| 应用 |
An HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 inhibitor. |
| 产品介绍 |
PCI-24781 (Abexinostat)是一种新型的pan-HDAC抑制剂，靶向作用于HDAC1，Ki为7 nM，对HDACs 2， 3， 6，和10有适中的抑制性，但比作用于HDAC8选择性强40倍。 |
| 备注 |
PCI-24781 is a novel pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM, modest potent to HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Phase 1/2. |
| 生化机理 |
PCI-24781 is a broad spectrum hydroxamic acid-based inhibitor of HDAC that shows antitumor activity in vitro. PCI-24781 inhibited pure recombinant HDAC1 with a Ki of 0.007 Mmol/L, as well as HDAC2, HDAC3/SMRT, HDAC6, HDAC8, and HDAC10 in the nanomolar range. Antitumor activity of PCI-24781 was observed in all 10 tumor cell lines tested, with GI50% values ranging from 0.15 to 3.09 μmol/L. |
| 别名 |
PCI 24781; 3-[(二甲基氨基)甲基]-N-[2-[4-[(羟基氨基)羰基]苯氧基]乙基]-2-苯并呋喃甲酰胺;CRA 024781; CRA 24781; PCI 24781; Abexinostat;3-[(Dimethylamino)methyl]-N-[2-[4-[(hydroxyamino)carbonyl]phenoxy]ethyl]-2-benzofurancarboxamide |
