硫代秋水仙碱

中文名称:

硫代秋水仙碱

中文同义词:

硫代秋水仙碱;硫秋水仙碱

英文名称:

thiocolchicine

英文同义词:

thiocolchicine;thiocholchicine;(S)-7-Acetylamino-6,7-dihydro-10-methylthio-1,2,3-trimethoxybenzo[a]heptalen-9(5H)-one;(S)-7α-Acetylamino-6,7-dihydro-10-(methylthio)-1,2,3-trimethoxybenzo[a]heptalene-9(5H)-one;10-Demethoxy-10-methylthiocolchicine;10-Thiocolchicine;N-[(S)-5,6,7,9-Tetrahydro-1,2,3-trimethoxy-10-methylthio-9-oxobenzo[a]heptalen-7-yl]acetamide;N-[(7S)-5,6,7,9-Tetrahydro-1,2,3-triMethoxy-10-(Methylthio)-9-oxobenzo[a]heptalen-7-yl]acetaMide

CAS号:

2730-71-4

分子式:

C22H25NO5S

分子量:

415.5

EINECS号:

220-346-8

相关类别:

Intermediates Fine Chemicals;Pharmaceuticals

Mol文件:

2730-71-4.mol

熔点 

193℃

比旋光度 

D20 -221°

沸点 

729.1±60.0 °C(Predicted)

密度 

1.27±0.1 g/cm3(Predicted)

储存条件 

-20°C

溶解度 

DMSO: soluble10mg/mL, clear

酸度系数(pKa)

14.75±0.40(Predicted)

形态

powder

颜色

white to beige

生物活性

Thiocolchicine 是秋水仙碱 (HY-16569) 的衍生物，是一种有效的微管蛋白聚合 (tubulin polymerization) 抑制剂 (IC50=2.5 µM)，竞争性结合微管蛋白 (Ki=0.7 µM)。Thiocolchicine 可以作为 ADC 的毒素分子。

体外研究

Thiocolchicine is against MCF-7, LoVo, LoVo/DX, A-549 and BALB/3T3 cells with IC 50 values of 0.01 μM, 0.021 μM, 0.398 μM, 0.011 μM and 0.114 μM, respectively.Thiocolchicine (1 nM-100 μM; 24-72 hours) shows a relationship between cell cycle blocking activity and growth inhibition in breast cancer cells. It inhibits cell proliferation of MDA-MB-231 and multidrug resistant (MDR) MCF-7 ADRr breast cancer cells with IC 50 s of 0.6 nM and 400 nM, respectively, as well as MDR CEM-VBL leukemia cells (IC 50 =50 nM).

危险品标志 

Xi

危险类别码 

36/37/38

安全说明 

26

危险品运输编号 

UN 1544PSN1 6.1 / PGI

WGK Germany 

3