1. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease
  2. FLT3 Drug Metabolite
  3. (S)-3-Hydroxy Midostaurin

(S)-3-Hydroxy Midostaurin  (Synonyms: (S)-CGP52421)

Cat. No.: HY-108263A
Handling Instructions

(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).

For research use only. We do not sell to patients.

(S)-3-Hydroxy Midostaurin Chemical Structure

(S)-3-Hydroxy Midostaurin Chemical Structure

CAS No. : 945260-14-0

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Description

(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].

In Vitro

(S)-3-Hydroxy Midostaurin ((S)-CGP52421; compound 4) 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

586.64

Formula

C35H30N4O5

CAS No.
SMILES

O[C@@H]1NC(C2=C1C(C3=C4C=CC=C3)=C5N4[C@]6(C)[C@@H]([C@@H](C[C@](O6)([H])N7C5=C2C8=C7C=CC=C8)N(C(C9=CC=CC=C9)=O)C)OC)=O

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Storage

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

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(S)-3-Hydroxy Midostaurin Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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(S)-3-Hydroxy Midostaurin
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