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290304-24-4

中文名称 (8S,10S)-8-乙酰基-7,8,9,10-四氢-6,8,11-三羟基-1-甲氧基-10-[[2,3,6-三脱氧-3-[[[[4-(BETA-D-吡喃半乳糖基氧基)-3-硝基苯基]甲氧基]羰基]氨基]-ALPHA-L-来苏-己糖吡喃糖苷]氧基]-5,12-并四苯醌
英文名称 Daun02
CAS 290304-24-4
分子式 C41H44N2O20
分子量 884.79
MOL 文件 290304-24-4.mol
更新日期 2024/11/05 14:08:42
290304-24-4 结构式 290304-24-4 结构式

基本信息

中文别名
(8S,10S)-8-乙酰基-7,8,9,10-四氢-6,8,11-三羟基-1-甲氧基-10-[[2,3,6-三脱氧-3-[[[[4-(BETA-D-吡喃半乳糖基氧基)-3-硝基苯基]甲氧基]羰基]氨基]-ALPHA-L-来苏-己糖吡喃糖苷]氧基]-5,12-并四苯醌
英文别名
Daun02
DAUN 02
DAUN-02
5,12-Naphthacenedione, 8-acetyl-7,8,9,10-tetrahydro-6,8,11-trihydroxy-1-methoxy-10-[[2,3,6-trideoxy-3-[[[[4-(β-D-galactopyranosyloxy)-3-nitrophenyl]methoxy]carbonyl]amino]-α-L-lyxo-hexopyranosyl]oxy]-, (8S,10S)-
(8S,10S)-8-Acetyl-7,8,9,10-tetrahydro-6,8,11-trihydroxy-1-methoxy-10-[[2,3,6-trideoxy-3-[[[[4-(beta-D-galactopyranosyloxy)-3-nitrophenyl]methoxy]carbonyl]amino]-alpha-L-lyxo-hexopyranosyl]oxy]-5,12-naphthacenedione
所属类别
生物化工:激动剂抑制剂

物理化学性质

沸点1128.4±65.0 °C(Predicted)
密度1.67±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度insoluble in H2O; insoluble in EtOH; ≥17.92 mg/mL in DMSO with ultrasonic
酸度系数(pKa)7.39±0.60(Predicted)
形态粉末
颜色Brown to wine

常见问题列表

生物活性
Daun02是拓扑异构酶抑制剂Daunorubicin的前药。
靶点

Topoisomerase

Daunorubicins/Doxorubicins

体外研究

Daun02 is a prodrug, which is converted by β-galactosidase to Daunorubicin, which has been shown to reduce calcium ion (Ca 2+ )-dependent action potentials in neuroblastoma cells. Daunorubicin is a topoisomerase inhibitor. Daun02 is a good substrate for β-galactosidase (β-gal). The concentration of Daun02 producing 50% (EC 50 ) decrease in cell viability is 0.5 μM, 1.5 μM, and 3.5 μM for T47-D, Panc02, and MCF-7, respectively.

体内研究

Daun02 is a good substrate for β-gal with K m and V max values of 0.37 mM and 8.6 μmol/min/mg protein. At a concentration of 10 -5 M, Daun02 is 79% bound to plasma protein compares to 94% for Daunomycin.

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