溶解性 | DMSO ≥78mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
存贮条件 | 储存温度-20°C |
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 |