生物活性
AS-605240选择性抑制PI3Kγ，IC50为8 nM，作用于PI3Kγ比作用于PI3Kδ/β和PI3Kα选择性分别高30和7.5倍以上。AS-605240抑制PI3Kγ，IC50为8 nM。AS-605240是PI3Kγ的ATP竞争性抑制剂，Ki值为7.8 nM。AS-605240也抑制PI3Kα,β,和δ,IC50分别为60,270, 和300 nM。
化学数据
| 分子量 | 257.27 |
| 分子式 | C12H7N3O2S |
| CAS号 | 648450-29-7 |
| 纯度 | >99% |
| 溶解性（25°C） | DMSO 4 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 | Jurkat cells |
| 方法 | Cell lines culture and survival assays.
Cell lines were cultured in RPMI-1640 medium, 10% fetal bovine serum (FBS), and penicillin/streptomycin at 37°C and 5% CO2. Medium was changed 12–24 h before all experiments. To measure IC50 values, cells (2–6 × 104) were incubated for 96 h with increasing concentrations of AS605240, prednisolone, L-asparaginase, MTX or DNR. To measure Combination Index (CI) values between AS605240 and the other drugs, 2-fold ratios of the calculated IC50 values (0.25×, 0.5×, 1×, 2× or 4×) of each drug were used either in combination or as single drugs. Cells were treated for a total of 96 h. When drug scheduling was applied, one of the drugs was added 48 h after the start of the experiment. Cell viability was measured by the MTT assay. IC50 and CI values were calculated with the GraphPad Prism 5 (GraphPad Software, La Jolla, CA, USA) and Calcusyn (Biosoft, Cambridge, UK) [65] softwares, respectively. |
| 浓度 | 0.1~100 μM |
| 处理时间 | 24 h |
| 动物实验 |
|---|
| 动物模型 | mouse CIA |
| 配制 | 0.5% carboxymethylcellulose /0.25% Tween- 20 (Sigma) |
| 剂量 | 50mg/kg twice a day for 7 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 | 3.887 mL | 19.4348 mL | 38.8697 mL |
| 5 mM | 0.7774 mL | 3.887 mL | 7.7739 mL |
| 10 mM | 0.3887 mL | 1.9435 mL | 3.887 mL |
