生物活性
IC-87114是一种选择性的PI3Kδ抑制剂，IC50为0.5 μM，作用于PI3Kδ比作用于PI3Kγ和PI3Kα/β选择性分别高58和100倍。IC87114是PI3Kδ的有效选择性抑制剂。IC87114作用于PI3Kδ，IC50为0.5 μM，且与作用于其他PI3K亚型相比，选择性高50倍,甚至更高。根据IC87114处理的细胞类型，PI3Kδ作用于TNFα诱导的信号中，降低Akt磷酸化和PDK1酶活。
化学数据
| 分子量 | 397.43 |
| 分子式 | C22H19N7O |
| CAS号 | 371242-69-2 |
| 纯度 | 99.37% |
| 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 | human neutrophil |
| 方法 | Measurement of neutrophil adhesion and migration
The adhesion assays were performed by the following modifications of the procedure described by Sadhu et al. Briefly, 96-well plates were coated overnight with 5 μg/ml ICAM-1/Ig, blocked with 1% HSA (no. 12666; Calbiochem, La Jolla, CA) in RPMI 1640, and 2 × 105neutrophils (untreated or pretreated with the indicated concentration of IC87114) were added in triplicate wells. After incubation at 37°C for the desired time, 5% CO2 glutaraldehyde was added to a 1% final concentration. Unbound cells were removed by washing the wells in water and the adherent cells were stained with crystal violet. Cell adhesion was quantified by reading the intensity of crystal violet on Spectra MAX (Molecular Devices, Sunnyvale, CA) at 570 nm. |
| 浓度 | 1 μ M |
| 处理时间 | 3 h |
| 动物实验 |
|---|
| 动物模型 | WT B6 and p110δD910A Mice |
| 配制 | 1% methylcellulose (MCL) |
| 剂量 | 30 mg/kg once |
| 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 | 2.5162 mL | 12.5808 mL | 25.1617 mL |
| 5 mM | 0.5032 mL | 2.5162 mL | 5.0323 mL |
| 10 mM | 0.2516 mL | 1.2581 mL | 2.5162 mL |
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