IPI-145

Availability: In Stock
Biological Description:
PI-145 (INK1197) is a novel and selective PI3K δ/γ inhibitor with Ki and IC50 of 23 pM/243 pM and 1 nM/50 nM, highly selective for PI3K δ/γ than other protein kinases.
IC50 value: 1 nM/50 nM (PI3K δ/γ) [1]
Target: PI3K δ/γ
in vitro: 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 [1].
in vivo: IPI-145 (10 mg/kg, p.o.) shows well pharmacokinetics with Cmax and AUC of 390 ng/mL and 137 ng?h/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 [1].

Purity: >98%

Molecular formula: C₂₂H₁₇ClN₆O

Molecular Weight: 416.86

Storage Instructions: Two years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO