Duvelisib (IPI-145, INK1197)

Catalog No.S7028

Duvelisib (IPI-145, INK1197) Chemical Structure

Molecular Weight(MW): 416.86

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.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 170 In stock
USD 970 In stock

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1 Customer Review

  • PI3K inhibitor IPI-145 demonstrated to be effective on ALL-SIL cells,showed an IC50 in the lower micromolar range.

    Dr. Antonino Maria Spartà from University of Bolog. Duvelisib (IPI-145, INK1197) purchased from Selleck.

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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

Solubility (25°C)

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

* 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.

Chemical Information

Molecular Weight 416.86
Formula

C22H17ClN6O

CAS No. 1201438-56-3
Storage powder
in solvent
Synonyms N/A

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Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02292225 Recruiting Lymphocytic Leukemia, Chronic|Lymphoma, Small Lymphocytic Infinity Pharmaceuticals, Inc. February 2015 Phase 1
NCT02391545 Recruiting CD20+ Follicular Lymphoma Infinity Pharmaceuticals, Inc. December 2014 Phase 1|Phase 2
NCT02307461 Completed Healthy Infinity Pharmaceuticals, Inc. November 2014 Phase 1
NCT02204982 Active, not recruiting Follicular Lymphoma Infinity Pharmaceuticals, Inc. September 2014 Phase 3
NCT02158091 Recruiting Chronic Lymphocytic Leukemia Dana-Farber Cancer Institute|Infinity Pharmaceuticals, Inc. July 2014 Phase 1|Phase 2
NCT02095587 Completed Hepatic Impairment Infinity Pharmaceuticals, Inc. March 2014 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    Whether IPI-145 S7028 is mixture of two chiral forms, if not, which form is it?

  • Answer:

    S7028 IPI-145 is S form.

PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID