(R)-3-Hydroxy Midostaurin

Modify Date: 2024-01-15 02:45:58

(R)-3-Hydroxy Midostaurin Structure
(R)-3-Hydroxy Midostaurin structure
Common Name (R)-3-Hydroxy Midostaurin
CAS Number 155848-20-7 Molecular Weight 586.64
Density N/A Boiling Point N/A
Molecular Formula C35H30N4O5 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of (R)-3-Hydroxy Midostaurin


(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].

 Names

Name (R)-3-Hydroxy Midostaurin

 (R)-3-Hydroxy Midostaurin Biological Activity

Description (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].
Related Catalog
In Vitro (R)-3-Hydroxy Midostaurin ((R)-CGP52421; compound 5) has IC50 values 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].
References

[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.

 Chemical & Physical Properties

Molecular Formula C35H30N4O5
Molecular Weight 586.64