生物活性
A66是一种有效的,特异性的p110α抑制剂,IC50为32 nM,作用于p110α比作用于其他I型PI3K亚型选择性高100倍以上。
化学数据
分子量 | 393.53 |
分子式 | C17H23N5O2S2 |
CAS号 | 1166227-08-2 |
纯度 | 99.92% |
溶解性(25°C) | DMSO 50 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 | CD4+ T lymphocytes |
方法 | T lymphocyte isolation and activation To obtain naive CD4+ T lymphocytes (CD4+CD62L+ T cells), spleens were passed through a 70 lm mesh. After centrifugation, red blood cells were lysed and the cells washed in culture medium (Click’s medium supplemented with 10% heat inactivated FCS). Then, naive CD4+ T cells were isolated using Miltenyi CD4+CD62L+ T cell isolation kit II for mouse cells (Ref. 130-093-227, Miltenyi Biotec, Bergisch Gladbach, Germany) according to the manufacturers’ instructions. The isolated cells were routinely >97% CD4+, >95% CD62L+. Cells (106) were cultured in 1 ml culture medium in 24- well culture plates (Costar) pre-coated with anti-CD3 antibody (YCD3-1, 5 lg ml 1). Where indicated, anti-CD28 (H57, 2.5 lg ml 1, eBioscience, San Diego, California), DMSO or inhibitors dissolved in DMSO (1 ll per culture) were added. At 24 h, the cultures were resuspended, centrifuged and the supernatants assayed for cytokine content. |
浓度 | 0~10 μ M |
处理时间 | 24 h |
动物实验 |
---|
动物模型 | mice bearing SK-OV-3, HCT-116 and U87MG xenograft models |
配制 | 20% 2-hydroxypropyl-β-cyclodextrin (Sigma–Aldrich) in water |
剂量 | 10 ml/kg once daily (QD) or twice daily (BID) daily for 21 days or twice daily for 16 days (SK-OV-3), daily for 14 days (U87MG) and daily for 7 days (HCT-116) |
给药处理 | intraperitoneal injection |
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 | 2.5411 mL | 12.7055 mL | 25.411 mL |
5 mM | 0.5082 mL | 2.5411 mL | 5.0822 mL |
10 mM | 0.2541 mL | 1.2706 mL | 2.5411 mL |