VII-31 是 NEDDylation 通路激活剂，可在体内外抑制肿瘤 。VII-31 还诱导凋亡 (apoptosis)。
| 生物活性 | VII-31 is a potentNEDDylationpathway activator to inhibit the tumor progression in vitro and in vivo. VII-31 inducesapoptosisvia intrinsic and extrinsic pathways[1]. |
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体外研究
(In Vitro) | VII-31 (100 nM, 200 nM; 48 hours) inhibits the cell viability of gastric cell line MGC803 with an IC50of 0.09±0.01 μM. VII-31 also inhibits the cell viability of MCF-7 and PC-3 with IC50s of 0.10±0.006 and 1.15±0.28μM , respectively[1].
VII-31 (50-150 nM; 24 hours) arrests MGC803 cells cycle in G2/M phase[1].
VII-31 (50-150 nM; 48 hours) induces apoptosis via intrinsic and extrinsic pathways[1].
VII-31 (50-150 nM; 24 hours) activates NEDDylation in MGC803 cells[1].
VII-31 (50-150 nM; 48 hours) up-regulates pro-apoptotic proteins FADD, Fasl, PIDD, Bax, Bad; while down-regulates anti-apoptotic proteins Bcl-xL, Bcl-2, XIAP, c-IAP1[1].
Cell Viability Assay[1] | Cell Line: | Gastric cancer MGC803 cells | | Concentration: | 100, 200 nM | | Incubation Time: | 48 hours | | Result: | Inhibited the cell viability in dose-depend manner. |
Cell Cycle Analysis[1] | Cell Line: | MGC803 cells | | Concentration: | 50, 100, 150 nM | | Incubation Time: | 24 hours | | Result: | Arrested cells in G2/M phase, and a clear sub-G1 peak was observed in the high dose group. |
Apoptosis Analysis[1] | Cell Line: | MGC803 cells | | Concentration: | 50, 75, 100, and 150 nM | | Incubation Time: | 48 hours | | Result: | High dose (150 nM) treatment significantly elevated the early and late apoptosis rate to 92.8% from 4.8%. |
Western Blot Analysis[1] | Cell Line: | MGC803 cells | | Concentration: | 50, 100, 150 nM | | Incubation Time: | 24 hours | | Result: | Resulted in NEDDylation activation of MGC803 cells, the NEDDylation of 3 important proteins NAE1, Ubc12 and CUL1 has been activated. |
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体内研究
(In Vivo) | VII-31 inhibits the tumor progression in vivo, while showing no obvious toxicity to mice[1].
| Animal Model: | Mice bearing MGC803 xenograft tumors[1] | | Dosage: | 50, 100, 150 mg/kg | | Administration: | Subcutaneous injection; daily for 28 days | | Result: | The mice had a much smaller tumor compared with vehicle control. The tumor volumes of middle/high dose treated mice at certain time points were evidently decreased comparing with untreated group. |
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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 : 250 mg/mL(584.78 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.3391 mL | 11.6956 mL | 23.3913 mL | | 5 mM | 0.4678 mL | 2.3391 mL | 4.6783 mL | | 10 mM | 0.2339 mL | 1.1696 mL | 2.3391 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: ≥ 2.08 mg/mL (4.87 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.87 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 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% (20%SBE-β-CDin saline) Solubility: 2.08 mg/mL (4.87 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (4.87 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (4.87 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.87 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 20.8 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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