Brilanestrant
产品说明书
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同义名 : | GDC-0810; ARN-810; RG-6046 |
| CAS号 : | 1365888-06-7 | |
| 货号 : | A897745 | |
| 分子式 : | C26H20ClFN2O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 446.9 | |
| MDL号 : | MFCD28902190 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Estrogen is essential for growth and development of the mammary glands and has been associated with the promotion and growth of breast cancer. Estrogen exerts many of its effects via two nuclear estrogen receptors (ERs), ERα and ERβ[3]. GDC-0810 is an orally bioavailable SERD (selective estrogen receptor degrader) which is a potent antagonist and degrader of both Erα and Erβ with IC50 values of 6.1 nM and 8.8 nM, respectively. And the EC50 value for Erα of GDC-0810 is 0.7 nM[2]. In MCF7 cells GDC-0810 effectively antagonized E2-mediated transcriptional activation of an ER reporter construct and inhibited cell proliferation with nanomolar potency. In mice, GDC-0810 exhibited low clearance (11 mL/min/kg) and 61% oral bioavailability. In the MCF7 xenograft model, GDC-0810 displayed dose dependent efficacy. The 100 mg/kg/day dose caused tumor regressions similar to withdrawal of estrogen pellets at the start of dosing[1]. In a tamoxifen-sensitive MCF-7 xenograft model, GDC-0810 (3 mg/kg, p.o.) showed substantial tumor-growth inhibition, while all animals showed tumor regression of more than 50% without weight loss at the highest dose of 100 mg/kg/day[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.24mL 0.45mL 0.22mL |
11.19mL 2.24mL 1.12mL |
22.38mL 4.48mL 2.24mL |
| 参考文献 |
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