
化学名称 : CUDC-101
CAS : 1012054-59-9
英文名称: CUDC-101
英文同义词: 7-[[4-(3-Ethynylphenylamino)-7-methoxyquinazolin-6-yl]oxy]-N-hydroxyheptanamide
溶解度:DMSO
储存条件:at -20℃ 2 years
生物活性
CUDC-101 is a drug which displays potent in vitro inhibitory activity against HDAC, EGFR, and HER2 with an IC50 of 4.4, 2.4, and 15.7 nM, respectively. [1] This drug has novel structure incorporating HDAC inhibitory functionality into the pharmacophore of the EGFR and HER2 inhibitors. [1]In most tumor cell lines tested, CUDC-101 exhibits efficient antiproliferative activity with greater potency than vorinostat (SAHA), erlotinib, lapatinib, and combinations of vorinostat/erlotinib and vorinostat/lapatinib. [2]In vivo, CUDC-101 promotes tumor regression or inhibition in various cancer xenograft models including nonsmall cell lung cancer (NSCLC), liver, breast, head and neck, colon, and pancreatic cancers. [2]
参考文献
[1] Cai X, et al . J Med Chem. 2010 Mar 11;53(5):2000-9.
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