| Field | Specification |
|---|---|
| Alternative names | (R)-CGP52421 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C35H30N4O5 |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
(R)-3-Hydroxy Midostaurin, also known as (R)-CGP52421, is a potent kinase inhibitor and a major metabolite of midostaurin (PKC412) formed through hepatic CYP3A4 metabolism. It has been studied for its potential relevance to acute myeloid leukemia (AML)[1].
It has the molecular formula C35H30N4O5 and a molecular weight of 586.64 g/mol.
Physical & Chemical Properties
| CAS Number | 155848-20-7 |
|---|---|
| Molecular Formula | C35H30N4O5 |
| Molecular Weight | 586.64 g/mol |
| SMILES | O[C@H]1NC(C2=C1C(C3=C4C=CC=C3)=C5N4[C@]6(O[C@@H](N7C5=C2C8=C7C=CC=C8)C[C@H]([C@H]6OC)N(C(C9=CC=CC=C9)=O)C)C)=O |
| Signaling Pathway | Protein Tyrosine Kinase/RTK; Metabolic Enzyme/Protease |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
(R)-3-Hydroxy Midostaurin ((R)-CGP52421; compound 5) shows IC50 values of 200-400 nM versus the ITD and D835Y mutants, with only low micromolar activity versus the wild-type enzyme[1]. Proliferation is substantially inhibited by the epimeric mixture of metabolites ((R)-3-Hydroxy Midostaurin + (S)-3-Hydroxy Midostaurin) in only the Tel-PDGFRβ line (GI50=63 nM), the KIT D816V line (GI50=320 nM), and the FLT3-ITD line (GI50=650 nM) among the BaF3 cell lines, whereas wild-type cells remain relatively insensitive[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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