155848-20-7
中文名稱
3 Hydroxy Midostaurin Epimer 2 (CGP52421 Epimer 2)
英文名稱
3 Hydroxy Midostaurin Epimer 2 (CGP52421 Epimer 2)
CAS
155848-20-7
分子式
C35H30N4O5
分子量
586.65
MOL 文件
155848-20-7.mol
155848-20-7 結(jié)構(gòu)式
基本信息
中文別名
N-[(3R,9S,10R,11R,13R)-2,3,10,11,12,13-六氫-3-羥基-10-甲氧基-9-甲基-1-氧代-9,13-環(huán)氧-1H,9H-二吲哚[1,2,3-GH:3′,2′,1′-LM]吡咯并[3,4-J][1,7]苯并二氮雜壬環(huán)-11-基]-N-甲基苯甲酰胺 英文別名
(R)-CGP52421Midostaurin Impurity 2
Midostaurin Impurity 4
(R)-3-Hydroxy Midostaurin
3 Hydroxy Midostaurin Epimer 2 (CGP52421 Epimer 2)
Benzamide, N-[(3R,9S,10R,11R,13R)-2,3,10,11,12,13-hexahydro-3-hydroxy-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl]-N-methyl-
常見問題列表
生物活性
(R)-3-Hydroxy Midostaurin ((R)-CGP52421) 是有效的激酶抑制劑。(R)-3-Hydroxy Midostaurin 是 Midostaurin (PKC412; HY-10230) 通過肝 CYP3A4 酶代謝的主要代謝產(chǎn)物。(R)-3-Hydroxy Midostaurin 具有潛在的用于急性髓細(xì)胞性白血病 (AML) 的潛力。體外研究
(R)-3-Hydroxy Midostaurin ((R)-CGP52421; compound 5) has IC
50
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 (GI
50
=63 nM), KIT D816V (GI
50
=320 nM), and FLT3-ITD (GI
50
=650 nM) BaF3 cell lines, while the wild-type cells are relatively insensitive.