3 Hydroxy Midostaurin Epimer 1 (CGP52421 Epimer 1)

(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 midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (S)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML)[1].

[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. DOI:10.1021/acs.biochem.8b00727