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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Acelarin
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
840506-29-8
- 规格：
50mg/25mg/10mg/5mg/1mg
| 规格： | 50mg | 产品价格： | ￥5340.0 |
|---|---|---|---|
| 规格： | 25mg | 产品价格： | ￥3490.0 |
| 规格： | 10mg | 产品价格： | ￥1790.0 |
| 规格： | 5mg | 产品价格： | ￥1090.0 |
| 规格： | 1mg | 产品价格： | ￥490.0 |
| 基本信息 | |
| CAS | No.840506-29-8 |
| 英文名称 | Acelarin |
| 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 |
| 分子式 | C25H27F2N4O8P |
| 分子量 | 580.47 |
| 溶解性 | Soluble in DMSO ≥3mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD27987942 |
| SMILES | CC(C(=O)OCC1=CC=CC=C1)NP(=O)(OCC2C(C(C(O2)N3C=CC(=NC3=O)N)(F)F)O)OC4=CC=CC=C4 |
| InChIKey | NHTKGYOMICWFQZ-KKQYNPQSSA-N |
| InChI | InChI=1S/C25H27F2N4O8P/c1-16(22(33)36-14-17-8-4-2-5-9-17)30-40(35，39-18-10-6-3-7-11-18)37-15-19-21(32)25(26，27)23(38-19)31-13-12-20(28)29-24(31)34/h2-13，16，19，21，23，32H，14-15H2，1H3，(H，30，35)(H2，28，29，34)/t16-，19+，21+，23+，40 /m0/s1 |
| PubChem CID | 11169170 |
| 靶点 | DNA/RNA Synthesis |
| 通路 | Cell Cycle;DNA Damage/DNA Repair |
| 背景说明 | 是一种 DNA synthesis 的抑制剂。 |
| 生物活性 | Acelarin (NUC-1031) is a ProTide transformation and enhancement of the widely-used nucleoside analogue， gemcitabine.[1] |
| IC50 | EC50：0.2 nM (DNA synthesis inhibitor)[1] |
| 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[1]. |
| 细胞实验 | 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]. |
| 细胞实验 | 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]. |
| 动物实验 | 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]. |
| 数据来源文献 | [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. |
| 单位 | 瓶 |
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文献和实验了样品的液流技术、细胞的分选和计数技术，以及数据的采集和分析技术等。 2.细胞的参量和荧光探针 FCM 是通过测量细胞的多种参量来获取信息的，细胞参数分为结构参量和功能参量两大类。结 构参量主要用于描述细胞的化学组分和形态特征，例如DNA、RNA的含量，总蛋白含量、胞内PH值 和细胞大小等；功能参量主要是描述细胞整体的理化和生物特性，如：细胞周期动力学、特殊配体的鉴 定、特殊细胞的生物活性等，这些参量有的需要经荧光标记才能被测定，有的并不需要荧光标记[4]。 2．1参数
了样品的液流技术、细胞的分选和计数技术，以及数据的采集和分析技术等。 2.细胞的参量和荧光探针 FCM 是通过测量细胞的多种参量来获取信息的，细胞参数分为结构参量和功能参量两大类。结 构参量主要用于描述细胞的化学组分和形态特征，例如DNA、RNA的含量，总蛋白含量、胞内PH值 和细胞大小等；功能参量主要是描述细胞整体的理化和生物特性，如：细胞周期动力学、特殊配体的鉴 定、特殊细胞的生物活性等，这些参量有的需要经荧光标记才能被测定，有的并不需要荧光标记[4]。 2．1参数
A逆转录技术和PCR技术相结合的一种RNA指纹图谱技术。每一种细胞（包括同一组织细胞经过不同的处理）都有其特异表达的不同于其他组织细胞的基因谱（有差异基因表达），即特异的RNA指纹图谱。差异基因表达是细胞分化的基础，正是这些基因在细胞中的特异表达与否，决定了生命历程中细胞的发育和分化、细胞周期调节、细胞衰老和凋亡等。mRNA DDR T－PCR 技术正是对组织特异性表达基因进行分离的一种快速而行之有效的方法。 其基本原理是从基因背景相同的2个或几个被比较的细胞系或组织中提取总RNA，逆转录成cDNA
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