| Identification | Back Directory | [Name]
CGP52421 | [CAS]
179237-49-1 | [Synonyms]
CGP52421
3-Hydroxy Midostaurin
3-Hydroxy Midostaurin (CGP 52421)
Midostaurin Impurity 1 (3-Hydroxy Midostaurin)
Benzamide, N-(2,3,10,11,12,13-hexahydro-3-hydroxy-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl)-N-methyl- | [Molecular Formula]
C35H30N4O5 | [MOL File]
179237-49-1.mol | [Molecular Weight]
586.65 |
| Hazard Information | Back Directory | [Uses]
3-Hydroxy Midostaurin-d5 is the deuterium labelled 3-Hydroxy Midostaurin (H939985(M)). 3-Hydroxy Midostaurin is a metabolite of Midostaurin (M343760), a compound shown to possess antiproliferative characteristics via inhibition of protein kinase C, kinase insert domain receptor, and c-kit. | [Biological Activity]
3-Hydroxy Midostaurin (CGP 52421), a metabolite of PKC412, potently inhibits FMS-like tyrosine kinase 3 (FLT3) autophosphorylation with IC50s of 132 nM and 9.8 μM in culture medium and plasma, respectively. Compared to PKC412, 3-Hydroxy Midostaurin is less selective but more cytotoxic. | [in vitro]
CGP52421 (200, 400, 600, 800, 1000 nM) is more cytotoxic than PKC412 over the dose range 100 to 500 nM. | [target]
IC50: 132 nM (FLT3 in culture medium) and 9.8 μM (FLT3 in plasma) |
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