945260-14-0
中文名稱
3 Hydroxy Midostaurin Epimer 1 (CGP52421 Epimer 1)
CAS
945260-14-0
分子式
C35H30N4O5
基本信息
英文別名
(S)-CGP52421Midostaurin Impurity 3
Midostaurin Impurity 1
(S)-3-Hydroxy Midostaurin
3 Hydroxy Midostaurin Epimer 1 (CGP52421 Epimer 1)
Benzamide, N-[(3S,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
(S)-3-Hydroxy Midostaurin ((S)-CGP52421) 是一種有效的激酶抑制劑，對 VEGFR-2，TRK-A，F(xiàn)LT3 等 13 種激酶的 IC50 值為 <400 nM。(S)-3-Hydroxy Midostaurin 是 Midostaurin (PKC412; HY-10230) 通過肝 CYP3A4 酶代謝的次要代謝產(chǎn)物。(S)-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
(S)-3-Hydroxy Midostaurin ((S)-CGP52421; compound 4) 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.