Acelarin | NUC-1031 | Nucleoside Analog | AmBeed-信号通路专用抑制剂

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乙酰水杨酸(NUC-1031) /Acelarin {[allProObj[0].p_purity_real_show]}

货号：A426804 同义名： NUC-1031;CPF-31

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

Acelarin 化学结构
CAS号：840506-29-8

Acelarin 3D分子结构
CAS号：840506-29-8

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Acelarin 纯度/质量文件产品仅供科研

货号：A426804 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell Host Microbe, 2024. Ambeed. [ A163338 ]; • Cancer Res., 2024. Ambeed. [ A295334 ]; • J. Pharm. Investig., 2024. Ambeed. [ A221527 , A691302 , A272538 , A187261 ]; • J. Fungi, 2024, 10(11): 751. Ambeed. [ A796919 ]; • JBC, 2024, 107935. Ambeed. [ A194396 ]; 更多 >

DNA 亚型比较

产品名称	DNA synthesis ↓ ↑	helicase ↓ ↑	RdRp ↓ ↑	ribonucleotide reductase ↓ ↑	tRNA synthetase ↓ ↑	YB-1 ↓ ↑	其他靶点	纯度
Fexinidazole	✔							98%
Daptomycin	✔							98%
Blasticidin S·HCl	✔							98%
Metronidazole	✔							98%
Daunorubicin HCl	+++ DNA synthesis, Ki: 20 nM							98%
Triglycidyl isocyanurate	✔						p53	98+%
Nedaplatin	✔							99%+
Bendamustine	✔							98+%
Trifluridine	✔							98%
Robinetin	✔							99%+
Carboplatin	✔							99%
Cidofovir	✔							99%
Cisplatin	✔							99%
Cytarabine	++++ DNA synthesis, IC50: 16 nM							98%
Acelarin	++++ DNA synthesis, EC50: 0.2 nM							99%+
Oxaliplatin	✔							98%
YK-4-279		✔						99%+
ML216		+ BLM^full-length, IC50: 2.98 μM BLM^636-1298, IC50: 0.97 μM						99%+
RK-33		✔						98%
Brr2-IN-3		✔						99%+
Phen-DC3 Trifluoromethanesulfonate		✔						98%
Favipiravir			✔					97%
Suramin sodium salt			++ RdRp, IC50: 0.26 μM					99%+
Clofarabine				++ Ribonucleotide reductase, IC50: 65 nM				97%
Didox				✔				98%
(E)-3-AP				✔				97%
Halofuginone					+++ prolyl-tRNA synthetase, Ki: 18.3nM			99%+
BC-LI-0186					+++ Leucyl-tRNA synthetase, Kd: 42.1 nM Leucyl-tRNA synthetase, IC50: 46.11 nM			98%
SU056						+ YB-1, IC50: 1.73 μM		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Acelarin 生物活性

靶点	DNA synthesis DNA synthesis, EC50:0.2 nM
描述	Gemcitabine is a pyrimidine nucleoside analogue commonly used for the treatment of solid tumors. Acelarin is a gemcitabine ProTide with cytotoxic activity against a range of cancer cell lines in vitro, including L1210 (IC50=0.035±0.02μM), CEM (IC50=0.1±0.03μM), MP-2 (IC50=0.44±0.06μM), and BxPC-3 (IC50=0.15±0.04μM). The colorimetric MTT assay showed that acelarin was more cytotoxic than gemcitabine and its activity was not significantly affected by deoxycytidine. In a nude mouse xenograft model of MiaPaCa-2 human pancreatic cancer cells, acelarin at a dose of 0.076mmol/kg achieved significantly greater reduction in tumor volume than gemcitabine on Day 7 after the first administration of the compounds^[2].
作用机制	Acelarin is a gemcitabine ProTide that bears a phosphoramidate moiety on the 5’-carbon of the ribose. It has been shown to resist cytidine deaminase-mediated degradation. Acelarin bypasses deoxycytidine kinase-mediated monophosphorylation and does not rely on the nucleoside transporter human equilibrative nucleoside transporter-1 to exert the anticancer effect.^[2]

Acelarin 参考文献

[1]Slusarczyk M, Lopez MH, 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.

[2]Slusarczyk M, Lopez MH, 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 development. J Med Chem. 2014;57(4):1531-1542

Acelarin 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.72mL

0.34mL

0.17mL

8.61mL

1.72mL

0.86mL

17.23mL

3.45mL

1.72mL

Acelarin 技术信息

CAS号	840506-29-8
分子式	C₂₅H₂₇F₂N₄O₈P
分子量	580.475

别名	NUC-1031;CPF-31;GTPL7389;MTL-007
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 35 mg/mL(60.3 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

乙酰水杨酸(NUC-1031) /Acelarin {[allProObj[0].p_purity_real_show]}

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乙酰水杨酸(NUC-1031) /Acelarin {[allProObj[0].p_purity_real_show]}

Acelarin 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Acelarin 质控信息

Acelarin 生物活性

Acelarin 参考文献

Acelarin 实验方案

Acelarin 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Acelarin 纯度/质量文件产品仅供科研