产品说明书
ARV-471
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同义名 : | Vepdegestrant |
| CAS号 : | 2229711-68-4 | |
| 货号 : | A1467731 | |
| 分子式 : | C45H49N5O4 | |
| 纯度 : | 99% +, 99.99% ee | |
| 分子量 : | 723.9 | |
| MDL号 : | MFCD34184413 | |
| 存储条件： |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(145.05 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Vepdegestrant (ARV-471) serves as an orally active PROTAC estrogen receptor degrader designed for breast cancer treatment. It facilitates interactions between estrogen receptor alpha and an intracellular E3 ligase complex, leading to ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant effectively degrades ER in ER-positive breast cancer cell lines, with a half-maximal degradation concentration (DC50) of approximately 2 nM [1]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.38mL 0.28mL 0.14mL |
6.91mL 1.38mL 0.69mL |
13.81mL 2.76mL 1.38mL |
| 参考文献 |
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