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Ripretinib

CAS No. : 1442472-39-0

MCE 站：Ripretinib

产品活性：Ripretinib (DCC-2618) 是一种口服生物利用的，选择性的 KIT 和 PDGFRA 开关控制抑制剂。Ripretinib (DCC-2618) 专门针对 KIT 和 PDGFRA 的野生型和突变型并与之结合在其开关口袋结合位点，从而防止这些激酶从无活性构象转变为有活性构象，并使它们的野生型和突变体形式失活。Ripretinib (DCC-2618) 还抑制多个其他激酶靶点，如 FLT3，KDR (VEGFR-2)。Ripretinib (DCC-2618) 具有抗肿瘤作用并诱导细胞凋亡。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：c-Kit  |  PDGFR  |  FLT3  |  VEGFR  |  Apoptosis

In Vitro: Ripretinib (DCC-2618) suppresses phosphorylation of KIT and decreases the expression of phosphosphorylated (p)STAT5, pAKT and pERK1/2 in neoplastic mast cells. Ripretinib inhibits the growth of ROSA^{KIT K509I} cells with an IC₅₀ of 34 ± 10 nM, and also induces apoptosis in these cells. Ripretinib (0.1-1.0 μM) inhibits IgE-dependent histamine release from basophils and spontaneous tryptase release from neoplastic mast cells, and also counteracts growth and survival of leukemic monocytes and blast cells at 0.01-5 μM.
Ripretinib (DCC-2618) is a pan-KIT and PDGFRA inhibitor, shows cytotoxic activity against gastrointestinal stromal tumors.

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