Ethynylcytidine (ECyD)
(Synonyms: ECyD; TAS-106; 3'-C-Ethynylcytidine) 目录号 : GC34112
A nucleoside analog with anticancer activity
Cas No.:180300-43-0
Sample solution is provided at 25 µL, 10mM.
Ethynylcitidine (ECyD) is a nucleoside analog with anticancer activity.1,2 It is cytotoxic to A549, NUGC-3, HT-29, MIA PaCa-2, and MCF-7 cancer cells (IC50s = 0.114, 1.032, 0.539, 0.198, and 0.326 ?M, respectively).1 ECyD (0.25 mg/kg per day) reduces tumor growth in CADO-LC11 lung, PAN-12 pancreas, AZ-521 stomach, and CO-3 colon cancer mouse xenograft models.2
1.Shimamoto, Y., Fujioka, A., Kazuno, H., et al.Antitumor activity and pharmacokinetics of TAS-106, 1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)cytosineJpn. J. Cancer Res.92(3)343-351(2001) 2.Takatori, S., Kanda, H., Takenaka, K., et al.Antitumor mechanisms and metabolism of the novel antitumor nucleoside analogues, 1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)cytosine and 1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)uracilCancer Chemother. Pharmacol.44(2)97-104(1999)
Cell experiment: |
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]. |
Animal experiment: |
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]. |
References: [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. |
Cas No. | 180300-43-0 | SDF | |
别名 | ECyD; TAS-106; 3'-C-Ethynylcytidine | ||
Canonical SMILES | OC[C@@H]1[C@@]([C@H]([C@H](N2C(N=C(C=C2)N)=O)O1)O)(C#C)O | ||
分子式 | C11H13N3O5 | 分子量 | 267.24 |
溶解度 | DMSO : 83.3 mg/mL (311.70 mM) | 储存条件 | Store at -20°C |
General tips | 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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1 mg | 5 mg | 10 mg |
1 mM | 3.742 mL | 18.7098 mL | 37.4195 mL |
5 mM | 0.7484 mL | 3.742 mL | 7.4839 mL |
10 mM | 0.3742 mL | 1.871 mL | 3.742 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet