Midostaurin | MedChemExpress (MCE)-产品咨询-资讯-生物在线

Midostaurin | MedChemExpress (MCE)

作者:MedChemExpress LLC 暂无发布时间 (访问量:177)

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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/γSykFlk-1AktPKAc-Kitc-Fgrc-SrcFLT3PDFRβVEGFR1/2IC50 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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