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Midostaurin
CAS No. : 120685-11-2
MCE 国际站:Midostaurin
产品活性:Midostaurin (PKC412; CGP 41251) 是一种具有口服活性的可逆多靶点蛋白激酶抑制剂。Midostaurin 抑制 PKCα/β/γ、Syk、Flk-1、Akt、PKA、c-Kit、c-Fgr、c-Src、FLT3、PDFRβ 和 VEGFR1/2,IC50 范围为 22-500 nM。Midostaurin 还上调内皮一氧化氮合酶 (eNOS) 基因表达。Midostaurin 显示出强大的抗癌作用。
研究领域:Epigenetics | TGF-beta/Smad | Protein Tyrosine Kinase/RTK | Immunology/Inflammation | Apoptosis
作用靶点:PKC | VEGFR | c-Kit | NO Synthase | Apoptosis
In Vitro: Midostaurin (PKC412) shows a broad antiproliferative activity against various tumor and normal cell lines in vitro, and is able to reverse the Pgp-mediated multidrug resistance of tumor cells in vitro. Exposure of cells to Midostaurin (PKC412) results in a dose-dependent increase in the G2/M phase of the cell cycle concomitant with increased polyploidy, apoptosis and enhanced sensitivity to ionizing radiation.
Midostaurin (PKC412) induces substantial inhibition of KIT-, Lyn-, and STAT5 activity, but does not suppress Btk in HMC-1 cells and primary neoplastic mast cells.
Midostaurin (PKC412) inhibits EN fusion tyrosine kinase in hematopoietic Ba/F3 cells. Midostaurin (PKC412) significantly inhibits EN phosphorylation in M0-91 and IMS-M2 cells in a dose-dependent manner.
In Vivo: Midostaurin (PKC412) strongly inhibits retinal neovascularization as well as laser-induced choroidal neovascularization in murine models.
Midostaurin (PKC412) (25 mg/kg, i.p.) protects mouse livers of the K18 Arg90Cys-overexpressing transgenic mice from Fas-induced apoptosis.
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