Sorafenib N-oxide is an active metabolite of sorafenib, an inhibitor of Raf-1, B-RAF, and receptor tyrosine kinases.
Cas No. | 583840-03-3 |
别名 | 索拉非尼N氧化物 |
Canonical SMILES | ClC1=C(C(F)(F)F)C=C(NC(NC2=CC=C(OC(C=C3C(NC)=O)=CC=[N]3=O)C=C2)=O)C=C1 |
分子式 | C21H16ClF3N4O4 |
分子量 | 480.8 |
溶解度 | DMSO: soluble,Methanol: very slightly soluble, heated |
储存条件 | Store at -20°C, protect from light |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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). |