(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].

(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].

586.64

C₃₅H₃₀N₄O₅

945260-14-0

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