Belinostat (PXD101)

属性

溶解性	DMSO 64 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
存贮条件	储存温度-20°C

描述

应用	一种新型HDAC抑制剂
产品介绍	Belinostat (PXD101)是一种新型的HDAC抑制剂，IC50为27 nM，对抵抗Cisplatin的肿瘤有效。
备注	Belinostat (PXD101) is a novel HDAC inhibitor with IC50 of 27 nM, with activity demonstrated in cisplatin-resistant tumors. Phase 1/2.
生化机理	Belinostat (PXD101) is a novel HDAC inhibitor with IC50 of 27 nM. Belinostat inhibits the growth of tumor cells (A2780, HCT116, HT29, WIL, CALU-3, MCF7, PC3 and HS852) with IC50 from 0.2-0.66 μM. PD101 shows low activity in A2780/cp70 and 2780AD cells. Belinostat inhibits bladder cancer cell growth, especially in 5637 cells, which shows accumulation of G0-G1 phase, decrease in S phase, and increase in G2-M phase. Belinostat also shows enhanced tubulin acetylation in ovarian cancer cell lines. A recent study shows that Belinostat activates protein kinase A in a TGF-β signaling-dependent mechanism and decreases survivin mRNA.
别名	N-羟基-3-(3-苯基氨基磺酰基苯基)丙烯酰胺;PXD101;PX105684;PXD-101;PXD 101;PX-105684;N-Hydroxy-3-(3-phenylsulfamoylphenyl)acrylamide;(2E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]acrylamide