Exatecan

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.

Exatecan is a potent topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL. Exatecan Mesylate (DX-8951f) significantly inhibits the proliferation of several cancer cell lines, with mean GI50s 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 GI50s 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.

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Antibody Drug Conjugates (ADC)

ADC Cytotoxin

ADC Cytotoxin | Topoisomerase

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171335-80-1

435.45

C24H22FN3O4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 20 mg/mL (45.93 mM; 超声助溶 )

N[C@@H]1C2=C3C(C=4N(C3)C(=O)C5=C(C4)[C@](CC)(O)C(=O)OC5)=NC=6C2=C(CC1)C(C)=C(F)C6

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(-20℃)

With Ice Pack

≥ 2 years