Duvelisib

Duvelisib is a pivotal pharmaceutical intermediate and certified reference standard in the industrial synthesis of the clinically approved PI3K inhibitor Copiktra®. As the active pharmaceutical ingredient (API) itself, Duvelisib serves as the primary target compound for generic manufacturers and as a reference standard for quality control applications. The isoquinolinone core of Duvelisib is constructed through a multi-step synthetic sequence starting from 2-chloro-6-methyl-N-phenylbenzamide, followed by bromination, substitution, oxidation, cyclization, imidization, and chiral reduction. In quality control contexts, Duvelisib and its impurities—including (S)-3-(1-aminoethyl)-8-chloro-2-phenylisoquinolin-1(2H)-one and various purine-related byproducts—are essential analytical reference standards for impurity profiling, analytical method development, forced degradation studies, and quality control testing for generic manufacturers filing Abbreviated New Drug Applications (ANDA). The unique dual PI3Kδ/γ inhibitory mechanism of Duvelisib has demonstrated therapeutic efficacy in difficult-to-treat hematologic cancers, making this conformationally locked isoquinolinone scaffold a compound of exceptional pharmaceutical importance.

 

 Product Parameters

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Parameter	Specification
Product Name	Duvelisib
CAS Number	1201438-56-3
Molecular Formula	C₂₂H₁₇ClN₆O
Molecular Weight	416.86 g/mol
Appearance	White solid
Melting Point	205-206℃
Boiling Point	757.8±60.0℃
Storage Condition	–20°C

 

Bioactivity

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Duvelisib (IPI-145, INK1197) is a novel selective inhibitor of PI3K δ/γ, with Ki and IC50 values of 23 pM/243 pM and 1 nM/50 nM respectively in cell-free assays, demonstrating higher selectivity for PI3K δ/γ compared to other protein kinases. Phase 3 clinical trial.

 

In Vitro S tudy

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IPI-145 inhibits the proliferation of murine/human B cells with an EC50 of 0.5 nM, and also suppresses human T cell proliferation with an EC50 of 9.5 nM.

 

 In Vivo Studies

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IPI-145 was administered orally to mice and rats at a dose of 10 mg/kg and exhibited favorable pharmacokinetic profiles, with Cmax and AUC values of 390 ng/mL and 137 ng·h/mL, respectively. IPI-145 (10 mg/kg) demonstrated efficacy in the murine delayed-type hypersensitivity (DTH) model, causing approximately 50% ear swelling. IPI-145 (10 mg/kg) showed dose-dependent efficacy in the collagen-induced arthritis (CIA) model in rats, preventing inflammation and protecting both joint bone and cartilage. Additionally, IPI-145 (10 mg/kg, once daily) exhibited therapeutic effects in the adjuvant-induced polyarthritis model in rats.

 

Contact Us

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Securing Duvelisib for your generic API manufacturing campaign, impurity profiling program, or kinase inhibitor research should be straightforward. Cosperpharm makes it simple.