Orteronel (TAK-700) is an inhibitor of the steroidogenic enzyme CYP17A1. It has higher specificity for the 17,20 lyase activity of CYP17A1 with IC50 of 38 nM. Phase III.
Orteronel (TAK-700) is a novel hormonal therapy that is currently in testing for the treatment of prostate cancer. Orteronel inhibits the 17,20 lyase activity of the enzyme CYP17A1, which is important for androgen synthesis in the testes, adrenal glands and prostate cancer cells.
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] Kazuhiro Suzuki,et al. A phase 1 multiple-dose study of orteronel in Japanese patients with castration-resistant prostate cancer. Cancer Chemother Pharmacol. 2015; 75: 373–380. Published online 2014 Dec 24. doi: 10.1007/s00280-014-2654-y.
分子式 C18H17N3O2 |
分子量 307.35 |
CAS号 566939-85-3 |
储存方式 -20 ℃长期冷藏储存。冰袋运输 |
溶剂(常温) |
DMSO 10 mM |
Water <1 mg/mL |
Ethanol <1 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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