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- 2025年12月05日
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- 详细信息
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名：
ARN-810; GDC-0810
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1365888-06-7
- 规格：
10 mM * 1 mL/2 mg/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1045.0 |
|---|---|---|---|
| 规格： | 2 mg | 产品价格： | ￥480.0 |
| 规格： | 5 mg | 产品价格： | ￥950.0 |
| 规格： | 10 mg | 产品价格： | ￥1425.0 |
| 规格： | 25 mg | 产品价格： | ￥2600.0 |
| 规格： | 50 mg | 产品价格： | ￥3770.0 |
| 规格： | 100 mg | 产品价格： | ￥5500.0 |
MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。
Brilanestrant
CAS No. : 1365888-06-7
MCE 国际站：Brilanestrant
产品活性：Brilanestrant (ARN-810; GDC-0810) 是一种可口服的，选择性的雌激素降能器 (selective estrogen receptor degrader)，IC50 值为 0.7 nM。
研究领域：Vitamin D Related/Nuclear Receptor
作用靶点：Estrogen Receptor/ERR
In Vitro: Brilanestrant (ARN-810; GDC-0810) is a potent ER-α binder (IC50=6.1 nM), a full transcriptional antagonist with no agonism (3× ERE, IC50=2 nM), and displays good potency and efficacy in ER-α degradation (EC50=0.7 nM) and MCF-7 breast cancer cell viability (IC50=2.5 nM) assays.Brilanestrant (ARN-810; GDC-0810) induces a distinct ERα conformation versus tamoxifen and other ER therapeutics, and does not exhibit tamoxifen-like ER agonism in MCF7 cells.
In Vivo: The pharmacokinetic profile of Brilanestrant (ARN-810) shows it is a olw clearance molecule across species, with good bioavailability (40%-60%). Brilanestrant (ARN-810) (3 mg/kg, p.o.) shows substantial tumor-growth inhibition in a tamoxifen-sensitive MCF-7 xenograft model, while at the highest dose of 100 mg/kg/day, all animals show tumor regression of more than 50% without weight loss.
Brilanestrant (ARN-810) exhibits low clearance (11 mL/min/kg) and 61% oral bioavailability. Brilanestrant (ARN-810) (1-100 mg/kg/day, p.o.) displays dose dependent efficacy in the MCF7 xenograft model.
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