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乙酰水杨酸(NUC-1031) /Acelarin 99%+

货号:A426804 同义名: NUC-1031;CPF-31 Ambeed 开学季,买赠积分,赢豪礼

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 化学结构
CAS号:840506-29-8
Acelarin 3D分子结构
CAS号:840506-29-8
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: 99%+
批次查询: 批次纯度:

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产品名称 DNA synthesis helicase RdRp ribonucleotide reductase tRNA synthetase YB-1 其他靶点 纯度
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Metronidazole 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

98%
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Nedaplatin 99%+
Bendamustine 98+%
Trifluridine 98%
Robinetin 99%+
Carboplatin 99%
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Cisplatin 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

99%+
Oxaliplatin 98%
YK-4-279 99%+
ML216 +

BLMfull-length, IC50: 2.98 μM

BLM636-1298, 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

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

液体 -20°C:3-6个月-80°C:12个月

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
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