Duvelisib (IPI-145, INK1197)

属性

溶解性	DMSO 84 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
存贮条件	储存温度-20°C

描述

产品介绍	Duvelisib (IPI-145) 是PI3K δ和γ高度选择性抑制剂, Ki和IC50分别为23 pM/243 pM和1 nM/50 nM。
生化机理	IPI-145 suppresses murine/human B-cell proliferation with EC50 of 0.5 nM/0.5 nM and also inhibits human T-cell proliferation with EC50 of 9.5 nM . IPI-145 (10 mg/kg, p.o.) shows well pharmacokinetics with Cmax and AUC of 390 ng/mL and 137 ng/mL in mouse and rat. IPI-145 (10 mg/kg) is active in murine DTH model with ~50% ear swelling. IPI-145 (10 mg/kg) demonstrates dose-dependent effect in rat collagen induced arthritis (CIA) model. IPI-145 prevents inflammation and protects joint bone and cartilage in the rat CIA model. IPI-145 (10 mg/kg,QD) demonstrates activity in rat adjuvant induced polyarthritis model.
别名	IPI 145; IPI145; INK 1197; INK-1197; 8-chloro-2-phenyl-3-((1s)-1-(9h-purin-6-ylamino)ethyl)-1(2h)-isoquinolinone