依喜替康

中文名称:

依喜替康

中文同义词:

依喜替康;依喜替康杂质

英文名称:

Exatecan

英文同义词:

10H,13H-BENZO[DE]PYRANO[3,4:6,7]INDOLIZINO[1,2-B]QUINOLINE-10,13-DIONE, 1-AMINO-9-ETHYL-5-FLUORO-1,2,3,9,12,15-HEXAHYDRO-9-HYDROXY-4-METHYL-, (1S,9S)-, MONOMETHANESULFONATE (SALT);exatecan alideximer;(1S,9S)-1-Amino-9-ethyl-5-fluoro-1,2,3,9,12,15-hexahydro-9-hydroxy-4-methyl-10H,13H-benzo(de)pyrano(3,4:6,7)indolizino(1,2-b)quinoline-10,13-dione;Exatecan;DX 8951;CS-147;Exatecan Impurity;10H,13H-Benzo[de]pyrano[3,4:6,7]indolizino[1,2-b]quinoline-10,13-dione, 1-amino-9-ethyl-5-fluoro-1,2,3,9,12,15-hexahydro-9-hydroxy-4-methyl-, (1S,9S)-

CAS号:

171335-80-1

分子式:

C24H22FN3O4

分子量:

435.45

EINECS号:

相关类别:

对照品-杂质对照品;原料药

Mol文件:

171335-80-1.mol

沸点 

818.4±65.0 °C(Predicted)

密度 

1.53±0.1 g/cm3(Predicted)

酸度系数(pKa)

11.19±0.40(Predicted)

生物活性

Exatecan (DX-8951) 是一种 DNA 拓扑异构酶 I (topoisomerase I) 抑制剂，IC50 值为 2.2 μM (0.975 μg/mL)，可用于癌症研究。

靶点

Topoisomerase I 2.2 μM (IC 50 )

Topoisomerase I 2.2 μM (IC 50 )

体外研究

Exatecan is a potent topoisomerase I inhibitor, with an IC 50 of 0.975 μg/mL. Exatecan Mesylate (DX-8951f) significantly inhibits the proliferation of several cancer cell lines, with mean GI 50 s of 2.02 ng/mL, 2.92 ng/mL, 1.53 ng/mL, and 0.877 ng/mL for breast cancer cells, colon cancer cells, stomach cancer cells and lung cancer cells, respectively. Exatecan Mesylate (DX-8951f) displays cytotoxic activities against PC-6, PC-6/SN2-5 cells, with mean GI 50 s of 0.186 and 0.395 ng/mL, respctively. Exatecan Mesylate (34 nM) stabilizes DNA-TopoI complexes in PC-6 and PC-6/SN2-5 cells.

体内研究

Exatecan Mesylate (DX-8951f, 3.325-50 mg/kg, i.v.) exhibits antitumor activities in the mice model bearing tumor cells, without toxic death. Exatecan Mesylate (15, 25 mg/kg, i.v.) hightly inhibits MIA-PaCa, BxPC-3 primary tumor growth in the MIA-PaCa-2 early-stage model and early-stage model of BxPC-3. Exatecan Mesylate (15, 25 mg/kg, i.v.) also significantly suppresses BxPC-3 lymphatic metastasis and completely eliminates lung metastasis in the BxPC-3 late-stage cancer model.