| 应用 |
A potent inhibitor of HDACs and receptor tyrosine kinases |
| 产品介绍 |
CUDC-101是HDAC，EGFR和HER2抑制剂，IC50分别为4.4，2.4和15.7 nM。 |
| 备注 |
CUDC-101 is a potent multi-targeted inhibitor against HDAC, EGFR and HER2 with IC50 of 4.4 nM, 2.4 nM, and 15.7 nM, and inhibits class I/II HDACs, but not class III, Sir-type HDACs. Phase 1. |
| 生化机理 |
CUDC-101 inhibits the erlotinib-resistant EGFR mutant T790M although its effects are incomplete with an Amax of ~60% of peak enzyme activity after inhibition. CUDC-101 treatment increases the acetylation of histone H3 and H4, as well as the acetylation of non-histone substrates of HDAC such as p53 and α-tubulin, in a dose-dependant manner in various cancer cell lines. CUDC-101 also suppresses HER3 expression, Met amplification, and AKT reactivation in tumor cells. |
| 别名 |
7-((4-(3-乙炔基苯基氨基)-7-甲氧基喹唑啉-6-基)氧基)-N-羟基庚酰胺;;CUDC101;CUDC 101;7-((4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yl)oxy)-n-hydroxyheptanamide |
