VII-31 - CAS:2305757-96-2

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VII-31

目录号 : KM10328 CAS No. : 2305757-96-2 纯度 : 98%

Data Sheet 产品使用指南

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)。

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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.

体外研究

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.
VII-31 (50-150 nM; 24 hours) arrests MGC803 cells cycle in G2/M phase.
VII-31 (50-150 nM; 48 hours) induces apoptosis via intrinsic and extrinsic pathways.
VII-31 (50-150 nM; 24 hours) activates NEDDylation in MGC803 cells.
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.

Cell Viability Assay

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

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

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

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

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

Animal Model:	Mice bearing MGC803 xenograft tumors
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.

分子式

C₂₃H₂₅NO₅S

分子量

427.51

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。
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。
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。