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Nur77 modulator 1

产品编号 T40130 CAS 2469975-55-9

别名: Nur77 modulator 1

Nur77 modulator 1 可与Nur77结合，KD 为 3.58 μM。它上调 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，Nur77 modulator 1显示出抗肝癌生物活性。

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Nur77 modulator 1, CAS 2469975-55-9

规格	价格/CNY	货期
1 mg	￥ 1,160	现货
5 mg	￥ 2,860	现货
10 mg	￥ 4,230	现货
25 mg	￥ 6,780	现货
50 mg	￥ 9,180	现货
100 mg	￥ 12,300	现货
500 mg	￥ 24,800	现货
1 mL * 10 mM (in DMSO)	￥ 2,950	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Nur77 modulator 1 is a good Nur77 binder (KD = 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. Nur77 modulator 1 shows anti-hepatoma activity.
靶点活性	Nur77:3.58 μM (KD)
体外活性	Nur77 modulator 1 (10g, 0-20 μM) displays potent and broad-spectrum antiproliferative activity against all tested three hepatoma cell lines which are HepG2, QGY-7703, and SMMC-7721 respectively, and less cytotoxicity against LO2 cells (human normal liver cell line) [1]. Nur77 modulator 1 (10g, ) could specifically up-regulate the expression of Nur77 in a dose-dependent manner [1]. Nur77 modulator 1 (10g, 2.0 μM) induces Nur77-dependent apoptosis [1] . 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) [1] . Cell Viability Assay [1] . Cell Line: Liver cancer cell lines (HepG2, QGY-7703, and SMMC-7721). Concentration: 0-20 μM. Incubation Time: 12-24 hours. Result: Exhibited IC 50 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.
体内活性	Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability [1]. Animal Model: Nude mouse hepatoma HepG2 xenograft [1]. 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. These results indicate that Nur77 modulator 1 has the potential to be developed as a novel Nur77-targeting anti-hepatoma drug.

别名	Nur77 modulator 1
分子量	495.6
分子式	C28H25N5O2S
CAS No.	2469975-55-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 125 mg/mL (252.22 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0178 mL	10.0888 mL	20.1776 mL	50.4439 mL
	5 mM	0.4036 mL	2.0178 mL	4.0355 mL	10.0888 mL
	10 mM	0.2018 mL	1.0089 mL	2.0178 mL	5.0444 mL
	20 mM	0.1009 mL	0.5044 mL	1.0089 mL	2.5222 mL
	50 mM	0.0404 mL	0.2018 mL	0.4036 mL	1.0089 mL
	100 mM	0.0202 mL	0.1009 mL	0.2018 mL	0.5044 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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参考文献

1. Baicun Li, et al. Design, synthesis, and biological evaluation of 5-((8-methoxy-2-methylquinolin-4-yl)amino)-1H-indole-2-carbohydrazide derivatives as novel Nur77 modulators. Eur J Med Chem. 2020 Oct 15;204:112608.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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