CGP52421
CGP52421 Basic information
- Product Name:
- CGP52421
- Synonyms:
-
- CGP52421
- 3-Hydroxy Midostaurin (CGP 52421)
- 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-
- Midostaurin Impurity 1 (3-Hydroxy Midostaurin)
- 3-Hydroxy Midostaurin D5Q: What is 3-Hydroxy Midostaurin D5 Q: What is the CAS Number of 3-Hydroxy Midostaurin D5
- Midostaurin metabolite - CGP52421
- N-[(9S,10R,11R,13R)-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 benzamide
- CAS:
- 179237-49-1
- MF:
- C35H30N4O5
- MW:
- 586.65
- Mol File:
- 179237-49-1.mol
CGP52421 Chemical Properties
- Density
- 1.53±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- pka
- 12.23±0.70(Predicted)
CGP52421 Usage And Synthesis
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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