(S)-3-Hydroxy Midostaurin(Synonyms: (S)-CGP52421)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

(S)-3-Hydroxy Midostaurin (Synonyms: (S)-CGP52421)

(S)-3-Hydroxy Midostaurin ((S)-CGP52421) 是一种有效的激酶抑制剂，对 VEGFR-2，TRK-A，FLT3 等 13 种激酶的 IC50 值为 <400 nM。(S)-3-Hydroxy Midostaurin 是 Midostaurin (PKC412; HY-10230) 通过肝 CYP3A4 酶代谢的次要代谢产物。(S)-3-Hydroxy Midostaurin 具有潜在的用于急性髓细胞性白血病 (AML) 的潜力。

(S)-3-Hydroxy Midostaurin(Synonyms: (S)-CGP52421)

(S)-3-Hydroxy Midostaurin Chemical Structure

CAS No. : 945260-14-0

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生物活性

(S)-3-Hydroxy Midostaurin ((S)-CGP52421) is a potent kinases inhibitor with IC50 values of <400 nm for 13 kinases (vegfr-2, trk-a, flt3, et). (s)-3-hydroxy midostaurin is a minor metabolite of (pkc412; hy-10230) undergoing by the hepatic cyp3a4 enzyme. has potential acute myeloid leukemia (aml)[1].

体外研究
(In Vitro)

(S)-3-Hydroxy Midostaurin ((S)-CGP52421; compound 4) 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[1].
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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

586.64

Formula

C35H30N4O5
CAS 号

945260-14-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Manley PW, et al. Comparison of the Kinase Profile of Midostaurin (Rydapt) with That of Its PredominantMetabolites and the Potential Relevance of Some Newly Identified Targets to Leukemia Therapy. Biochemistry. 2018 Sep 25;57(38):5576-5590.

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