(R)-3-Hydroxy Midostaurin ((R)-CGP52421) is a potent kinases inhibitor. (R)-3-Hydroxy Midostaurin is a major metabolite of midostaurin (PKC412; HY-10230) undergoing by the hepatic CYP3A4 enzyme. (R)-3-Hydroxy Midostaurin has the potential for acute myeloid leukemia (AML)^[1].

(R)-3-Hydroxy Midostaurin ((R)-CGP52421; compound 5) 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

155848-20-7

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.