A multi-target inhibitor that potently blocks EGFR and HER2 (IC50s = 2.4 and 16.4 nM

CUDC-101 – 50 mg

Brand:
Cayman
CAS:
1012054-59-9
Storage:
-20
UN-No:
Non-Hazardous - /

CUDC-101 is a multi-target inhibitor, combining functional groups of potent inhibitors of human epidermal growth factor receptor (HER) kinases and histone deacetylases (HDACs). It potently blocks the receptor tyrosine kinases EGFR (aka HER1) and HER2 (IC50s = 2.4 and 16.4 nM, respectively).{26830} CUDC-101 also inhibits the activity of class I and class II HDACs at nanomolar concentrations (e.g., IC50s = 4.5, 12.6, 13.2, and 11.4 nM for HDAC1, 2, 4, and 5, respectively).{26830} It has only weak effects on over 60 other kinases when tested at 5 µM.{26830} CUDC-101 prevents the growth of a wide range of cancer cell lines in vitro, and slows tumor growth or induces tumor regression through cancer cell apoptosis in xenograft models.{26830} In cancer cells that have acquired resistance to single-target EGFR inhibitors, CUDC-101 blocks proliferation and reduces cell migration.{26829}  

 

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Description

A multi-target inhibitor that potently blocks EGFR and HER2 (IC50s = 2.4 and 16.4 nM, respectively) and inhibits the activity of class I and class II HDACs at nanomolar concentrations (e.g., IC50s = 4.5, 12.6, 13.2, and 11.4 nM for HDAC1, 2, 4, and 5, respectively)

Formal name: 7-[[4-[(3-ethynylphenyl)amino]-7-methoxy-6-quinazolinyl]oxy]-N-hydroxy-heptanamide

Synonyms: 

Molecular weight: 434.5

CAS: 1012054-59-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Activators|Deacetylases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Epigenetics, Transcription, & Translation|Erasers|Histone Deacetylation

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