Exatecan (DX-8951) 是一种具有 2.2 μM (0.975 μg/mL) IC50 的 DNA 拓扑异构酶 I 抑制剂，用于癌症研究。
HazMat Fee +
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
Exatecan is a highly potent inhibitor of topoisomerase I, possessing an IC50 value of 0.975 μg/mL. Exatecan Mesylate (DX-8951f) effectively suppresses the proliferation of various cancer cell lines, with mean GI50 values of 2.02 ng/mL, 2.92 ng/mL, 1.53 ng/mL, and 0.877 ng/mL for breast, colon, stomach, and lung cancer cells, respectively [1]. Exatecan Mesylate (DX-8951f) exhibits cytotoxic effects against PC-6 and PC-6/SN2-5 cells, with mean GI50 values of 0.186 and 0.395 ng/mL, respectively. At a concentration of 34 nM, Exatecan Mesylate stabilizes DNA-TopoI complexes in both PC-6 and SN2-5 cells [3].
体内研究
Exatecan Mesylate (DX-8951f, 3.325-50 mg/kg, i.v.) demonstrates antitumor effects in mouse models bearing tumor cells, without causing toxic fatalities [1].
Exatecan Mesylate (15, 25 mg/kg, i.v.) effectively suppresses primary tumor growth in MIA-PaCa and BxPC-3 models at early stages. Additionally, at the same doses, it significantly inhibits lymphatic metastasis in BxPC-3 and completely eradicates lung metastasis in the late-stage BxPC-3 cancer model [2].
体外研究
Exatecan is a highly potent inhibitor of topoisomerase I, possessing an IC50 value of 0.975 μg/mL. Exatecan Mesylate (DX-8951f) effectively suppresses the proliferation of various cancer cell lines, with mean GI50 values of 2.02 ng/mL, 2.92 ng/mL, 1.53 ng/mL, and 0.877 ng/mL for breast, colon, stomach, and lung cancer cells, respectively [1].
Exatecan Mesylate (DX-8951f) exhibits cytotoxic effects against PC-6 and PC-6/SN2-5 cells, with mean GI50 values of 0.186 and 0.395 ng/mL, respectively. At a concentration of 34 nM, Exatecan Mesylate stabilizes DNA-TopoI complexes in both PC-6 and SN2-5 cells [3].
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