Sapacitabine
(Synonyms: N-[1-[(2R,3S,4S,5R)-3-氰基-4-羟基-5-(羟甲基)氧杂环戊-2-基]-2-氧代嘧啶-4-基]十六酰胺,CS682; CYC682) 目录号 : GC19319
Sapacitabine 是一种可口服的核苷类似物前药，在结构上与阿糖胞苷相关。
Cas No.:151823-14-2
Sample solution is provided at 25 µL, 10mM.
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Sapacitabine is an orally available nucleoside analog prodrug that is structurally related to cytarabine.
Concentrations of Sapacitabine required to achieve an IC50 range from 3±0.6 uM for the colon cancer cell line HCT116 to 67±14 uM for the breast cancer cell line MDA-MB-435. Cell cycle analysis shows that 35% Sapacitabine-treated cells are arrested in late-S phase and 41% in G2/M phase. L1210 cells with deoxycytidine kinase (dCK) activity are sensitive to Sapacitabine, (IC50 20±6 uM). In the docetaxel/Sapacitabine combinations, synergistic effects (CI<1) are observed when docetaxel is given before Sapacitabine in both cell lines[1].
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].
References:
[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.
Cell experiment: | A panel of 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 flow cytometer and analysed by FACS Calibur[1]. |
Animal experiment: | 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]. |
References: [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. | |
| Cas No. | 151823-14-2 | SDF | |
| 别名 | N-[1-[(2R,3S,4S,5R)-3-氰基-4-羟基-5-(羟甲基)氧杂环戊-2-基]-2-氧代嘧啶-4-基]十六酰胺,CS682; CYC682 | ||
| Canonical SMILES | O=C(N=C(NC(CCCCCCCCCCCCCCC)=O)C=C1)N1[C@H]2[C@@H](C#N)[C@H](O)[C@@H](CO)O2 | ||
| 分子式 | C26H42N4O5 | 分子量 | 490.64 |
| 溶解度 | DMSO : 25 mg/mL (50.95 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 | 2.0382 mL | 10.1908 mL | 20.3815 mL |
| 5 mM | 0.4076 mL | 2.0382 mL | 4.0763 mL |
| 10 mM | 0.2038 mL | 1.0191 mL | 2.0382 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: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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