Ethynylcytidine (Synonyms: ECyD; TAS-106; 3'-C-Ethynylcytidine)

目录号: HY-16200 纯度: 99.97%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

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。Ethynylcytidine 是一种点击化学试剂。它含有 Alkyne 基团，可以和含有 Azide 基团的分子发生铜催化的叠氮-炔环加成反应 (CuAAc)。

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Ethynylcytidine Chemical Structure

CAS No. : 180300-43-0

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1540	In-stock
5 mg	￥1400	In-stock
10 mg	￥2400	In-stock
25 mg	￥5400	In-stock
50 mg		询价
100 mg		询价

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Ethynylcytidine (ECyD), a nucleoside analog and a potent inhibitor of RNA synthesis, inhibits RNA polymerases I, II and II. Ethynylcytidine has robust antitumor activity in a wide range of models of cancer^[1]^[2]^[3]. Ethynylcytidine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC₅₀ & Target

nucleoside antimetabolite^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
BHK-21	EC₅₀	> 100 μM Compound: NM 176	Antiviral activity against Yellow fever virus infected in BHK21 cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay Antiviral activity against Yellow fever virus infected in BHK21 cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay	[PMID: 25082514]
BHK-21	EC₅₀	> 100 μM Compound: NM 176	Antiviral activity against Reovirus type-1 infected in BHK21 cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay Antiviral activity against Reovirus type-1 infected in BHK21 cells assessed as inhibition of virus-induced cytopathogenicity after 3 to 4 days by MTT assay	[PMID: 25082514]
BHK-21	EC₅₀	> 100 μM Compound: NM 176	Antiviral activity against Yellow fever virus infected in BHK-21 cells assessed as inhibition of virus-induced cytopathicity after 3 to 4 days by MTT assay Antiviral activity against Yellow fever virus infected in BHK-21 cells assessed as inhibition of virus-induced cytopathicity after 3 to 4 days by MTT assay	[PMID: 19482481]
BHK-21	EC₅₀	> 100 μM Compound: NM 176	Antiviral activity against Reovirus-1 infected in BHK-21 cells assessed as inhibition of virus-induced cytopathicity after 3 to 4 days by MTT assay Antiviral activity against Reovirus-1 infected in BHK-21 cells assessed as inhibition of virus-induced cytopathicity after 3 to 4 days by MTT assay	[PMID: 19482481]
BHK-21	CC₅₀	> 100 μM Compound: NM 176	Cytotoxicity against mock-infected BHK21 cells after 48 to 96 hrs by MTT assay Cytotoxicity against mock-infected BHK21 cells after 48 to 96 hrs by MTT assay	[PMID: 25082514]
BHK-21	CC₅₀	> 100 μM Compound: NM 176	Cytotoxicity against hamster BHK21 cells assessed as reduction in cell viability after 48 to 96 hrs by MTT assay Cytotoxicity against hamster BHK21 cells assessed as reduction in cell viability after 48 to 96 hrs by MTT assay	[PMID: 19482481]
MT4	CC₅₀	> 100 μM Compound: NM 176	Cytotoxicity against mock-infected human MT4 cells after 96 hrs by MTT assay Cytotoxicity against mock-infected human MT4 cells after 96 hrs by MTT assay	[PMID: 25082514]
MT4	CC₅₀	≥ 100 μM Compound: NM 176	Cytotoxicity against human MT4 cells after 96 hrs by MTT assay Cytotoxicity against human MT4 cells after 96 hrs by MTT assay	[PMID: 19482481]
Vero	CC₅₀	> 100 μM Compound: NM 176	Cytotoxicity against african green monkey Vero 76 cells by crystal violet staining Cytotoxicity against african green monkey Vero 76 cells by crystal violet staining	[PMID: 19482481]
Vero	EC₅₀	> 100 μM Compound: NM 176	Antiviral activity against Vesicular stomatitis virus infected in african green monkey Vero 76 cells assessed as reduction in plaque number after 2 days by plaque reduction assay Antiviral activity against Vesicular stomatitis virus infected in african green monkey Vero 76 cells assessed as reduction in plaque number after 2 days by plaque reduction assay	[PMID: 25082514]
Vero	EC₅₀	> 100 μM Compound: NM 176	Antiviral activity against Vaccinia Virus infected in african green monkey Vero 76 cells assessed as reduction in plaque number after 3 days by plaque reduction assay Antiviral activity against Vaccinia Virus infected in african green monkey Vero 76 cells assessed as reduction in plaque number after 3 days by plaque reduction assay	[PMID: 25082514]
Vero	EC₅₀	> 100 μM Compound: NM 176	Antiviral activity against HSV1 infected in african green monkey Vero 76 cells assessed as reduction in plaque number after 3 days by plaque reduction assay Antiviral activity against HSV1 infected in african green monkey Vero 76 cells assessed as reduction in plaque number after 3 days by plaque reduction assay	[PMID: 25082514]
Vero	EC₅₀	> 100 μM Compound: NM 176	Antiviral activity against Respiratory syncytial virus infected in african green monkey Vero 76 cells assessed as reduction in plaque number after 5 days by plaque reduction assay Antiviral activity against Respiratory syncytial virus infected in african green monkey Vero 76 cells assessed as reduction in plaque number after 5 days by plaque reduction assay	[PMID: 25082514]
Vero	EC₅₀	25 μM Compound: NM 176	Antiviral activity against Poliovirus type 1 Sabin strain infected in african green monkey Vero 76 cells assessed as reduction in plaque number after 2 days by plaque reduction assay Antiviral activity against Poliovirus type 1 Sabin strain infected in african green monkey Vero 76 cells assessed as reduction in plaque number after 2 days by plaque reduction assay	[PMID: 25082514]
Vero	EC₅₀	30 μM Compound: NM 176	Antiviral activity against Coxsackievirus B5 infected in african green monkey Vero 76 cells assessed as reduction in plaque number after 3 days by plaque reduction assay Antiviral activity against Coxsackievirus B5 infected in african green monkey Vero 76 cells assessed as reduction in plaque number after 3 days by plaque reduction assay	[PMID: 25082514]
Vero 76	CC₅₀	> 100 μM Compound: NM 176	Cytotoxicity against mock-infected african green monkey Vero 76 cells after 48 to 96 hrs by MTT assay Cytotoxicity against mock-infected african green monkey Vero 76 cells after 48 to 96 hrs by MTT assay	[PMID: 25082514]
Vero 76	EC₅₀	> 100 μM Compound: NM 176	Antiviral activity against HSV1 infected in Vero-76 cells after 3 days by plaque reduction assay Antiviral activity against HSV1 infected in Vero-76 cells after 3 days by plaque reduction assay	[PMID: 19482481]
Vero 76	EC₅₀	> 100 μM Compound: NM 176	Antiviral activity against Respiratory syncytial virus A2 infected in Vero-76 cells after 5 days by plaque reduction assay Antiviral activity against Respiratory syncytial virus A2 infected in Vero-76 cells after 5 days by plaque reduction assay	[PMID: 19482481]
Vero 76	EC₅₀	24 μM Compound: NM 176	Antiviral activity against Coxsackie virus type B2 virus infected in african green monkey Vero-76 cells after 3 days by plaque reduction assay Antiviral activity against Coxsackie virus type B2 virus infected in african green monkey Vero-76 cells after 3 days by plaque reduction assay	[PMID: 19482481]

