A4092-200mg | CUDC-101 [1012054-59-9] Biotrend

Background

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

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.

Product Citation

1. Bagnall NH, Hines BM, et al. "Insecticidal activities of histone deacetylase inhibitors against a dipteran parasite of sheep, Lucilia cuprina." Int J Parasitol Drugs Drug Resist. 2017 Apr;7(1):51-60. PMID:28110187

Chemical Properties

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
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

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.

Biological Activity

Description	CUDC-101 is a potent inhibitor of HDAC, EGFR and HER2 with IC50 values of 4.4 nM, 2.4 nM, and 15.7 nM, respectively.
Targets	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