Acelarin
产品说明书
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同义名 : | NUC-1031; CPF-31; GTPL7389; MTL-007 |
| CAS号 : | 840506-29-8 | |
| 货号 : | A426804 | |
| 分子式 : | C25H27F2N4O8P | |
| 纯度 : | 99%+ | |
| 分子量 : | 580.47 | |
| MDL号 : | MFCD27987942 | |
| 存储条件： |
Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 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 |
| 生物活性 | |||
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| 靶点 |
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| 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] | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.72mL 0.34mL 0.17mL |
8.61mL 1.72mL 0.86mL |
17.23mL 3.45mL 1.72mL |
| 参考文献 |
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