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ChemicalBook--->CAS DataBase List--->179237-49-1

179237-49-1

179237-49-1 Structure

179237-49-1 Structure
IdentificationBack 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
Chemical PropertiesBack Directory
[density ]

1.53±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

Soluble in DMSO
[form ]

Solid
[pka]

12.23±0.70(Predicted)
[color ]

Light yellow to yellow
Hazard InformationBack 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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