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.
Name | IPI-145 (INK1197) |
Synonym | IPI-145, INK1197, IPI145, IPI 145, INK-1197, INK 1197 |
CAS NO. | 1201438-56-3 |
Chemical Formula | C22H17ClN6O |
MW | 416.86 |
Purity | >98% |
Solubility(R.T.: 25℃) | DMSO |
Stability |
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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/γin 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].