中文名称:

甲磺酸伊喜替康

中文同义词:

依喜替康甲磺酸盐;依沙替康甲磺酸盐;(1S,9S)-1-氨基-9-乙基-5-氟-9-羟基-4-甲基-2,3,9,10,13,15-六氢-1H,12H-苯并[DE]吡喃[3,4:6,7]氮茚并[1,2-B]喹啉-10,13-二酮甲磺酸盐;甲磺酸伊喜替康;甲磺酸依喜替康

英文名称:

Exatecan mesilate

英文同义词:

169869-90-3 （free base）;DX 8951; DX 8951;169869-90-3 (FREE BASE);(1S,9S)-1-AMINO-9-ETHYL-5-FLUORO-9-HYDROXY-4-METHYL-2,3,9,10,13,15-HEXAHYDRO-1H,12H-BENZO[DE]PYRANO[3,4:6,7]INDOLIZINO[1,2-B]QUINOLINE-10,13-DIONE MESYLATE;Exatecan mesilate;DX 8951f;Exatecan Meslate;Exatecan (DX-8951) mesylate;DX8951F;DX 8951F;DX-8951F

CAS号:

169869-90-3

分子式:

C25H26FN3O7S

分子量:

531.56

EINECS号:

相关类别:

ADC毒素药物

Mol文件:

169869-90-3.mol

用途

甲磺酸伊喜替康是一种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。

生物活性

Exatecan mesylate (DX8951f) 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 0.975 μg/mL (IC 50 )

Topoisomerase I 0.975 μg/mL (IC 50 )

体外研究

Exatecan mesylate 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.