VII-31

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VII-31  纯度: 98.28%

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)。

VII-31

VII-31 Chemical Structure

CAS No. : 2305757-96-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3300 In-stock
5 mg ￥3000 In-stock
10 mg ￥4800 In-stock
25 mg ￥9000 In-stock
50 mg ￥13500 In-stock
100 mg ￥20000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

VII-31 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Oxygen Sensing Compound Library
  • Ubiquitination Compound Library

生物活性

VII-31 is a potent NEDDylation pathway activator to inhibit the tumor progression in vitro and in vivo. VII-31 induces apoptosis via intrinsic and extrinsic pathways[1].

IC50 & Target

NEDDylation[1]
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 IC50 of 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

VII-31 inhibits the tumor progression in vivo, while showing no obvious toxicity to mice[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

427.51

Formula

C23H25NO5S
CAS 号

2305757-96-2
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
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (584.78 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 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 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Dong-Jun Fu, et al. Discovery of Novel Tertiary Amide Derivatives as NEDDylation Pathway Activators to Inhibit the Tumor Progression in Vitro and in Vivo. Eur J Med Chem. 2020 Apr 15;192:112153.

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