Eganelisib (IPI-549)

Catalog No.S8330

For research use only.

Eganelisib (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.

Eganelisib (IPI-549) Chemical Structure

CAS No. 1693758-51-8

Selleck's Eganelisib (IPI-549) has been cited by 13 publications

Purity & Quality Control

Choose Selective PI3K Inhibitors

Other PI3K Products

Biological Activity

Description Eganelisib (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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Sf9 NVfsfXdnTnWwY4Tpc44h[XO|YYm= NIC5fHlDcW6maX7nJIFn\mmwaYT5JJRwKGi3bXHuJJJm[2:vYnnuZY51KG[3bHygcIVv\3SqIF6teIVzdWmwYXygTIl{NXSjZ3fl[EBRUTONZ3HtcYEh\XiycnXzd4VlKGmwIGPmPUBqdnOnY4SgZ4VtdHNiYomg[ZF2cWyrYoLpeY0h\my3b4Lld4NmdmOnIITpeJJifGmxbjDhcoFtgXOrczygT4QhRSByLkCwNFI6KM7:TT6= NInXd489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{[2NFY6Oid-Mke2OlA3QTJ:L3G+
RAW264.7 M4TqXWZ2dmO2aX;uJIF{e2G7 NH\LSVc{OCCvaX7z Mn;OTY5pcWKrdHnvckBw\iCSSUPL[4FudWFiaX6gR|ViNXO2aX31cIF1\WRibX;1d4UhWkGZMk[0Mlch[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIFHLWEBxcG:|cHjvdplt[XSrb36gZZQhWzR5MzDpcoN2[mG2ZXSg[o9zKDNyIH3pcpMh\m:ubH;3[YQh[nlic4TpcZVt[XSrb36ge4l1cCCFNXGg[o9zKDNibXnud{BjgSCHTFnTRUwhUUN3MDC9JFAvODBzMjFOwG0v NULRTGZRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke2OlA3QTJpPkK3OlYxPjl{PD;hQi=>
Sf9 NXv1fWtUTnWwY4Tpc44h[XO|YYm= NVnsS2RsOTVibXnudy=> MnK4TY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCodXzsJIxmdme2aDDOMZRmem2rbnHsJGhqey22YXfn[YQhWEl|S3fhcY1iKGW6cILld5Nm\CCrbjDT[lkhcW6|ZXP0JINmdGy|IIXzbY5oKGSrQ{jQTXAzKGG|IIP1ZpN1emG2ZTDpcoN2[mG2ZXSg[o9zKDF3IH3pcpMh\m:ubH;3[YQh[nlic4Xid5Rz[XSnIHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDJiaIKgZpkhSUSSLVfsc{BtfW2rbnXzZ4Vv[2ViYYPzZZktKEmFNUCgQUAxNjBzNjFOwG0v MkfLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd4NkC2PVIoRjJ5Nk[wOlkzRC:jPh?=
Sf9 M{LtNGZ2dmO2aX;uJIF{e2G7 NFPaPJNDcW6maX7nJIFn\mmwaYT5JJRwKGi3bXHuJJJm[2:vYnnuZY51KG[3bHygcIVv\3SqIF6teIVzdWmwYXygTIl{Pi22YXfn[YQhWEl|SzDwNVEx[WyyaHGvdFg2[WyyaHGgZ49mgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4Y6KGmwc3XjeEBk\WyuczDifUBmeXWrbHnidol2dSCobIXvdoV{[2WwY3WgeIl1emG2aX;uJIFv[Wy7c3nzMEBM\CB;IECuNFE4KM7:TT6= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzZ4ME[5Nkc,Ojd4NkC2PVI9N2F-
Sf9 MUTGeY5kfGmxbjDhd5NigQ>? M{n0XWJqdmSrbnegZYZncW6rdImgeI8hcHWvYX6gdoVkd22kaX7hcpQh\nWubDDs[Y5ofGhiTj30[ZJucW6jbDDHV3QufGGpZ3XkJHBKO0ticEGxNIRmdHSjL4C4OYFteGijIHPv[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|IHnu[oVkfGWmIGPmPUBqdnOnY4SgZ4VtdHNiYomg[ZF2cWyrYoLpeY0h\my3b4Lld4NmdmOnIITpeJJifGmxbjDhcoFtgXOrczygT4QhRSByLkCyN{DPxE1w MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzZ4ME[5Nkc,Ojd4NkC2PVI9N2F-
Sf9 MoTFSpVv[3Srb36gZZN{[Xl? MVzCbY5lcW6pIHHm[olvcXS7IITvJIh2dWGwIILlZ49u[mmwYX70JIZ2dGxibHXu[5RpKE5vdHXycYlv[WxiSHnzOk11[WepZXSgVGk{UyCyMUGwZoV1[S:yOEXhcJBp[SClb3X4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCVZkmgbY5{\WO2IHPlcIx{KGK7IHXxeYltcWK{aYXtJIZtfW:{ZYPj[Y5k\SC2aYTyZZRqd25iYX7hcJl{cXNuIFvkJF0hOC5yOEKg{txONg>? MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzZ4ME[5Nkc,Ojd4NkC2PVI9N2F-
