中文名称:

CS-2069

中文同义词:

ALDH1A1抑制剂(NCT-501)

英文名称:

NCT-501

英文同义词:

NCT-501;CS-2069;1H-Purine-2,6-dione, 8-[[4-(cyclopropylcarbonyl)-1-piperazinyl]methyl]-3,7-dihydro-1,3-dimethyl-7-(3-methylbutyl)-;NCT-501 >=98% (HPLC)

CAS号:

1802088-50-1

分子式:

C21H32N6O3

分子量:

416.52

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

1802088-50-1.mol

沸点 

627.3±65.0 °C(Predicted)

密度 

1.37±0.1 g/cm3(Predicted)

酸度系数(pKa)

5.26±0.10(Predicted)

生物活性

NCT-501 是一种茶碱类的有效醛脱氢酶 1A1 (ALDH1A1) 选择性抑制剂, 抑制 hALDH1A1 时 IC50 值为 40 nM, 选择性超过其它 ALDH 同工酶和其它脱氢酶 (作用于 hALDH1B1, hALDH3A1, 和 hALDH2 时, IC50值 >57 UM)。

靶点

IC50: 40 nM (hALDH1A1)

体外研究

NCT-501 shows a 16% decrease in the Cal-27 CisR cell line at 20 nM concentration, though the difference was not statistically significant.

体内研究

NCT-501 (100 µg/animal; i.t.; every alternate day for 20 days) shows a 78% inhibition in tumor growth in Cal-27 CisR derived xenografts. Animal Model: 5-6 weeks old male Hsd: Athymic Nude-Foxn1nu (immuno-deficient-mice bearing Cal-27 CisR cells) Dosage: 100µg/animal Administration: Intra-tumorally (i.t); every alternate day for 20 days Result: Showed a 78% inhibition in tumor growth in Cal-27 CisR derived xenografts.

Animal Model:

5-6 weeks old male Hsd: Athymic Nude-Foxn1nu (immuno-deficient-mice bearing Cal-27 CisR cells)

Dosage:

100µg/animal

Administration:

Intra-tumorally (i.t); every alternate day for 20 days

Result:

Showed a 78% inhibition in tumor growth in Cal-27 CisR derived xenografts.