Ethynylcytidine - CAS:180300-43-0 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	Ethynylcytidine 一键复制产品信息
英文名称:	Ethynylcytidine
别名:	1-(3-C-ETHYNYL-BETA-D-RIBO-PENTOFURANOSYL)CYTOSINE ECyD; TAS-106; 3'-C-Ethynylcytidine
CAS No:	180300-43-0	分子式:	C₁₁H₁₃N₃O₅	分子量:	267.24
CAS No:	180300-43-0
分子式:	C₁₁H₁₃N₃O₅
分子量:	267.24

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

E10387 Ethynylcytidine ≥95% (普西唐-psaitong)

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包装规格：

5mg 10mg 25mg in glass bottle

溶解性：

溶于DMSO（250 mg/mL 超声）

产品描述：

基本信息

产品编号：E10387
产品名称：Ethynylcytidine
CAS:	180300-43-0	储存条件	粉末	-20℃	四年

分子式：	C11H13N3O5		溶于液体	-80℃	六个月
分子量	267.24			-20℃	一个月
化学名：	4-Amino-1-((2R,3R,4S,5R)-4-ethynyl-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one
Solubility (25°C)	体外	DMSO	200mg/mL (748.39mM; Need ultrasonic)
		Ethanol
		Water
	体内	现配现用
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	3.7420mL	18.7098mL	37.4195mL
5mM	0.7484mL	3.7420mL	7.4839mL
10mM	0.3742mL	1.8710mL	3.7420mL

生物活性

产品描述	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/IC₅₀	nucleoside antimetabolite
体外研究	The IC50 values of Ethynylcytidine in the five human tumors with 4, 24 and 72 h exposure range from 0.114 to 1.032μM, 0.015 to 0.067μM, and 0.008 to 0.058μM, respectively. These results suggest that the cytotoxicity of Ethynylcytidine tends to become stronger as the exposure time becomes longer. The differences in IC50 values between the 24 and 72 h exposure times are not large, and Ethynylcytidine appeares to show sufficiently potent cytotoxicity at the 24h exposure time in all 5 human tumors. Even at the 4 h exposure time, Ethynylcytidine clearly shows potent cytotoxicity with IC50 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 6mg/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.

推荐实验方法(仅供参考)

细胞实验：

Cell Assay

MIAPaCa-2 cells are maintained in Dulbecco’s modified Eagle’s medium supplemented with 10% FCS and 2.5% horse serum. Cells in the exponential growth phase are seeded onto 6-well plates (5×104 cells/1.8mL/well) on day 0. Twenty-four hours after seeding, on day 1, Ethynylcytidine (TAS-106) (6 concentrations range from 0 to 100μM) is added to cultured cells (3 wells at each concentration) at a volume of 0.2mL/well. After 4 and 24 h, on the 4 and 24 h Ethynylcytidine exposure schedules, the drug-containing medium is removed, and the cells are washed twice with Dulbecco’s phosphate buffered saline and subsequently cultured in drug-free medium until day 4. On the 72 h exposure schedule, after adding the Ethynylcytidine, cells are cultured continuously until day 4. On day 4, cell numbers are determined and converted to values related to the cell numbers on day 1. The concentration of Ethynylcytidine which inhibits cell growth by 50% (IC50) is calculated from this relative cell growth. Two or three individual experiments are conducted on each cell line to confirm reproducibility.

动物实验:

Animal Administration

Nude rats s.c. transplanted with LX-1 human lung tumors are given a single i.v. dose of [³H]Ethynylcytidine (TAS-106) (6mg/kg, 3.7MBq/kg). For analysis of the distribution of radioactivity and intratumoral Ethynylcytidine metabolism, serum and various tissues (tumor, skin, lung, liver, kidney, spleen, small intestine, large intestine, testis, brain, and bone marrow cells) are sampled from 3 rats at each of the following 6 time points: 0.5, 1, 2, 4, 8 and 24 h after i.v. administration. At each point in time, bone marrow cells are collected from the 3 rats and combined into a cell pellet. All samples of serum, bone marrow cell pellets, and tissues are immediately frozen on dry ice and stored at -30°C until used.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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