(R)-3-Hydroxy Midostaurin,1558

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(R)-3-Hydroxy Midostaurin

CAS No. : 155848-20-7

MCE 国际站：(R)-3-Hydroxy Midostaurin

产品活性：(R)-3-Hydroxy Midostaurin ((R)-CGP52421) 是有效的激酶抑制剂。(R)-3-Hydroxy Midostaurin 是 Midostaurin (PKC412; HY-10230) 通过肝 CYP3A4 酶代谢的主要代谢产物。(R)-3-Hydroxy Midostaurin 具有潜在的用于急性髓细胞性白血病 (AML) 的潜力。

研究领域：Protein Tyrosine Kinase/RTK  |  Metabolic Enzyme/Protease

作用靶点：FLT3  |  Drug Metabolite

In Vitro: (R)-3-Hydroxy Midostaurin ((R)-CGP52421; compound 5) has IC₅₀ values in the range of 200-400 nM against the ITD and D835Y mutants and low micromolar activity against the wild-type enzyme.
The epimeric mixture of metabolites ((R)-3-Hydroxy Midostaurin + (S)-3-Hydroxy Midostaurin) substantially inhibits the proliferation of only the Tel-PDGFRβ (GI₅₀=63 nM), KIT D816V (GI₅₀=320 nM), and FLT3-ITD (GI₅₀=650 nM) BaF3 cell lines, while the wild-type cells are relatively insensitive.

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