似的活性，对 VEGFR 的选择性比对 VEGFR 的选择性高约 10 倍PDGFR 和 Ret。

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