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CUDC-101

CUDC-101 is a potent inhibitor of HDAC, EGFR, and HER2 with IC50s of 4.4, 2.4, and 15.7 nM, respectively. CUDC-101 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Product Specifications

CAS Number

1012054-59-9

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

EGFR; HDAC

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/CUDC-101.html

Purity

99.05

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

C#CC1=CC=CC(NC2=NC=NC3=CC(OC)=C(C=C23)OCCCCCCC(NO)=O)=C1

Molecular Formula

C24H26N4O4

Molecular Weight

434.49

Precautions

H302, H315, H319, H335

References & Citations

[1]Xiong Cai et al Discovery of 7- (4- (3-Ethynylphenylamino) -7-methoxyquinazolin-6-yloxy) -N-hydroxyheptanamide (CUDC-101) as a Potent Multi-Acting HDAC, EGFR, and HER2 Inhibitor for the Treatment of Cancer J. Med. Chem., 2010, 53 (5), pp 2000–2009|[2]Sun H, et al. CUDC-101, a Novel Inhibitor of Full-Length Androgen Receptor (flAR) and Androgen Receptor Variant 7 (AR-V7) Activity: Mechanism of Action and In Vivo Efficacy. Horm Cancer. 2016 Jun;7 (3) :196-210.|[3]Zhang L, et al. Dual inhibition of HDAC and EGFR signaling with CUDC-101 induces potent suppression of tumor growth and metastasis in anaplastic thyroid cancer. Oncotarget. 2015 Apr 20;6 (11) :9073-85.|[4]Lai CJ, 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 Res. 2010 May 1;70 (9) :3647-56. Epub 2010 Apr 13.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

Phase 1

Isoform

EGFR/ErbB1/HER1; ErbB2/HER2; HDAC; HDAC1; HDAC10; HDAC2; HDAC3; HDAC4; HDAC5; HDAC6; HDAC7; HDAC8; HDAC9

Available Sizes

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