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(S)-3-Hydroxy Midostaurin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(S)-3-Hydroxy Midostaurin图片
CAS NO:945260-14-0
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
(S)-CGP52421
产品介绍
(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。
生物活性

(S)-3-Hydroxy Midostaurin ((S)-CGP52421) is a potent kinases inhibitor withIC50values of<400 nm for 13 kinases (vegfr-2, trk-a,FLT3, et). (S)-3-Hydroxy Midostaurin is a minor metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (S)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML)[1].

体外研究
(In Vitro)

(S)-3-Hydroxy Midostaurin ((S)-CGP52421; compound 4) has IC50values 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].

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.