Cyclopamine是一种特异性的Hedgehog (Hh)信号通路拮抗剂,作用于Smoothened (Smo),IC50为46 nM。
Cyclopamine is a naturally occurring Hedgehog (Hh)‑specific small‑molecule signaling steroidal alkaloid inhibitor, causes a profound inhibition of tumor growth, has significant anti‑invasive, anti‑proliferative and anti‑estrogenic potency in human breast cancer cells [2] [1]. The EC50 of cyclopamine is 10.57 μM, it was identified by an FXR-bla (farnesoid X receptor- b-lactamase) assay.
3 μM
50 mg/kg/day 皮下注射处理
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,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Peukert S, et al. Bioorg Med Chem Lett, 2009, 19(2), 328-331.
[2] Berman, David M., et al., 2002. Medulloblastoma growth inhibition by hedgehog pathway blockade. Science (New York, N.Y.). 297(5586): 1559-61.
[3] Chen, James K., et al., 2002. Small molecule modulation of Smoothened activity. Proceedings of the National Academy of Sciences of the United States of America. 99(22): 14071-6.
分子式 C27H41NO2 |
分子量 411.62 |
CAS号 4449-51-8 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 4 mg/mL |
Water |
Ethanol 5 mg/mL |
体内溶解度
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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