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180300-43-0

中文名稱 1KG | 備注:廠家優(yōu)勢供應(yīng)
英文名稱 1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)cytosine
CAS 180300-43-0
分子式 C11H13N3O5
分子量 267.24
MOL 文件 180300-43-0.mol
180300-43-0 結(jié)構(gòu)式 180300-43-0 結(jié)構(gòu)式

基本信息

中文別名
化合物ETHYNYLCYTIDINE
英文別名
ECyd
TAS 106
ETHYNYCYTIDINE
Ethynylcytidine
3'-Ethynylcytidine
3'-C-Ethynylcytidine
3’-β-C-Ethynylcytidine
cytidine, 3'-c-ethynyl-
3'-beta-C-Ethynylcytidine
Ethynylcytidine (TAS-106)
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

熔點233-235 °C
沸點536.4±60.0 °C(Predicted)
密度1.61±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
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)
酸度系數(shù)(pKa)11.54±0.70(Predicted)
形態(tài)固體
顏色White to yellow
3'-β-C-乙炔胞苷價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2026/06/05HY-162001KG | 備注:廠家優(yōu)勢供應(yīng)
Ethynylcytidine
180300-43-05mg1400元
2026/06/05HY-162001KG | 備注:廠家優(yōu)勢供應(yīng)
Ethynylcytidine
180300-43-010mM * 1mLin DMSO1540元
2026/06/05HY-162001KG | 備注:廠家優(yōu)勢供應(yīng)
Ethynylcytidine
180300-43-010mg2400元

常見問題列表

生物活性
Ethynylcytidine (ECyD) 是一種核苷類似物,是 RNA 合成 (RNA synthesis) 的有效抑制劑,可抑制 RNA 聚合酶 I,II 和 II。Ethynylcytidine 在多種癌癥模型中均具有強大的抗腫瘤活性。
靶點

nucleoside antimetabolite

體外研究

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.

體內(nèi)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.

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