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Catalog Number | orb1693535 |
---|---|
Category | Small Molecules |
Description | Sorafenib N-oxide |
CAS Number | 583840-03-3 |
Purity | 98% |
MW | 480.83 |
SMILES | CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)cc2)ccn1=O |
Formula | C21H16ClF3N4O4 |
Biological Activity | Sorafenib N-oxide is an active metabolite of sorafenib , an inhibitor of Raf-1, B-RAF, and receptor tyrosine kinases. Sorafenib N-oxide inhibits FLT3 that contains the internal tandem duplication mutation (FLT3-ITD; Kd = 70 nM) and inhibits proliferation of MV4-11 acute myeloid leukemia (AML) cells expressing FLT3-ITD (IC50 = 25.8 nM). It is selective for AML cell lines containing FLT3-ITD over lines containing wild-type FLT3 (IC50s = 3.9-13.3 μM). Sorafenib N-oxide is also a linear-mixed inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 (Ki = 15 μM in human liver microsomes). |
Storage | -20°C |
Note | For research use only |
Expiration Date | 12 months from date of receipt. |