生物活性
Veliparib (ABT-888)是一种有效的PARP1和PARP2抑制剂，Ki分别为5.2 nM和2.9 nM，抑制SIRT2。ABT-888有效抑制PARP，作用于PARP-1和PARP-2时Ki值分别为5.2和2.9 nM。ABT-888降低肺癌H460细胞中克隆基因的存活率，且抑制DNA修复。ABT-888抑制C41细胞，EC50为2 nM。
化学数据
| 分子量 | 244.29 |
| 分子式 | C13H16N4O |
| CAS号 | 912444-00-9 |
| 纯度 | 99.76% |
| 溶解性（25°C） | DMSO ≥45 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 | C41 cells |
| 方法 | Cellular PARP Assay. C41 cells were treated with test compound for 30 min in a 96-well plate. PARP was activated by damaging DNA with 1 mM H2O2 for 10 min. Cells were washed with ice-cold PBS once and fixed with prechilled methanol/acetone (7:3) at -20 °C for 10 min. After air-drying, plates were rehydrated with PBS and blocked using 5% nonfat dry milk in PBS-tween (0.05%) (blocking solution) for 30 min at room temperature. Cells were incubated with anti-PAR antibody 10H (1:50) in blocking solution at room temperature for 60 min followed by washing with PBS-Tween20 5 times and incubation with goat antimouse fluorescein 5(6)-isothiocyanate (FITC)-coupled antibody (1:50) and 1 μg/mL 4′,6-diamidino-2-phenylindole (DAPI) in blocking solution at room temperature for 60 min. After washing with PBS-Tween20 5 times, analysis was performed using an fmax Fluorescence Microplate Reader set at the excitation and emission wavelength for FITC or the excitation and emission wavelength for DAPI. PARP activity (FITC signal) was normalized with cell numbers (DAPI). |
| 浓度 | 0~1uM |
| 处理时间 | 30 min |
| 动物实验 |
|---|
| 动物模型 | MX-1 Tumor Model |
| 配制 | 2.5% EtOH, 1 drop TW-80, 25% PEG400, PBS |
| 剂量 | 12.5mg/kg, BID, P6-11 |
| 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 | 4.0935 mL | 20.4675 mL | 40.935 mL |
| 5 mM | 0.8187 mL | 4.0935 mL | 8.187 mL |
| 10 mM | 0.4093 mL | 2.0467 mL | 4.0935 mL |
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