Sapacitabine
目录号: PL07943 纯度: ≥98%
CAS No. :151823-14-2
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中文名称
Sapacitabine
中文别名
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;2-氰基-4,6-二甲基嘧啶;沙帕他滨;10G, 50G, 100G, 1KG
英文名称
Sapacitabine
英文别名
CS-682;Sapacitabine;N-[1-[(2R,3S,4S,5R)-3-Cyano-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-2-oxopyrimidin-4-yl]hexadecanamide;CYC-682;CNDAC;CYC 682;Sapacitabine (CYC682);1-(2-Deoxy-2-cyano-β-D-arabinofuranosyl)cytosine;1-(2-C-Cyano-2-deoxy-β-D-arabino-pentofuranosyl)cytosine;2'-cyano-2'-deoxy-N4-palMitoyl-1-β-D-arabinofuranosyl-cytosine, sapacitabine, CYC682;4-Amino-1-[(3β-cyano-4α-hydroxy-5β-hydroxymethyltetrahydrofuran)-2β-yl]pyrimidin-2(1H)-one;1-(2-cyano-2-deoxy-β-D-arabinofuranosyl)-4-(palMitoylaMino)pyriMidin-2(1H)-one,Sapacitabine
Cas No.
151823-14-2
分子式
C26H42N4O5
分子量
490.64
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Sapacitabine 是口服可用的核苷类似物前体药物,与阿糖胞苷结构上相关。
生物活性
Sapacitabine is an orally available nucleoside analog prodrug that is structurally related to cytarabine.
性状
Solid
IC50 & Target[1][2]
nucleoside analog
体外研究(In Vitro)
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% 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 μM). In the docetaxel/Sapacitabine combinations, synergistic effects (CI<1) are observed when docetaxel is given before Sapacitabine in both cell lines. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
On Day 14, the Sapacitabine (5?mg/kg)+vorinostat (33?mg/kg) group has a mean tumour volume of 245?mm 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?mm and a TGI of 112%. has not independently confirmed the accuracy of these methods. They are for reference only.
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
ClinicalTrial
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.
溶解度数据
In Vitro: DMSO : 33.33 mg/mL (67.93 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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