Choose Your Country or Region

Eganelisib (IPI-549)

Name: Eganelisib (IPI-549)
Brand: Selleck Chemicals
SKU: S8330
Rating: 5 (13 reviews)

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.

CAS No. 1693758-51-8

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

Purity & Quality Control

Choose Selective PI3K Inhibitors

Related Compound Libraries

Other PI3K Products

Taselisib (GDC 0032)^New

Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with K_i of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.
Pilaralisib (XL147)^New

Pilaralisib (XL147) is a selective and reversible class I PI3K inhibitor for PI3Kα/δ/γ with IC50 of 39 nM/36 nM/23 nM in cell-free assays, less potent to PI3Kβ. Phase 1/2.
LY294002

LY294002 (SF 1101, NSC 697286) is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively; more stable in solution than Wortmannin, and also blocks autophagosome formation. It not only binds to class I PI3Ks and other PI3K-related kinases, but also to novel targets seemingly unrelated to the PI3K family. LY294002 also inhibits CK2 with IC50 of 98 nM. LY294002 is a non-specific DNA-PKcs inhibitor and activates autophagy and apoptosis.
3-Methyladenine (3-MA)

3-Methyladenine (3-MA, NSC 66389) is a selective PI3K inhibitor for Vps34 and PI3Kγ with IC50 of 25 μM and 60 μM in HeLa cells; blocks class I PI3K consistently, whereas suppression of class III PI3K is transient, and also blocks autophagosome formation. 3-Methyladenine (3-MA) is successfully used to suppress mitophagy. Solutions of 3-MA are best fresh-prepared by heating.
Idelalisib

Idelalisib (CAL-101, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy.
Wortmannin (KY 12420)

Wortmannin (KY 12420, SL-2052, BRN 0067676, NSC 627609) is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.
Dactolisib (BEZ235)

Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3^TopBP1-ER cell. Dactolisib induces autophagy and suppresses HIV-1 replication. Phase 2.
Buparlisib (BKM120)

Buparlisib (BKM120, NVP-BKM120) is a selective PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Buparlisib induces apoptosis. Phase 2.
Pictilisib (GDC-0941)

Pictilisib (GDC-0941, RG7321) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM in cell-free assays, with modest selectivity against p110β (11-fold) and p110γ (25-fold). Pictilisib (GDC-0941) induces autophagy and apoptosis. Phase 2.

