CUDC-101
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
CUDC-101是组蛋白去乙酰化酶的多靶点抑制剂,直接抑制表皮生长因子受体(EGFR)和HER2,以及I类和II类HDACs。据报道,在体外和体内异种移植模型中,CUDC-101能够有效抑制广泛的肿瘤类型的发展,包括lapatinib和erlotinib耐受的癌细胞系。机制研究表明,CUDC-101不仅直接抑制EGFR和HER2信号,还间接衰减Akt、 HER3和MET信号通路。
参考文献:
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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 434.49 |
Cas No. | 1012054-59-9 |
Formula | C24H26N4O4 |
Synonyms | CUDC101, CUDC 101 |
Solubility | ≥21.7 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | 7-[4-(3-ethynylanilino)-7-methoxyquinazolin-6-yl]oxy-N-hydroxyheptanamide |
SDF | Download SDF |
Canonical SMILES | COC1=C(C=C2C(=C1)N=CN=C2NC3=CC=CC(=C3)C#C)OCCCCCCC(=O)NO |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
MDA-MB-231细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月 |
反应条件 |
1 ?M,16h |
实验结果 |
在MDA-MB-231人乳腺癌细胞中,1 μM CUDC-101显著降低HGF和EGF诱导的迁移。迁移和侵袭的抑制不是细胞死亡或生长抑制的次要效应,因为在所有测试条件下没有检测到细胞活力的显著降低。 |
动物实验[2]: | |
动物模型 |
携带人HepG2肝癌细胞异种移植物的4至6周龄雌性无胸腺小鼠(nude nu/nu CD-1) |
剂量 |
在肿瘤达到平均大小为281 mm3之后,用120 mg/kg日剂量的CUDC-101口服治疗小鼠。 |
实验结果 |
CUDC-101诱导30%肿瘤消退。CUDC-101处理的其中一只小鼠在给药周期结束时肿瘤完全消退,治疗后产生至少6个月的持续效果。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
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. |
描述 | CUDC-101是一种有效的HDAC、EGFR和HER2抑制剂,IC50值分别为4.4 nM、2.4 nM和15.7 nM。 | |||||
靶点 | EGFR | HDAC | HDAC1 | HDAC6 | HDAC3 | HDAC5 |
IC50 | 2.4 nM | 4.4 nM | 4.5 nM | 5.1 nM | 9.1 nM | 11.4 nM |
质量控制和MSDS
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