Application
一种有效、选择性和口服有效的组蛋白脱乙酰酶（HDAC）抑制剂，具有潜在的抗肿瘤活性,抑制HDAC6和HDAC3, IC50值分别为4nM and 76nM。
Citarinostat is a potent, selective and orally available histone deacetylase (HDAC) inhibitor, with potential antineoplastic activity. Upon oral administration, ACY-241 inhibits the activity of HDACs; this results in an accumulation of highly acetylated chromatin histones, the induction of chromatin remodeling and an altered pattern of gene expression. This leads to the inhibition of tumor oncogene transcription, and the selective transcription of tumor suppressor genes, which inhibit tumor cell division and induce tumor cell apoptosis。
Citarinostat是一种有效的，选择性的且可口服的组蛋白脱乙酰基酶（HDAC）抑制剂，具有潜在的抗肿瘤活性。 口服后，ACY-241会抑制HDAC的活性。 这导致高度乙酰化的染色质组蛋白的积累，染色质重塑的诱导和基因表达模式的改变。 这导致对肿瘤癌基因转录的抑制，以及对肿瘤抑制基因的选择性转录，从而抑制肿瘤细胞分裂并诱导肿瘤细胞凋亡。
性质
| Iupac Name | 2-((2-chlorophenyl)(phenyl)amino)-N-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide |
| Inchi Code | 1S/C24H26ClN5O3/c25-20-12-7-8-13-21(20)30(19-10-4-3-5-11-19)24-27-16-18(17-28-24)23(32)26-15-9-2-1-6-14-22(31)29-33/h3-5,7-8,10-13,16-17,33H,1-2,6,9,14-15H2,(H,26,32)(H,29,31) |
| Inchi Key | VLIUIBXPEDFJRF-UHFFFAOYSA-N |
安全信息
RIDADR NONH for all modes of transport
