3'-β-C-乙炔胞苷

生物活性靶点体外研究体内研究 3'-β-C-乙炔胞苷试剂级价格

3'-β-C-乙炔胞苷

CAS号:180300-43-0
英文名:1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)cytosine
中文名:3'-β-C-乙炔胞苷
CBNumber:CB02490124
分子式:C11H13N3O5
分子量:267.24
MOL File:180300-43-0.mol

3'-β-C-乙炔胞苷化学性质

熔点 :233-235 °C
沸点 :536.4±60.0 °C(Predicted)
密度 :1.61±0.1 g/cm3(Predicted)
储存条件 :Store at -20°C
溶解度 :DMSO:127.5(Max Conc. mg/mL);477.1(Max Conc. mM)
DMF:5.0(Max Conc. mg/mL);18.71(Max Conc. mM)
PBS (pH 7.2):10.0(Max Conc. mg/mL);37.42(Max Conc. mM)
形态 :A solid
酸度系数(pKa) :11.54±0.70(Predicted)
颜色 :White to yellow

3'-β-C-乙炔胞苷性质、用途与生产工艺

生物活性 Ethynylcytidine (ECyD) 是一种核苷类似物，是 RNA 合成 (RNA synthesis) 的有效抑制剂，可抑制 RNA 聚合酶 I，II 和 II。Ethynylcytidine 在多种癌症模型中均具有强大的抗肿瘤活性。
靶点

nucleoside antimetabolite
体外研究

The IC ₅₀ 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. These results suggest that the cytotoxicity of Ethynylcytidine tends to become stronger as the exposure time becomes longer. The differences in IC ₅₀ values between the 24 and 72 h exposure times are not large, and Ethynylcytidine appeares to show sufficiently potent cytotoxicity at the 24 h exposure time in all 5 human tumors. Even at the 4 h exposure time, Ethynylcytidine clearly shows potent cytotoxicity with IC ₅₀ values at submicromolar concentrations in 4 of the 5 human tumors.
体内研究

In both OCUM-2MD3 and LX-1 xenografts, tumor regression is noted and a very potent antitumor effect with an tumor growth inhibition rate (IR) on day 15 of approximately 90% or even higher is observed at the minimum toxic doses of Ethynylcytidine (TAS-106) on all three administration schedules. In particular, 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.