ARV-471 是一种用于乳腺癌的口服雌激素受体 PROTAC 蛋白降解剂。 ARV-471 是一种异双功能分子，可促进雌激素受体 α 和细胞内 E3 连接酶复合物之间的相互作用。 ARV-471 通过蛋白酶体导致雌激素受体的泛素化和随后的降解。 ARV-471 强烈降解 ER 阳性乳腺癌细胞系中的 ER，半最大降解浓度 (DC50) 约为 2 nM。
| Cas No. | 2229711-68-4 |
| 别名 | ARV-471 |
| 分子式 | C45H49N5O4 |
| 分子量 | 723.9 |
| 溶解度 | DMSO : 110 mg/mL (151.95 mM; Need ultrasonic) |
| 储存条件 | Store at -20°C, sealed storage, away from moisture and 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 | ARV-471 is a best-in-class, orally active estrogen receptor (ER) PROTAC degrader. ARV-471 is developed for the research of breast cancer[1]. [1]. John J. Flanagan, et al. ARV-471, an oral estrogen receptor PROTAC™ protein degrader for breast cancer. American Association for Cancer Research.2019. 79 (4): P5-04-18. |
