169869-90-3
169869-90-3 結(jié)構(gòu)式
基本信息
甲磺酸伊喜替康
依沙替康甲磺酸鹽
依喜替康甲磺酸鹽
(1S,9S)-1-氨基-9-乙基-5-氟-9-羥基-4-甲基-2,3,9,10,13,15-六氫-1H,12H-苯并[DE]吡喃[3',4':6,7]氮茚并[1,2-B]喹啉-10,13-二酮甲磺酸鹽
Exatecan Meslate
Exatecan mesilate
169869-90-3 （free base）
Exatecan?Mesylate top3
DX8951F
DX 8951F
DX-8951F
Exatecan Mesylate (DX8951f)
Exatecan (DX-8951) mesylate
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
物理化學(xué)性質(zhì)
Water:0.0(Max Conc. mg/mL);0.19(Max Conc. mM)
安全數(shù)據(jù)
very toxic hazardous materials
Muta. 1B
Repr. 1B
常見問題列表
甲磺酸伊喜替康是一種DNA 拓?fù)洚悩?gòu)酶 I (topoisomerase I) 抑制劑，IC50 值為 2.2 μM (0.975 μg/mL)，可用于癌癥研究。
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Topoisomerase I 0.975 μg/mL (IC 50 ) |
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.
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.