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- 详细信息
- 技术资料
- 保存条件:
-20°C, sealed storage, away from moisture and light
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
2505067-70-7
- 规格:
1 mg
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Bexirestrant
CAS No. : 2505067-70-7
MCE 国际站:Bexirestrant
产品活性:Bexirestrant 是一种具有口服活性的 ER-α 降解剂。Bexirestrant 可用于抗雌激素、抗肿瘤的研究。
研究领域:Vitamin D Related/Nuclear Receptor
作用靶点:Estrogen Receptor/ERR
In Vitro: Bexirestrant (compound Formula Ia) inhibits the growth of wild type (WT), Y537S and D538G mutated MCF-7 cells with IC50s of 0.3. 6.0, 2.2 nM, respectively.
Bexirestrant induces the ER-α degradation in WT, Y537S and D538G mutated MCF-7 cells with IC50s of 0.3. 19.6, 12.7 nM, respectively.
Bexirestrant shows 16.3% ER-α remaining in WT MCF-7 cells at concentration of 1 nM.
In Vivo: Bexirestrant (50mg/kg; p.o.; 28 days) shows a good efficacy in an MCF-Y537S xenograft.Pharmacokinetic parameters in rat at 50 mg/kg p.o. dose:
| Tmax (h) | Cmax (ng/mL) | AUClast (hr× ng/mL) | AUCinf_obs (hr×ng/mL) | T1/2 (h) |
| 4.00 | 343 | 7582 | 9804 | 26 |
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