CUDC-101
Dual HDAC and EGFR inhibitor / A novel hybrid dual-acting HDAC and receptor tyrosine kinase inhibitor. It is a potent HDAC inhibitor which also inhibits EGFR and HER2, IC50 = 4.4, 2.4 and 15.7 nM respectively.1 It not only blocks EGFR and HER2 but also attenuates multiple compensatory pathways such as AKT, HER3 and MET which enable tumor cells to escape the effects of conventional EGFR/HER2 inhibitors.1,2
Biochemicals & reagents
1012054-59-9
1) Lai et al. (2010), CUDC-101, a multitargeted inhibitor of histone deacetylase, epidermal growth factor receptor, and human epidermal growth factor receptor 2, exerts potential anticancer activity; Cancer Res., 70 3647 2) Cai et al. (2010), 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., 53 2000
-20°C
TARGET: Kinase; Protein deacetylase -- PATHWAY: AKT; Chromatin; Posttranslational modification -- RESEARCH AREA: Epigenetics -- DISEASE AREA: Cancer