生物活性
(R)-Bicalutamide is an active competitive non-steroidal androgen receptor antagonist with an IC50 of 0.17 μM for MDA 453 cells. (R)-Bicalutamide possesses virtually all activities. (R)-Bicalutamide is the leading antiandrogen. (R)-Bicalutamide is used for the treatment of prostate cancer and breast cancer. (R)-Bicalutamide prevents the activation of the androgen receptor and subsequent upregulation of androgen responsive genes by androgenic hormones. In addition, (R)-bicalutamide accelerates the degradation of the androgen receptor.
化学数据
| 分子量 | 430.37 |
| 分子式 | C18H14F4N2O4S |
| CAS号 | 113299-40-4 |
| 纯度 | >98% |
| 溶解性（25°C） | DMSO |
| 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 | C4-2 cell |
| 方法 | Plating exponentially growing C4-2 cells into two 96-well plates and incubating overnight at 37 ?C. One plate is aspirated and stored at -80 ?C and the other treated with 10-fold serial concentrations of ridaforolimus (1000 nM to 0.0001 nM) or vehicle (ethanol) after 24h. Following 72 hours culture at 37 ?C, using the Cy qUANT Cell Proliferation Assay kit the plates to assess simultaneously for cell growth. Bicalutamide and Ridaforolimus combination proliferation assays are performed similarly except cell growth is determined as the change in cell number between vehicle control and compound treated cells after 72 hours in culture. |
| 浓度 | 0-1 μM |
| 处理时间 | 72 hours |
| 动物实验 |
|---|
| 动物模型 | Male nude mice bearing C4-2 cells |
| 配制 | 4% ethanol, 5% Tween 80, and 5% propylene glycol |
| 剂量 | 10 mg/kg |
| 给药处理 | Administered via p.o. |
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 | 2.3236 mL | 11.6179 mL | 23.2358 mL |
| 5 mM | 0.4647 mL | 2.3236 mL | 4.6472 mL |
| 10 mM | 0.2324 mL | 1.1618 mL | 2.3236 mL |
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