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TAS-103 dihydrochloride

CAS No. : 174634-09-4

MCE 站：TAS-103 dihydrochloride

产品活性：TAS-103 dihydrochloride 是一种 DNA 拓扑异构酶 I/II (topoisomerase I/II) 双重抑制剂，可用于癌症研究。

研究领域：Cell Cycle/DNA Damage

作用靶点：Topoisomerase

In Vitro: TAS-103 is a dual inhibitor of DNA topoisomerase I/II. TAS-103 (0.1-10 μM) is active on CCRF-CEM cells, with an IC₅₀ value of 5 nM. TAS-103 (0.1 μM) significantly increases levels of topo IIα FITC immunofluorescence in individual CCRF-CEM cells. TAS-103 (0.01-1 μM) is highly cytotoxic to Lewis lung carcinoma (LLC) cells, and Liposomal TAS-103 is almost as active as free TAS-103. TAS-103 inhibits the viability of HeLa cells, with an IC₅₀ of 40 nM. TAS-103 (10 μM) disrupts signal recognition particle (SRP) complex formation, and induces destabilization of SRP14 and SRP19 and its eventual degradation.

In Vivo: TAS-103 (30 mg/kg, i.v.) causes significant tumor growth suppression in mice bearing Lewis lung carcinoma (LLC) cells, without obvious body weight loss, and the liposomal TAS-103 is more active than free TAS-103.

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