(1R,9R)-Exatecan mesylate is a potent inhibitor of topoisomerase I, with an IC50 of 0.975 μg/mL in mice and 0.82 μg/mL in humans. This non-prodrug camptothecin derivative stabilizes the enzyme-DNA cleavable complex, effectively blocking topoisomerase I activity and inducing apoptosis. (1R,9R)-Exatecan mesylate demonstrates significant anti-proliferative effects on a variety of malignant tumor cells and addresses P-glycoprotein-mediated multidrug resistance. It is utilized in preclinical research across multiple cancer types, including pancreatic, lung, breast cancers, and leukemia.
(1R,9R)-Exatecan mesylate is a potent inhibitor of topoisomerase I, with an IC50 of 0.975 μg/mL in mice and 0.82 μg/mL in humans. This non-prodrug camptothecin derivative stabilizes the enzyme-DNA cleavable complex, effectively blocking topoisomerase I activity and inducing apoptosis. (1R,9R)-Exatecan mesylate demonstrates significant anti-proliferative effects on a variety of malignant tumor cells and addresses P-glycoprotein-mediated multidrug resistance. It is utilized in preclinical research across multiple cancer types, including pancreatic, lung, breast cancers, and leukemia.
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