IPI-549

Catalog No.S8330

IPI-549 Chemical Structure

Molecular Weight(MW): 528.56

IPI-549 is a potent inhibitor of PI3K-γ with >100-fold selectivity over other lipid and protein kinases. The biochemical IC50 for PI3K-γ is 16 nM.

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Biological Activity

Description IPI-549 is a potent inhibitor of PI3K-γ with >100-fold selectivity over other lipid and protein kinases. The biochemical IC50 for PI3K-γ is 16 nM.
Targets
PI3Kγ [1]
(Cell-free assay)
16 nM
In vitro

IPI-549 is found to be a remarkably tight binder to PI3K-γ with a Kd of 290 pM and >58-fold weaker affinity for other Class I PI3K isoforms. It does not significantly inhibit a panel of 468 mutant and nonmutant protein and lipid kinases (including Class II PI3K isoforms) at 1 μM. In PI3K-α, -β, -γ, and -δ dependent cellular phospho-AKT assays, IPI-549 demonstrates excellent PI3K-γ potency (IC50 = 1.2 nM) and selectivity against other Class I PI3K isoforms (>146-fold). Furthermore, IPI-549 dose dependently inhibits PI3K-γ-dependent bone marrow-derived macrophage (BMDM) migration in vitro. IPI-549 is also found to be selective against a panel of 80 GPCRs, ion channels, and transporters at 10 μM. In vitro, IPI-549 shows moderate to high cell permeability across Caco-2 cell monolayers, is slowly metabolized in cultured hepatocytes (t1/2 > 360 min), and demonstrates IC50s greater than 20 μM for the CYP isoforms tested (1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4)[1].
In vivo In vivo (mice, rats, dog, and monkeys), IPI-549 has excellent oral bioavailability, low clearance, and distributes into tissues with a mean volume of distribution of 1.2 L/kg. It has a favorable pharmacokinetic profile to allow potent and selective inhibition of PI3K-γ in vivo. IPI-549 can significantly reduce neutrophil migration in a dose-dependent manner in mouse model when administered orally at all of the tested doses. In addition, IPI-54 has been shown to inhibit tumor growth in murine syngeneic models through alteration of immune cells in the tumor microenvironment[1].

Protocol

Cell Research:

[1]
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  • Cell lines: SKOV-3 cells
  • Concentrations: --
  • Incubation Time: 30 min
  • Method:

    SKOV-3 cells are seeded into 96-well cell culture-grade plates at a density of 200,000 cells/200 μL/well of RPMI-1640 with 10% FBS. Cells are incubated overnight at 5% CO2 and 37 °C. Compounds are added to the cells, resulting in a final DMSO concentration of 0.5%, and incubated for 30 minutes at 5% CO2 and 37 °C. Media is then aspirated and 50 μL/well of ice-cold lysis buffer is added. Plates are incubated on ice for 5 minutes and then centrifuged at 3000 rpm at 4 °C for 5 minutes.


    (Only for Reference)
Animal Research:

[1]
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  • Animal Models: CD-1 mice, Sprague-Dawley rats, beagle dogs and cynomolgus monkeys.
  • Formulation: 5% N-methyl-2-pyrrolidone, 40% PEG400 and 55% PBS (v/v)(dissolved); 0.5% (w/v) of carboxymethylcellulose and 0.05% Tween80(suspended)
  • Dosages: 0.5-1.25 mg/mL(For PO dosing); 5-10 mg/mL(for efficacy studies); 0.25-0.4 mg/mL(for IV dosing)
  • Administration: p.o.; i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (189.19 mM)
Ethanol 8 mg/mL (15.13 mM)
Water 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 528.56
Formula

C30H24N8O2
CAS No. 1693758-51-8
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03795610 Not yet recruiting Head and Neck Squamous Cell Carcinoma|Head and Neck Cancer|Head and Neck Carcinoma|Head and Neck Cancer Stage IV|Head and Neck Cancer Stage III|HPV-Related Carcinoma|HPV-Related Malignancy|HPV-Related Squamous Cell Carcinoma Ezra Cohen|The V Foundation for Cancer Research|University of California San Diego June 2019 Phase 2
NCT03795610 Not yet recruiting Head and Neck Squamous Cell Carcinoma|Head and Neck Cancer|Head and Neck Carcinoma|Head and Neck Cancer Stage IV|Head and Neck Cancer Stage III|HPV-Related Carcinoma|HPV-Related Malignancy|HPV-Related Squamous Cell Carcinoma Ezra Cohen|The V Foundation for Cancer Research|University of California San Diego June 2019 Phase 2
NCT02637531 Recruiting Advanced Solid Tumors (Part A/B/C/D)|Non-small Cell Lung Cancer (Part E)|Melanoma (Part E)|Squamous Cell Cancer of the Head and Neck (Part E)|Triple Negative Breast Cancer (Part F)|Adrenocortical Carcinoma (Part G)|Mesothelioma (Part G)|High-circulating Myeloid-derived Suppressor Cells (Part H) Infinity Pharmaceuticals Inc. December 2015 Phase 1
NCT02637531 Recruiting Advanced Solid Tumors (Part A/B/C/D)|Non-small Cell Lung Cancer (Part E)|Melanoma (Part E)|Squamous Cell Cancer of the Head and Neck (Part E)|Triple Negative Breast Cancer (Part F)|Adrenocortical Carcinoma (Part G)|Mesothelioma (Part G)|High-circulating Myeloid-derived Suppressor Cells (Part H) Infinity Pharmaceuticals Inc. December 2015 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID