生物活性
Enzastaurin (LY317615)是一种有效的PKCβ选择性抑制剂,IC50为6 nM,比对PKCα, PKCγ和PKCε的作用强6到20倍。Enzastaurin阻断U87MG恶性胶质瘤细胞,PC-3前列腺癌细胞 ,及HCT116结肠癌细胞的增殖。当Enzastaurin浓度低于1 μM时则可能对HCT116和U87MG细胞有温和的诱导。Enzastaurin阻断许多细胞系如K-562, MOLT-4, HOP-92, 和PC-3细胞系的增殖。
化学数据
分子量 | 515.61 |
分子式 | C32H29N5O2 |
CAS号 | 170364-57-5 |
纯度 | >99% |
溶解性(25°C) | DMSO 20 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 |
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细胞系 | PC-3 prostate cancer, HCT116 colon cancer, and U87MG glioblastoma cell lines |
方法 | Proliferation assays. Proliferation was assessed for all cell lines over a 6-day time course in media supplemented with 1% FBS (7 days total). Briefly, 1,000 cells were plated per well in a 96-well plate and changed to fresh media (1% FBS) with or without enzastaurin on days 1 and 4. On day 7, the media were removed and 100 μL propidium iodide (PI) solution (10 μg/mL in D-PBS) were added to each well. An initial reading for PI staining (excitation at 500 nmol/L, absorbance at 615 nmol/L) was done using the WallacVictor plate reader following a 30-minute incubation to determine the nonviable cell fraction. The plate was then frozen at –80 °C for 2 hours, thawed, and reread. The proliferative index was scored by subtracting the prefreeze data (nonviable cells) from the postfreeze data (all cells). |
浓度 | 0~10μM |
处理时间 | 6 days |
动物实验 |
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动物模型 | Athymic nude mice bearing HCT116 colon cancer xenografts |
配制 | 10% acacia (Fisher Scientific, Fair Lawn, NJ) in water |
剂量 | twice daily at 75 mg/kg |
给药处理 | gavage |
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 |
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1 mM | 1.9395 mL | 9.6973 mL | 19.3945 mL |
5 mM | 0.3879 mL | 1.9395 mL | 3.8789 mL |
10 mM | 0.1939 mL | 0.9697 mL | 1.9395 mL |