CUDC-101

• Description :

  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.

• 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

• CAS Number :

  [1012054-59-9]