Duvelisib (IPI-145)

Catalog No.S7028 Batch:S702803

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Technical Data

Formula

C22H17ClN6O
Molecular Weight 416.86 CAS No. 1201438-56-3
Solubility (25°C)* In vitro DMSO 83 mg/mL (199.1 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
30%PEG400 0.5%Tween80 5%propylene glycol
30.0mg/ml Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description 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.
Targets
PI3Kδ [1]
(Cell-free assay)		 PI3Kβ [1]
(Cell-free assay)		 PI3Kγ [1]
(Cell-free assay)
23 pM(Ki) 1564 pM(Ki) 243 pM(Ki)
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]

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    AML cell lines

  • Concentrations

    10 μM

  • Incubation Time

    72 h

  • Method

    AML cell lines were treated with 10 μM IPI-145 and cultured for 72 hours.
Animal Study:

[3]
  • Animal Models

    Brown Norway rats

  • Dosages

    (0.1, 0.3, 1, or 10 mg/kg

  • Administration

    p.o.

Customer Product Validation

, , Dr. Antonino Maria Spartà from University of Bolog

Data from [Data independently produced by , , Leukemia, 2018, 32(9):1958-1969]

Data from [Data independently produced by , , Blood Cancer J, 2017, 7(3):e539]

Data from [Data independently produced by , , PLoS One, 2016, 11(12):e0169230.]

Selleck's Duvelisib (IPI-145) has been cited by 51 publications

Genomic and transcriptomic profiling of peripheral T cell lymphoma reveals distinct molecular and microenvironment subtypes [ Cell Rep Med, 2024, 5(2):101416] PubMed: 38350451
A molecular circuit linking the BCR to the NAD biosynthetic enzyme NAMPT is an actionable target in Richter syndrome [ Blood Adv, 2024, 8(8):1920-1933] PubMed: 38359376
Dual inhibition of phosphoinositide 3-kinases delta and gamma reduces chronic B cell activation and autoantibody production in a mouse model of lupus [ Front Immunol, 2023, 14:1115244] PubMed: 37234154
Selective Inhibition of PI3K Isoforms in Brain Tumors Suppresses Tumor Growth by Increasing Radiosensitivity [ Yonsei Med J, 2023, 64(2):139-147] PubMed: 36719022
Targetable leukemia dependency on noncanonical PI3Kγ signaling [ bioRxiv, 2023, 10.1101/2023.12.15.571909] PubMed: none
Proteogenomics refines the molecular classification of chronic lymphocytic leukemia [ Nat Commun, 2022, 13(1):6226] PubMed: 36266272
Proteogenomics refines the molecular classification of chronic lymphocytic leukemia [ Nat Commun, 2022, 13(1):6226] PubMed: 36266272
Functional Testing to Characterize and Stratify PI3K Inhibitor Responses in Chronic Lymphocytic Leukemia [ Clin Cancer Res, 2022, 28-20:4444-4455] PubMed: 35998013
Resistance to PI3κδ inhibitors in marginal zone lymphoma can be reverted by targeting the IL-6/PDGFRA axis [ Haematologica, 2022, 10.3324/haematol.2021.279957] PubMed: 35484662
PI3K Isoform-Specific Regulation of Leader and Follower Cell Function for Collective Migration and Proliferation in Response to Injury [ Cells, 2022, 11(21)3515] PubMed: 36359913

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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