生物活性
Abiraterone Acetate (CB 7630) is a highly active and selective 17α-hydroxylase/17,20 lyase (CYP17A1) inhibitor with an IC50 of 72 nM. Abiraterone Acetate (CB 7630) inhibitor CYP11B1, CYP11B2 and CYP3A4 with IC50 of 1.6, 1.8 and 2.7 μM. Abiraterone Acetate (CB 7630) is used in the study of castration-resistant prostate cancer. Abiraterone Acetate (CB 7630) blocks the formation of testosterone by inhibiting CYP17A1. Abiraterone Acetate (CB 7630) caused significant reductions in the weights of the ventral prostate and seminal vesicles. There was no reduction seen in the weight of these organs with KC. Abiraterone Acetate (CB 7630) reduced plasma testosterone to 0.1 nM or less, despite a three- to four-fold increase in the plasma level of luteinizing hormone (LH).
化学数据
| 分子量 | 391.55 |
| 分子式 | C26H33NO2 |
| CAS号 | 154229-18-2 |
| 纯度 | 99.86% |
| 溶解性（25°C） | Ethanol 20 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 | LNCaP and VCaP cells |
| 方法 | Seeding LNCaP and VCaP cells in 96-well plates and growing in CSS-supplemented phenol red-free or FBS-supplemented media for 7 days.Treatig cells with Abiraterone at 24 hours and 96 hours after plating and determining cell viability on day 7 by adding CellTiter Glo and measuring luminescence |
| 浓度 | 0 μM -10 μM |
| 处理时间 | 24 hours and 96 hours |
| 动物实验 |
|---|
| 动物模型 | Male NOD/SCID mice with LAPC4 cells |
| 配制 | 0.1 mL 5% benzyl alcohol and 95% safflower oil solution |
| 剂量 | 0.5 mmol/kg/d |
| 给药处理 | Administered via s.c. |
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 | 2.554 mL | 12.7698 mL | 25.5395 mL |
| 5 mM | 0.5108 mL | 2.554 mL | 5.1079 mL |
| 10 mM | 0.2554 mL | 1.277 mL | 2.554 mL |
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