生物活性
Olaparib (AZD2281, Ku-0059436)是一种选择性的PARP1/2抑制剂，IC50为5 nM/1 nM，比对Tankyrase-1的作用强300倍。Olaparib是PARP抑制剂，也作用于BRCA1或BRCA2突变。Olaparib对端锚(聚合)酶-1作用效果不大，IC50值大于。Olaparib浓度为30-100 nM作用于SW620细胞，使PARP-1失活。
化学数据
| 分子量 | 434.46 |
| 分子式 | C24H23FN4O3 |
| CAS号 | 763113-22-0 |
| 纯度 | 99.86% |
| 溶解性（25°C） | DMSO 80 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 | SW620 colorectal cell line |
| 方法 | Potentiation of MMS Cytotoxicity by 47 Determined by the Use of Sulforhodamine B Cell Growth Assays. SW620 cells were seeded in 96-well plates and were left to attach overnight. Cells were preincubated with vehicle control (DMSO) or with a single concentration of KU-0059436 (1, 3, 10, 30, 100 or 300 nM) for 1 h before the addition of increasing concentrations of MMS. Cells were incubated in the presence of each drug combination for 4 days before cell growth was quantified by the use of an SRB assay.44 Data were calculated from triplicate wells as the mean percentage of cell growth relative to KU-0059436-only wells, and (SE and IC50 were calculated by the use of XL-FIT 4 software. SW620 cells showed<24% growth inhibition (>76% cell growth)
when only KU-0059436 was used at concentrations below 300 nM (data not shown). |
| 浓度 | 1, 3, 10, 100 and 300 nM |
| 处理时间 | 4 days |
| 动物实验 |
|---|
| 动物模型 | mouse bearing SW620 xenografted tumors |
| 配制 | methylcellulose/PBS |
| 剂量 | 10 mg/kg once daily for 5 consecutive days |
| 给药处理 | orally |
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 | 2.3017 mL | 11.5085 mL | 23.0171 mL |
| 5 mM | 0.4603 mL | 2.3017 mL | 4.6034 mL |
| 10 mM | 0.2302 mL | 1.1509 mL | 2.3017 mL |
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