171335-80-1

中文名称依喜替康

英文名称 Exatecan

CAS 171335-80-1

分子式 C24H22FN3O4

分子量 435.45

MOL 文件 171335-80-1.mol

更新日期 2024/05/14 13:22:09

171335-80-1 结构式

基本信息物理化学性质安全数据常见问题列表

基本信息

中文别名

依喜替康
依喜替康杂质

英文别名

CS-147
DX 8951
Exatecan
Exatecan Impurity
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
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)-
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)

所属类别

生物化工：激动剂抑制剂

物理化学性质

沸点818.4±65.0 °C(Predicted)

密度1.53±0.1 g/cm3(Predicted)

储存条件Store at -20°C,protect from light

溶解度溶于二甲基亚砜

酸度系数(pKa)11.19±0.40(Predicted)

安全数据

危险性符号(GHS)

GHS07

警示词警告

危险性描述H302-H315-H319-H332-H335

防范说明P261-P280-P305+P351+P338

常见问题列表

生物活性

依喜替康 (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 )

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.