生物活性
Apalutamide (ARN-509)是一种具有潜在抗肿瘤活性的雄激素受体拮抗剂，IC50 为 16 nM。ARN-509与靶组织中的AR结合，从而阻止了雄激素诱导的受体激活，并促进了无法转运至细胞核的无活性复合物的形成。这防止了AR应答基因的结合和转录。
靶点信息
| Androgen Receptor (Cell-free assay) | GABAA receptor (Cell-free assay) | | | |
| 16 nM | 3 μM | | | |
化学数据
| 目录号 | A11923 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 477.4 |
| Formula | C21H15F4N5O2S |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 956104-40-8 |
| Synonyms | ARN509 |
| SMILES | CNC(=O)C1=C(C=C(C=C1)N2C(=S)N(C(=O)C23CCC3)C4=CN=C(C(=C4)C(F)(F)F)C#N)F |
溶解度
| In vitro (25°C) | DMSO | 18 mg/mL (37.7 mM) |
| Water | Insoluble |
| Ethanol | 5 mg/mL (10.47 mM) |
| In vivo | 2% DMSO+40% PEG 300+2% Tween 80+ddH2O | 2 mg/mL |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 20.95 mL | 104.73 mL | 209.47 mL |
| 0.5 mM | 4.19 mL | 20.95 mL | 41.89 mL |
| 1 mM | 2.09 mL | 10.47 mL | 20.95 mL |
| 5 mM | 0.42 mL | 2.09 mL | 4.19 mL |
*The above data is based on the productmolecular weight 477.4 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
m.cnreagent.com