中文名称 |
Salinosporamide A (NPI-0052, Marizomib)
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中文别名 |
假尿苷
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英文名称 |
Salinosporamide A (NPI-0052, Marizomib)
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英文别名 |
(-)-Salinosporamide A;(1S,2R,5R)-2-(2-chloroethyl)-5-[(S)-[(1S)-cyclohex-2-en-1-yl]-hydroxymethyl]-1-methyl-7-oxa-4-azabicyclo[3.2.0]heptane-3,6-dione;MarizoMib;Marizomib(Salinosporamide A);Marizomib(Salinosporamide A)〜D4;NPI-0052;Salinosporamide A;ML 858;NPI 0052;(1R,4R,5S)-4-(2-Chloroethyl)-1-[(S)-(1S)-2-cyclohexen-1-ylhydroxymethyl]-5-methyl-6-oxa-2-azabicyclo[3.2.0]heptane-3,7-dione
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Cas No. |
437742-34-2
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分子式 |
C15H20NO4Cl
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分子量 |
313.78
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包装储存 |
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生物活性 |
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively). |
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性状 |
Solid |
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IC50 & Target[1][2] |
IC50: 3.5 nM (CT-L), 28 nM (CT-T-laspase-like), 430 nM (trypsin-like) |
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体外研究(In Vitro) |
Marizomib (Salinosporamide A) (0.1-10000 nM; 72 hours) effectively reduces survival of D-54 and U-251 cells in a dose-dependent manner. The IC50s are ~52 nM for U-251 and ~20 nM for D-54. Medlife has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation Assay
Apoptosis Analysis
Western Blot Analysis
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体内研究(In Vivo) |
Marizomib (Salinosporamide A) (0.15 mg/kg; i.v; twice a week for three weeks) significantly decreases tumor growth, and is not associated with any toxicity. Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
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运输条件 |
Room temperature or refrigerated transportation. |
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储存方式 |
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ClinicalTrial |
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参考文献 |
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溶解度数据 |
体外研究:
DMSO : ≥ 100 mg/mL (318.69 mM) * "≥" means soluble, but saturation unknown. 配制储备溶液
*
产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效。 体内研究:
建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。
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