体外研究
(In Vitro)

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. 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 24 h 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^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

267.24

Formula

C₁₁H₁₃N₃O₅

CAS 号

180300-43-0

性状

固体

颜色

White to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 250 mg/mL (935.49 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.7420 mL	18.7098 mL	37.4195 mL
5 mM	0.7484 mL	3.7420 mL	7.4839 mL
10 mM	0.3742 mL	1.8710 mL	3.7420 mL

查看完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.78 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.78 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (7.78 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.97%

选择批次：

Data Sheet (634 KB) SDS (252 KB)

COA (197 KB) HNMR (264 KB) RP-HPLC (243 KB) MS (68 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Shimamoto Y, et al. Antitumor activity and pharmacokinetics of TAS-106, 1-(3-C-ethynyl-beta-D-ribo-pentofuranosyl)cytosine. Jpn J Cancer Res. 2001 Mar;92(3):343-51. [Content Brief]

[2]. Abdelrahim M, et al. TAS-106: preclinical, clinical and beyond. Oncology. 2013;85(6):356-363. [Content Brief]

[3]. Hammond-Thelin LA, et al. Phase I and pharmacokinetic study of 3'-C-ethynylcytidine (TAS-106), an inhibitor of RNA polymerase I, II and III,in patients with advanced solid malignancies. Invest New Drugs. 2012;30(1):316-326. [Content Brief]

Cell Assay ^[1]	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/1.8 mL/well) on day 0. Twenty-four hours after seeding, on day 1, Ethynylcytidine (TAS-106) (6 concentrations range from 0 to 100 μM) is added to cultured cells (3 wells at each concentration) at a volume of 0.2 mL/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^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Nude rats s.c. transplanted with LX-1 human lung tumors are given a single i.v. dose of [³H]Ethynylcytidine (TAS-106) (6 mg/kg, 3.7 MBq/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^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Shimamoto Y, et al. Antitumor activity and pharmacokinetics of TAS-106, 1-(3-C-ethynyl-beta-D-ribo-pentofuranosyl)cytosine. Jpn J Cancer Res. 2001 Mar;92(3):343-51. [Content Brief] [2]. Abdelrahim M, et al. TAS-106: preclinical, clinical and beyond. Oncology. 2013;85(6):356-363. [Content Brief] [3]. Hammond-Thelin LA, et al. Phase I and pharmacokinetic study of 3'-C-ethynylcytidine (TAS-106), an inhibitor of RNA polymerase I, II and III,in patients with advanced solid malignancies. Invest New Drugs. 2012;30(1):316-326. [Content Brief]

Ethynylcytidine 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.7420 mL	18.7098 mL	37.4195 mL	93.5489 mL
	5 mM	0.7484 mL	3.7420 mL	7.4839 mL	18.7098 mL
	10 mM	0.3742 mL	1.8710 mL	3.7420 mL	9.3549 mL
	15 mM	0.2495 mL	1.2473 mL	2.4946 mL	6.2366 mL
	20 mM	0.1871 mL	0.9355 mL	1.8710 mL	4.6774 mL
	25 mM	0.1497 mL	0.7484 mL	1.4968 mL	3.7420 mL
	30 mM	0.1247 mL	0.6237 mL	1.2473 mL	3.1183 mL
	40 mM	0.0935 mL	0.4677 mL	0.9355 mL	2.3387 mL
	50 mM	0.0748 mL	0.3742 mL	0.7484 mL	1.8710 mL
	60 mM	0.0624 mL	0.3118 mL	0.6237 mL	1.5591 mL
	80 mM	0.0468 mL	0.2339 mL	0.4677 mL	1.1694 mL
	100 mM	0.0374 mL	0.1871 mL	0.3742 mL	0.9355 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Ethynylcytidine (Synonyms: ECyD; TAS-106; 3'-C-Ethynylcytidine)

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参考文献

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Ethynylcytidine (Synonyms: ECyD; TAS-106; 3'-C-Ethynylcytidine)

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参考文献

Ethynylcytidine 相关抗体:

摩尔计算器

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完整储备液配制表

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