化合物Ethynylcytidine TQ0006

Product Introduction
Bioactivity


英文名: Ethynylcytidine

描述: Ethynylcytidine is a nucleoside antimetabolite.

体外活性: The cytotoxicity of Ethynylcytidine tends to become stronger as the exposure time becomes longer. The IC50 values of Ethynylcytidine in the five human tumors with 4, 24 and 72 h exposure range from 0.114 to 1.032 μM, 0.015 to 0.067 μM, and 0.008 to 0.058 μM, respectively. The differences in IC50 values between the 24 and 72 h exposure times are not large, and Ethynylcytidine appears to show sufficiently potent cytotoxicity at the 24 h exposure time in all 5 human tumors.

体内活性: In both OCUM-2MD3 and LX-1 xenografts, tumor regression is noted and a very potent antitumor effect with a tumor growth inhibition rate on day 15 of approximately 90% or even higher is observed at the minimum toxic doses of Ethynylcytidine on all three administration schedules. In particular, the administration of Ethynylcytidine at 6 mg/kg once weekly exhibits a marked tumor-shrinking effect with an IR of 98% against the LX-1 tumor. While Ethynylcytidine treatment on an either 3 or 5 times weekly schedule has a potent antitumor effect with an IR of approximately 85%, the IR of Ethynylcytidine once weekly is less than 60% and its antitumor effect is rather weak.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 240 mg/mL (898.07 mM)


关键字: TAS106 | TAS 106 | Ethynylcytidine

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