Acelarin (NUC-1031)
(Synonyms: N-(2'-脱氧-2',2'-二氟-P-苯基-5'-胞苷酰)-L-丙氨酸苄酯,NUC-1031) 目录号 : GC34090
A prodrug form of gemcitabine
Cas No.:840506-29-8
Sample solution is provided at 25 µL, 10mM.
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NUC-1031 is a prodrug form of the anticancer nucleoside analog gemcitabine .1,2 NUC-1031 is more lipophilic than gemcitabine and enters cells through passive diffusion.1 It inhibits the growth of L1210, CEM, MP-2, and BxPC-3 cancer cells in vitro (IC50 = 35, 30, 60, and 40 nM, respectively).2 NUC-1031 (0.076 mmol/kg) reduces tumor growth in Mia-PaCa-2 and BxPC-3 mouse xenograft models, which are partially responsive and resistant to gemcitabine, respectively.3
1.Thornton, P.J., Kadri, H., Miccoli, A., et al.Nucleoside phosphate and phosphonate prodrug clinical candidatesJ. Med. Chem.59(23)10400-10410(2016) 2.Slusarczyk, M., Lopez, M.H., Balzarini, J., et al.Application of ProTide technology to gemcitabine: A successful approach to overcome the key cancer resistance mechanisms leads to a new agent (NUC-1031) in clinical developmentJ. Med. Chem.57(4)1531-1542(2014) 3.McGuigan, C., Habib, N.A., Wasan, H.S., et al.A phosphoramidate ProTide (NUC-1031) and acquired and intrinsic resistance to gemcitabineJ. Clin. Oncol.29(15_suppl)e13540(2016)
Cell experiment: | 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]. |
Animal experiment: | 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]. |
References: [1]. Slusarczyk M, et al. Application of ProTide technology to gemcitabine: a successful approach to overcome the key cancer resistance mechanisms leads to a new agent (NUC-1031) in clinical development. J Med Chem. 2014 Feb 27;57(4):1531-42. | |
| Cas No. | 840506-29-8 | SDF | |
| 别名 | N-(2'-脱氧-2',2'-二氟-P-苯基-5'-胞苷酰)-L-丙氨酸苄酯,NUC-1031 | ||
| Canonical SMILES | O=C1N=C(N)C=CN1[C@@H]2O[C@H](COP(OC3=CC=CC=C3)(N[C@H](C(OCC4=CC=CC=C4)=O)C)=O)[C@@H](O)C2(F)F | ||
| 分子式 | C25H27F2N4O8P | 分子量 | 580.47 |
| 溶解度 | DMSO : ≥ 36 mg/mL (62.02 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 | 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 |
| 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
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet