Nur77 modulator 1|cas:2469975-55-9|西域试剂

Nur77 modulator 1,98.23%

产品编号：Bellancom-131364| CAS NO：2469975-55-9| 分子式：C₂₈H₂₅N₅O₂S| 分子量：495.60

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货号	价格	库存与货期
Bellancom-131364	￥3500.00	杭州北京（现货）
Bellancom-131364	￥5800.00	杭州北京（现货）
Bellancom-131364	￥11000.00	杭州北京（现货）
Bellancom-131364	￥17000.00	杭州北京（现货）
Bellancom-131364	￥25000.00	杭州北京（现货）

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Nur77 modulator 1

产品介绍

Nur77 modulator 1 可结合到Nur77 (K_D = 3.58 μM)。Nur77 modulator 1 上调 Nur77 表达，介导Nur77亚细胞定位，诱导Nur77 依赖的内质网应激和自噬，可导致细胞凋亡。抗肝癌生物活性。

生物活性

Nur77 modulator 1 is a good Nur77 binder (K_D = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity.

体外研究

Nur77 modulator 1 (10g, 0-20 μM) displays potent and broad-spectrum antiproliferative activity against all tested three hepatoma cell lines (HepG2, QGY-7703, and SMMC-7721), and less cytotoxicity against LO2 cells (human normal liver cell line).
Nur77 modulator 1 (10g, ) could specifically up-regulate the expression of Nur77 in a dose-dependent manner.
Nur77 modulator 1 (10g, 2.0 μM) induces Nur77-dependent apoptosis.
Nur77 modulator 1 (10g, 2.0 μM) increased LC3-II and Beclin1 protein levels in a dose-dependent manner (10g treatment does not enhance p62 degradation, indicating that autophagy induced by 10g is incomplete).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay.

Cell Line:	Liver cancer cell lines (HepG2, QGY-7703, and SMMC-7721).
Concentration:	0-20 μM.
Incubation Time:	12-24 hours.
Result:	Exhibited IC₅₀ values of 0.6 µM, 0.89 µM, 1.40 µM and >20 µM in HepG2, QGY-7703, SMMC-7721 and LO2 cells, respectively. Reduced the viability in a time-dependent manner. Induced cell morphology alteration, such as cell shrinkage, vesicles accumulated, and reduced cell number.

体内研究
(In Vivo)

Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude mouse hepatoma HepG2 xenograft.
Dosage:	10 and 20 mg/kg/day.
Administration:	IP, once every day for 15 days.
Result:	Lead to substantial suppression of tumor growth. The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively. Exhibited almost no influence on the body weight of experimental mice.

体内研究

Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude mouse hepatoma HepG2 xenograft.
Dosage:	10 and 20 mg/kg/day.
Administration:	IP, once every day for 15 days.
Result:	Lead to substantial suppression of tumor growth. The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively. Exhibited almost no influence on the body weight of experimental mice.

体内研究

Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude mouse hepatoma HepG2 xenograft.
Dosage:	10 and 20 mg/kg/day.
Administration:	IP, once every day for 15 days.
Result:	Lead to substantial suppression of tumor growth. The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively. Exhibited almost no influence on the body weight of experimental mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (252.22 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0178 mL	10.0888 mL	20.1776 mL
5 mM	0.4036 mL	2.0178 mL	4.0355 mL
10 mM	0.2018 mL	1.0089 mL	2.0178 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 (protect from light)。-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 90% (20% SBE-β-CD in saline)
Solubility: 2.08 mg/mL (4.20 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.20 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.20 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.20 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。