CUDC-101

目录号: GC16008纯度: >99.00%同义词: 7-[[4-(3-乙炔基苯基氨基)-7-甲氧基喹唑啉-6-基]氧基]-N-羟基庚酰胺,CUDC101, CUDC 101
A multi-target inhibitor of HDACs, EGFR, and HER2

CUDC-101
Cas No.: 1012054-59-9
规格价格库存数量操作
10mg¥557.00现货
1
50mg¥2,195.00现货
1
200mg¥6,027.00现货
1
10mM (in 1mL DMSO)¥651.00现货
1

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产品描述 Description

CUDC-101 is a multitargeted inhibitor of histone deacetylase. It is designed to directly inhibit epidermal growth factor receptor (EGFR) and HER2 as well as class I and class II HDACs. It has been shown that CUDC-101 is able to effectively suppress the progression of a broad range of tumor types in both in vitro and in vivo xenograft models, including lapatinib- and erlotinib-resistant cancer cell lines. Mechanistic studies provide the evidence that CUDC-101 not only directly inhibits both EGFR and HER2 signaling but also indirectly attenuates the survival signaling pathways Akt, HER3, and MET.

Reference

[1].Cheng-Jung Lai, Rudi Bao, Xu Tao, Jing Wang, Ruzanna Atoyan, Hui Qu, Da-Gong Wang, Ling Yin, Maria Samson, Jeffrey Forrester, Brian Zifcak, Guang-Xin Xu, Steven DellaRocca, Hai-Xiao Zhai, Xiong Cai, William E. Munger, Mitchell Keegan, Carmen V. Pepicelli, and Changgeng Qian. CUDC-101, a Multitargeted Inhibitor of Histone Deacetylase, Epidermal Growth Factor Receptor, and Human Epidermal Growth Factor Receptor 2, Exerts Potent Anticancer Activity. Cancer Res May 1, 2010 70; 3647.

实验参考方法 Experimental Reference Method

Cell experiment: [1]

Cell lines

MDA-MB-231 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

1 µM, 16h.

Applications

MDA-MB-231 human breast carcinoma cells showed that HGF- and EGF-induced migration was significantly reduced by 1 µM CUDC-101. The inhibition of migration and invasion was not a secondary effect of cell death or growth inhibition, as no significant decrease in cell viability under all conditions tested has been detected.

Animal experiment : [2]

Animal models

four-to 6-week-old female athymic mice (nude nu/nu CD-1) bearing human HepG2 liver cancer cell xenografts

Dosage form

After tumors reached an average of 281 mm3 in size, mice were orally treated with CUDC-101 at a daily dose of 120 mg/kg.

Applications

CUDC-101 induced 30% tumor regression. One of the treated mice displayed complete tumor regression at the end of the dosing cycle, an effect that lasted for at least 6 months after treatment.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Wang J, Pursell N W, Samson M E S, et al. Potential advantages of CUDC-101, a multitargeted HDAC, EGFR, and HER2 inhibitor, in treating drug resistance and preventing cancer cell migration and invasion. Molecular cancer therapeutics, 2013, 12(6): 925-936.

[2] Lai C J, Bao R, Tao X U, et al. CUDC-101, a multitargeted inhibitor of histone deacetylase, epidermal growth factor receptor, and human epidermal growth factor receptor 2, exerts potent anticancer activity. Cancer research, 2010, 70(9): 3647-3656.

产品文档 Product Documents

Purity:>99.00%

化学性质Chemical Properties

CAS 号
1012054-59-9
同义词
7-[[4-(3-乙炔基苯基氨基)-7-甲氧基喹唑啉-6-基]氧基]-N-羟基庚酰胺,CUDC101, CUDC 101
化学名
7-[4-(3-ethynylanilino)-7-methoxyquinazolin-6-yl]oxy-N-hydroxyheptanamide
SMILES
COC1=C(C=C2C(=C1)N=CN=C2NC3=CC=CC(=C3)C#C)OCCCCCCC(=O)NO
分子式
C24H26N4O4
分子量
434.49 g/mol
溶解性
≥ 21.7 mg/mL in DMSO
保存条件
Store at -20°C
General tips
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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol