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IPI-145

(CAS No:1201438-56-3)

Duvelisib (IPI-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 in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3.

CAS No:1201438-56-3

Molecular Weight(MW):416.86

Purity:99.00%

Specification:500MG;1G;5G;10G;50G;100G

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COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	1201438-56-3
Molecular formula(MF)	C₂₂H₁₇ClN₆O
Molecular Weight(MW):	416.86
Alias	IPI 145;IPI-145;IPI-145 (INK-1197);8-Chloro-2-phenyl-3-[(1S)-1-(9H-purin-6-ylamino)ethyl]-1(2H)-isoquinolinone;Duvelisib;Duvelisib (IPI-145, INK1197);1(2H)-Isoquinolinone, 8-chloro-2-phenyl-3-[(1S)-1-(9H-purin-6-ylamino)ethyl]-;8-Chloro-2-phenyl-3-[(1S)-1-(9H-purin-6-ylamino)ethyl]-1(2H)-isoquinolinone Duvelisib (IPI-145, INK1197)

Solubility

In vitro	DMSO	83 mg/mL (199.1 mM)
	Water	<1 mg/mL
	Ethanol	<1 mg/mL
In vivo	30% PEG400+0.5% Tween80+5% propylene glycol	30 mg/mL

Biological Activity

Description

Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with K_i and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3.

Targets

PI3Kδ ^[1] (Cell-free assay)	PI3Kγ ^[1] (Cell-free assay)	PI3Kδ ^[1] (Cell-free assay)	PI3Kβ ^[1] (Cell-free assay)	PI3Kα ^[1] (Cell-free assay)	View More
23 pM(Ki)	243 pM(Ki)	23 pM(Ki)	1564 pM(Ki)	25900 pM(Ki)	View More

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 C_max 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]