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Sapacitabine

Sapacitabine

产品编号 TQ0245   CAS 151823-14-2
别名: CS682, CYC682

Sapacitabine is a nucleoside analog prodrug with antitumor activity.

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Sapacitabine Chemical Structure
Sapacitabine, CAS 151823-14-2
规格 价格/CNY 货期 数量
2 mg ¥ 374 5日内发货
5 mg ¥ 622 5日内发货
10 mg ¥ 1,080 5日内发货
100 mg ¥ 6,390 8-10周
1 mL * 10 mM (in DMSO) ¥ 672 5日内发货
产品目录号及名称: Sapacitabine (TQ0245)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Sapacitabine is a nucleoside analog prodrug with antitumor activity.
体外活性 Concentrations of Sapacitabine required to achieve an IC50 range from 3±0.6?μM for the colon cancer cell line HCT116 to 67±14?μM for the breast cancer cell line MDA-MB-435. Cell cycle analysis shows that 35% of Sapacitabine-treated cells are arrested in the late-S phase and 41% in the G2/M phase. L1210 cells with deoxycytidine kinase (dCK) activity are sensitive to Sapacitabine, (IC50 20±6 μM) [1].
体内活性 On Day 14, the Sapacitabine (5?mg/kg)+vorinostat (33?mg/kg) group has a mean tumour volume of 245?mm3 and a tumour growth inhibition (TGI) of 92%, whereas the Sapacitabine (15?mg/kg)+vorinostat (33 mg/kg) group has a mean tumour volume of 107?mm3 and a TGI of 112% [2].
细胞实验 A panel of the colon (HT29, HCT116, COLO205, HCC2998), breast (MCF7, MDA-MB-435), lung (HOP62, HOP92), ovarian (OVCAR3, IGROV1) cancer cell lines are used in this study. The cell cycle stage and percentage of apoptotic cells are assessed by flow cytometry. In brief, cells are seeded in 25 cm3 flasks and are untreated or treated with various concentrations of Sapacitabine. At the indicated time points, adherent and non-adherent cells are collected, washed with PBS, fixed in 70% ethanol and stored at 4°C until use. Cells are rehydrated in PBS, incubated for 20?min at room temperature (25°C) with 250?μg/mL RNAse A with Triton X-100 and 20?min at 4°C with 50?μg/mL propidium iodide in the dark. The cell cycle distribution and percentage of apoptotic cells are determined with a flow cytometer and analysed by FACS Calibur [1].
动物实验 Female (nu/nu) mice are injected subcutaneously with 1×107 MV4-11 cells resuspended in 50% Matrigel at a single site on their flanks. Once tumour volumes are 126 to 256?mm3 (16 days post-implantation) animals are pair-matched by tumour size into treatment groups (minimum of six mice per group) with a mean tumour size of ~190?mm3. Tumour measurements are calculated using the formula: volume (mm3)=width2 (mm)×length (mm)×0.5. Sapacitabine is administered once a day orally (5 or 15?mg/kg) for 4 days, followed by a 3-day break before another 4 days of treatment; dosing starts on the same day as distribution to the treatment groups [2].
别名 CS682, CYC682
分子量 490.64
分子式 C26H42N4O5
CAS No. 151823-14-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 24 mg/mL (48.91 mM), sonification/heating is recommended.

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0382 mL 10.1908 mL 20.3815 mL 50.9539 mL
5 mM 0.4076 mL 2.0382 mL 4.0763 mL 10.1908 mL
10 mM 0.2038 mL 1.0191 mL 2.0382 mL 5.0954 mL
20 mM 0.1019 mL 0.5095 mL 1.0191 mL 2.5477 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Serova M, et al. Antiproliferative effects of sapacitabine (CYC682), a novel 2'-deoxycytidine-derivative, in human cancer cells. Br J Cancer. 2007 Sep 3;97(5):628-36. 2. Green SR, et al. Combination of sapacitabine and HDAC inhibitors stimulates cell death in AML and other tumour types. Br J Cancer. 2010 Oct 26;103(9):1391-9.
8-Azaguanosine 2'-Deoxy-2'-fluorocytidine Orotic acid Ascamycin Fludarabine 5,6-Dihydro-5-methyluracil 5-OHdU N2-Methylguanosine

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Sapacitabine 151823-14-2 Cell Cycle/Checkpoint DNA Damage/DNA Repair Nucleoside Antimetabolite/Analog CYC-682 CS682 CS 682 CYC682 CYC 682 CS-682 Inhibitor inhibitor inhibit

 

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