Nelfinavir (AG-1341) 是一种有效的口服生物可利用的HIV-1 蛋白酶抑制剂 (Ki=2 nM) 用于 HIV 感染。Nelfinavir (AG-1341) 是一种广谱的抗癌剂。
| 生物活性 | Nelfinavir (AG-1341) is a potent and orally bioavailableHIV-1proteaseinhibitor (Ki=2 nM) for HIVinfection. Nelfinavir is a broad-spectrum, anticancer agent[1][2][3]. |
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体外研究
(In Vitro) | Nelfinavir (AG1341) (1-10 μM; 48 hours) inhibits the proliferation of multiple myeloma cells[4].
Nelfinavir inhibits 26S chymotrypsin-like proteasome activity, impairs proliferation and triggers apoptosis of the myeloma cell lines and fresh plasma cells[4].
Nelfinavir (1-10 μM; 17 hours) induces apoptosis of multiple myeloma cell lines[4].
Nelfinavir (5 μM; 0-24 hours) decreases the phosphorylation of AKT[4].
Nelfinavir activates the cleavage of caspase-3, decreases the phosphorylation of AKT, STAT-3, ERK1/2, and activates the pro-apoptotic pathway of the unfolded protein response system[4].
Nelfinavir is also aSARS-CoV 3CLproinhibitor with anIC50of 35.93 μM[5].
Cell Proliferation Assay[4] | Cell Line: | RPMI, LP1, U266, OPM2 and MM1S cells | | Concentration: | 1, 2, 5, 10 μM | | Incubation Time: | 48 hours | | Result: | Inhibited the proliferation of RPMI, LP1, U266, OPM2 and MM1S cell lines in a dose-dependent manner with an IC50of 1-5 μM. |
Apoptosis Analysis[4] | Cell Line: | LP1 and U266 cells | | Concentration: | 1-10 μM | | Incubation Time: | 17 hours | | Result: | Induced a dose-dependent increase in the percentage of annexin V+/propidium iodide+cells. |
Western Blot Analysis[4] | Cell Line: | U266 cells | | Concentration: | 5 μM | | Incubation Time: | 0-24 hours | | Result: | The level of AKT phosphorylation in U266 cells decreased. |
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体内研究
(In Vivo) | Nelfinavir (AG1341) (75 mg/kg; i.p.; 5 days a week for 21 days) decreases multiple myeloma cell growth in NOD/SCID mice[4].
| Animal Model: | NOD/SCID mice (bearing U266-luc cells)[4] | | Dosage: | 75 mg/kg | | Administration: | I.p.; 5 days a week for 21 days | | Result: | Decreased MM cell growth in NOD/SCID mice. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(176.12 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 1.7612 mL | 8.8062 mL | 17.6125 mL | | 5 mM | 0.3522 mL | 1.7612 mL | 3.5225 mL | | 10 mM | 0.1761 mL | 0.8806 mL | 1.7612 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.40 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (4.40 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.40 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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