1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis
  3. Acelarin

Acelarin (Synonyms: NUC-1031)

目录号: HY-100885 纯度: 99.76%
产品使用指南

Acelarin(NUC-1031)是广泛使用的核苷类似物吉西他滨的蛋白转化和增强。

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Acelarin Chemical Structure

Acelarin Chemical Structure

CAS No. : 840506-29-8

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Acelarin (NUC-1031) is a ProTide transformation and enhancement of the widely-used nucleoside analogue, gemcitabine.

IC50 & Target

EC50:0.2 nM (DNA synthesis inhibitor)[1]

体外研究
(In Vitro)

Gemcitabine is a nucleoside analogue commonly used in cancer therapy but with limited efficacy due to a high susceptibility to cancer cell resistance. The addition of a phosphoramidate motif to the gemcitabine can protect it against many of the key cancer resistance mechanisms. A series of gemcitabine phosphoramidate prodrugs are synthesized and screened for cytostatic activity in a range of different tumor cell lines. Among the synthesized compounds, NUC-1031 is shown to be potent in vitro.

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

体内研究
(In Vivo)

The ProTide demonstrates a significant reduction in tumor size against pancreatic xenograft models compared with the gemcitabine treated group, and less adverse effects on body weight, indicating a better safety profile. Data strongly suggests that the ProTides are not reliant on kinases or nucleoside transporters to exert their activity inside tumor cells and remain stable in the presence of deaminases. The ProTide NUC-1031 is currently advancing through phase I/II clinical studies and has already generated strong pharmacokinetic data that confirm significantly higher intracellular levels of gemcitabine triphosphate, together with promising early efficacy signals and a favorable safety profile. The phosphoramidate chemistry is potentially a great source of new and very effective anticancer agents, bringing a considerable array of advanced treatments specifically designed to overcome cancer resistance mechanisms that will benefit a greater proportion of patients[1].

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

Clinical Trial
分子量

580.47

Formula

C25H27F2N4O8P

CAS 号
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 36 mg/mL (62.02 mM)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7227 mL 8.6137 mL 17.2274 mL
5 mM 0.3445 mL 1.7227 mL 3.4455 mL
10 mM 0.1723 mL 0.8614 mL 1.7227 mL
*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.58 mM,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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.58 mM,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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.58 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    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。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
Cell Assay
[1]

NUC-1031(5.0 mg) is dissolved in DMSO (0.050 mL) and D2O (0.15 mL). After recording the control 31P NMR at 37 °C, a previously defrosted human, rat, or dog serum (0.30 mL) is added to the sample, which is next submitted to the 31P NMR experiments at 37°C. The spectra are recorded every 30 min over 13 h. 31P NMR recorded data are processed and analyzed with the Bruker Topspin 2.1 program[1].

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

Animal Administration
[1]

Balb/c nude mice are female, six to eight week old, with the weight of 20 ± 2 g. They are intraperitoneally given NUC-1031 (i.p 0.228 mmol/kg, 132.3 mg/kg, 2×/WK) or vehicle for 2 weeks. NUC-1031 is dissolved in 40% Captisol solution. (40% Captisol is prepared by dissolving 20mg of Captisol with pure water, and made the final volume 50 mL. The solvent is filtered with 0.22 μm filter). Mice are monitored daily for body weight change and clinical symptoms for 2 weeks[1].

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

参考文献

纯度: 99.76%

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质量   浓度   体积   分子量 *
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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)
× = ×
C1   V1   C2   V2

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目录号:
HY-100885
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