CAS NO: | 209783-80-2 |
规格: | 98% |
分子量: | 376.4 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
Background:
Entinostat (also known as MS-275 or SNDX-275), a derivative of 2-aminophenyl benzamides, is a potent and orally-available inhibitor of histone deacetylases (HDACs), a family of enzymes associated with a variety of well-characterized cellular oncogenes and tumor suppressors, that potently inhibits class I HDACs, including HDAC1, HDAC3 and HDAC8, with values of 50% inhibition concentration IC50of 0.368 μM, 0.501 μM and 63.4 μM respectively. Entinostat has been widely investigated for the treatment of cancer, in which results have shown the in vitro anti-proliferative activity of entinostat in a wide range of human cancer cell lines, including breast, colon, lung, myeloma, ovary, pancreas, prostate and leukemia.
Reference
Hess-Stumpp H, Bracker TU, Henderson D, Politz O. MS-275, a potent orally available inhibitor of histone deacetylases--the development of an anticancer agent. Int J Biochem Cell Biol. 2007;39(7-8):1388-405. Epub 2007 Feb 16.
Hess-Stumpp H. Histone deacetylase inhibitors and cancer: from cell biology to the clinic. Eur J Cell Biol. 2005 Mar;84(2-3):109-21.