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Exatecan mesylate

CAS No. : 169869-90-3

MCE 站：Exatecan mesylate

产品活性：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。

研究领域：Cell Cycle/DNA Damage

作用靶点：Topoisomerase

In Vitro: Exatecan mesylate 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.

In Vivo: 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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