生物活性
Fulvestrant是一种Estrogen receptor（ER）（雌激素受体）拮抗剂， IC50为0.094 nM。Fulvestrant 有效抑制ER阳性的MCF-7生长(IC50为 0.29 nM)，而对ER阴性的的 BT-20人类乳腺癌细胞的生长没有作用效果。Fulvestrant 使细胞在 G0/G1 期累积，也降低了能持续进行DNA合成的细胞比例。 Fulvestrant 竞争性地抑制雌二醇与雌激素受体结合。
化学数据
| 分子量 | 606.77 |
| 分子式 | C32H47F5O3S |
| CAS号 | 129453-61-8 |
| 纯度 | 100.00% |
| 溶解性（25°C） | DMSO 50 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | MCF-7 |
| 方法 | MCF-7 cells were plated at 10 000 cells/well in 96-well culture plates in MEM with 10% fetal bovine serum, and they were allowed to adhere for 48 h. Thereafter, the cultures were washed with serum-free MEM and incubated in 100 μl serum-free MEM. After 72 h, the medium was removed and replaced with 2% charcoal-stripped FBS–MEM containing 10 pmol/l E2 with either RAD1901 or additional E2 at concentrations ranging from 10–15 to 10–6 mol/l. The medium was removed after 48 h of incubation and the cells were lysed by adding 100 μl of CellTiter Glo (Promega, Madison, Wisconsin, USA), diluted 1 : 1 in water, per well. The plates were gently mixed on a plate shaker for 10 min before the luminescent signal was measured on a luminometer. The EC50 and IC50 of the test compound were defined as the concentrations that resulted in half-maximum shift. |
| 浓度 | Ranging from 10–15 to 10–6 mol/l |
| 处理时间 | 48 h |
| 动物实验 |
|---|
| 动物模型 | MCF-7 xenograft models: Female athymic nude mice [Crl:NU(NCr)-Foxn1nu] |
| 配制 | Formulated for use as a homogenous suspension in 0.5% (w/v) methylcellulose in deionized water |
| 剂量 | 0.5 mg/animal daily |
| 给药处理 | subcutaneous injection |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6481 mL | 8.2404 mL | 16.4807 mL |
| 5 mM | 0.3296 mL | 1.6481 mL | 3.2961 mL |
| 10 mM | 0.1648 mL | 0.824 mL | 1.6481 mL |
