6H-Pyrido[4,3-b]carbazolium,2-[2-(diethylamino)ethyl]-9-hydroxy-5,11-dimethyl-, chloride (1:1);2-[2-(diethylamino)ethyl]-5,11-dimethyl-6H-pyrido[4,3-b]carbazol-2-ium-9-ol,chloride;Datelliptium;Datelliptium chloride;2-(2-(Diethylamino)ethyl)-9-hydroxy-5,11-dimethyl-6H-pyrido(4,3-b)carbazolium chloride;2-[2-(diethylamino)ethyl]-9-hydroxy-5,11-dimethyl-6H-pyrido[4,;Chlorure de datelliptium;Chlorure de datelliptium [French];Cloruro de dateliptio;Cloruro de dateliptio [Spanish];Datelliptii chloridum;Datelliptii chloridum [Latin];Datelliptium chloride [INN];N-2-(Diethylaminoethyl)-9-hydroxyellipticinum chloride;UNII-L374Y6WE0D;UNII-V5QKF7Q20O
Cas No.
105118-14-7
分子式
C23H28N3O+.C2H3O2-
分子量
421.53
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
Datelliptium chloride 是一种源于 ellipticine 的 DNA 嵌合剂,具有抗肿瘤活性。
生物活性
Datelliptium chloride is a DNA-intercalating agent derived from ellipticine, with anti-tumor activities.
性状
Solid
体外研究(In Vitro)
Datelliptium (100 μM) shows significantly cytotoxic effects after 2 hr of treatment in suspension and primary cultures of rat hepatocytes. Datelliptium mobilizes glycogen in both rat systems in vitro concentration dependently. The half-maximal effect is 14.3 μM in isolated hepatocytes, whereas in cultured rat hepatocytes it is 5.9 μM. Datelliptium also leads to a concentration-dependent decrease in gluconeogenesis from lactate in cells. Datelliptium acetate is selectively cytotoxic for solid tumors over leukemia L1210. Human tumors H-125 and HCT-116 demonstrates less sensitivity to datelliptium acetate. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Upon intravenous administration, datelliptium acetate shows potent inhibitory activities in vivo against a variety of murine solid tumors. Datelliptium acetate is highly active against early-stage colon #38 with highest non-toxic dose (HNTD) of 170 mg/kg TD, and weight loss of 10%, T/C of 0%. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Donato MT, et al. Toxicity of the antitumoral drug datelliptium in hepatic cells: Use of models in vitro for the prediction of toxicity in vivo. Toxicol In Vitro. 1992 Jul;6(4):295-302.[2]. Mucci-LoRusso P, et al. Activity of datelliptium acetate (NSC 311152; SR 95156A) against solid tumors of mice. Invest New Drugs. 1990 Aug;8(3):253-61.
溶解度数据
In Vitro: H2O : 41.67 mg/mL (104.71 mM; Need ultrasonic)DMSO : 5 mg/mL (12.56 mM; Need ultrasonic)配制储备液