Raji M3\3UmZ2dmO2aX;uJIF{e2G7 MlnmN|AhdWmwcx?= MXHJcohq[mm2aX;uJI9nKFCLM1vk[Yx1[SCrbjDJ[20ue3SrbYXsZZRm\CCqdX3hckBT[WqrIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBCU1RicHjvd5Bpd3K7bHH0bY9vKGG2IGO0O|MhcW6ldXLheIVlKG[xcjCzNEBucW6|IH\vcIxwf2WmIHL5JJN1cW23bHH0bY9vKHerdHigTYdOKG[xcjCzNEBucW6|IHL5JGVNUVODLDDJR|UxKD1iMD6xPEDPxE1w MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzZ4ME[5Nkc,Ojd4NkC2PVI9N2F-
786-O NXmwWJNCTnWwY4Tpc44h[XO|YYm= NWTZO5ZMOzBibXnudy=> NX\Md4RlUW6qaXLpeIlwdiCxZjDQTVNM[mW2YTDpckBpfW2jbjC3PFYuVyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gRWtVKHCqb4PwbI9zgWyjdHnvckBifCCVNEezJIFnfGW{IEOwJI1qdnNiYomgSWxKW0FuIFnDOVAhRSByLkK0JO69VS5? NG\NN449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{[2NFY6Oid-Mke2OlA3QTJ:L3G+
SKOV-3 MXPGeY5kfGmxbjDhd5NigQ>? MVezNEBucW6| M{nCdWlvcGmkaYTpc44hd2ZiUFmzT4FteGijIHnuJIh2dWGwIGPLU3YuOyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gRWtVKHCqb4PwbI9zgWyjdHnvckBifCCVNEezJIFnfGW{IEOwJI1qdnNiYomgSWxKW0FuIFnDOVAhRSByLkK1JO69VS5? M1SwTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5Nk[wOlkzLz5{N{[2NFY6OjxxYU6=
Sf9 Mk\0SpVv[3Srb36gZZN{[Xl? NUnBS41jOTVibXnudy=> NHrqVZpKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IH\1cIwhdGWwZ4ToJG4ufGW{bXnuZYwhUGm|Nj30ZYdo\WRiUFmzT{BxOTFyYXzwbIEweDh3YXzwbIEh[2:neIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z7IHnud4VkfCClZXzsd{B2e2mwZzDkbWM5WEmSMjDhd{B{fWK|dILheIUhcW6ldXLheIVlKG[xcjCxOUBucW6|IH\vcIxwf2WmIHL5JJN2[nO2cnH0[UBi\GSrdHnvckBu\WG|dYLl[EBi\nSncjCyJIhzKGK7IFHEVE1IdG9uIFnDOVAhRSB|LkKg{txONg>? M2nBXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5Nk[wOlkzLz5{N{[2NFY6OjxxYU6=
Sf9 MW\GeY5kfGmxbjDhd5NigQ>? Mlf2NVUhdWmwcx?= Mo\CTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCodXzsJIxmdme2aDDOMZRmem2rbnHsJGhqezZvdHHn[4VlKFCLM1ugdFEyOGKndHGvdFg2[WyyaHGgZ49mgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4Y6KGmwc3XjeEBk\WyuczD1d4lv\yCmaVO4VGlROiCjczDzeYJ{fHKjdHWgbY5kfWKjdHXkJIZweiBzNTDtbY5{KG[xbHzve4VlKGK7IIP1ZpN1emG2ZTDh[IRqfGmxbjDt[YF{fXKnZDDh[pRmeiB{IHjyJIJ6KEGGUD3HcI8hNCCLQ{WwJF0hOy53IN88UU4> MoHHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd4NkC2PVIoRjJ5Nk[wOlkzRC:jPh?=
Assay
Methods Test Index PMID
Western blot p-AKT / AKT / p-p65 / p65 27642729
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 (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: CD-1 mice, Sprague-Dawley rats, beagle dogs and cynomolgus monkeys.
  • 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.

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(189.19 mM)
Ethanol 8 mg/mL
(15.13 mM)
Water Insoluble

Chemical Information

Molecular Weight 528.56
Formula

C30H24N8O2

CAS No. 1693758-51-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C1=CC2=C(C(=CC=C2)C#CC3=CN(N=C3)C)C(=O)N1C4=CC=CC=C4)NC(=O)C5=C6N=CC=CN6N=C5N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03980041 Active not recruiting Drug: IPI-549 (eganelisib)|Drug: Nivolumab|Drug: Placebos Bladder Cancer|Urothelial Carcinoma|Solid Tumor|Advanced Cancer Infinity Pharmaceuticals Inc.|Bristol-Myers Squibb September 25 2019 Phase 2
NCT02637531 Active not recruiting Drug: IPI-549 (eganelisib)|Drug: Nivolumab 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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Eganelisib (IPI-549) | Eganelisib (IPI-549) supplier | purchase Eganelisib (IPI-549) | Eganelisib (IPI-549) cost | Eganelisib (IPI-549) manufacturer | order Eganelisib (IPI-549) | Eganelisib (IPI-549) distributor