Download Inhibitor Catalog

PI3K Signaling Pathway Map

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	MVzGeY5kfGmxbjDhd5NigQ>?		NXPlTXQ{SmmwZHnu[{Bi\m[rbnn0fUB1dyCqdX3hckBz\WOxbXLpcoFvfCCodXzsJIxmdme2aDDOMZRmem2rbnHsJGhqey22YXfn[YQhWEl\|S3fhcY1iKGW6cILld5Nm\CCrbjDT[lkhcW6\|ZXP0JINmdGy\|IHL5JIVyfWmuaXLybZVuKG[udX;y[ZNk\W6lZTD0bZRz[XSrb36gZY5idHm\|aYOsJGtlKD1iMD6wNFAzQSEQvF2u	M33UN\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5Nk[wOlkzLz5{N{[2NFY6OjxxYU6=
RAW264.7	MUfGeY5kfGmxbjDhd5NigQ>?	NEXlU5Q{OCCvaX7z	NInERY1KdmirYnn0bY9vKG:oIGDJN2to[W2vYTDpckBEPWFvc4TpcZVt[XSnZDDtc5V{\SCUQWeyOlQvPyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gRWtVKHCqb4PwbI9zgWyjdHnvckBifCCVNEezJIlv[3WkYYTl[EBnd3JiM{CgcYlveyCob3zsc5dm\CCkeTDzeIlufWyjdHnvckB4cXSqIFO1ZUBnd3JiMzDtbY5{KGK7IFXMTXNCNCCLQ{WwJF0hOC5yMEGyJO69VS5?	NHzTN3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{[2NFY6Oid-Mke2OlA3QTJ:L3G+
Sf9	NYHwVldWTnWwY4Tpc44h[XO\|YYm=	M2TsVlE2KG2rboO=	NHOydGZKdmirYnn0bY9vKG:oIHj1cYFvKHKnY3;tZolv[W62IH\1cIwhdGWwZ4ToJG4ufGW{bXnuZYwhUGm\|LYTh[4dm\CCSSUPL[4FudWFiZYjwdoV{e2WmIHnuJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiZHnDPHBKWDJiYYOgd5Vje3S{YYTlJIlv[3WkYYTl[EBnd3JiMUWgcYlveyCob3zsc5dm\CCkeTDzeYJ{fHKjdHWgZYRlcXSrb36gcYVie3W{ZXSgZYZ1\XJiMjDodkBjgSCDRGCtS4xwKGy3bXnu[ZNk\W6lZTDhd5NigSxiSVO1NEA:KDBwMEG2JO69VS5?	M3HEbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5Nk[wOlkzLz5{N{[2NFY6OjxxYU6=
Sf9	MUjGeY5kfGmxbjDhd5NigQ>?		NH\HNI9DcW6maX7nJIFn\mmwaYT5JJRwKGi3bXHuJJJm[2:vYnnuZY51KG[3bHygcIVv\3SqIF6teIVzdWmwYXygTIl{Pi22YXfn[YQhWEl\|SzDwNVEx[WyyaHGvdFg2[WyyaHGgZ49mgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOgbY5n\WO2ZXSgV4Y6KGmwc3XjeEBk\WyuczDifUBmeXWrbHnidol2dSCobIXvdoV{[2WwY3WgeIl1emG2aX;uJIFv[Wy7c3nzMEBM\CB;IECuNFE4KM7:TT6=	NHGzXlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{[2NFY6Oid-Mke2OlA3QTJ:L3G+
Sf9	NVzRbpMyTnWwY4Tpc44h[XO\|YYm=		NFzuOVZDcW6maX7nJIFn\mmwaYT5JJRwKGi3bXHuJJJm[2:vYnnuZY51KG[3bHygcIVv\3SqIF6teIVzdWmwYXygS3NVNXSjZ3fl[EBRUTONIICxNVBl\Wy2YT;wPFVidHCqYTDjc4V5eHKnc4Pl[EBqdiCkYXP1cI93cXK3czDpcoZm[3SnZDDT[lkhcW6\|ZXP0JINmdGy\|IHL5JIVyfWmuaXLybZVuKG[udX;y[ZNk\W6lZTD0bZRz[XSrb36gZY5idHm\|aYOsJGtlKD1iMD6wNlMh\|ryPLh?=	M3i2d\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5Nk[wOlkzLz5{N{[2NFY6OjxxYU6=
Sf9	NHr0T3RHfW6ldHnvckBie3OjeR?=		MV;CbY5lcW6pIHHm[olvcXS7IITvJIh2dWGwIILlZ49u[mmwYX70JIZ2dGxibHXu[5RpKE5vdHXycYlv[WxiSHnzOk11[WepZXSgVGk{UyCyMUGwZoV1[S:yOEXhcJBp[SClb3X4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CCVZkmgbY5{\WO2IHPlcIx{KGK7IHXxeYltcWK{aYXtJIZtfW:{ZYPj[Y5k\SC2aYTyZZRqd25iYX7hcJl{cXNuIFvkJF0hOC5yOEKg{txONg>?	NFXtN5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{[2NFY6Oid-Mke2OlA3QTJ:L3G+
Raji	M4nJPGZ2dmO2aX;uJIF{e2G7	MW[zNEBucW6\|	NHW0VVFKdmirYnn0bY9vKG:oIGDJN2tl\Wy2YTDpckBK\01vc4TpcZVt[XSnZDDoeY1idiCUYXrpJINmdGy\|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCDS2SgdIhwe3Cqb4L5cIF1cW:wIHH0JHM1PzNiaX7jeYJifGWmIH\vdkA{OCCvaX7zJIZwdGyxd3XkJIJ6KHO2aX31cIF1cW:wIIfpeIghUWePIH\vdkA{OCCvaX7zJIJ6KEWOSWPBMEBKSzVyIE2gNE4yQCEQvF2u	MmHRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd4NkC2PVIoRjJ5Nk[wOlkzRC:jPh?=
786-O	NGDuPWFHfW6ldHnvckBie3OjeR?=	MXOzNEBucW6\|	NEDFNGNKdmirYnn0bY9vKG:oIGDJN2tj\XSjIHnuJIh2dWGwIEe4Ok1QKGOnbHzzJIF{e2W\|c3XkJIF{KHKnZIXjeIlwdiCrbjDBT3QheGixc4Doc5J6dGG2aX;uJIF1KFN2N{OgZYZ1\XJiM{CgcYlveyCkeTDFUGlUSSxiSVO1NEA:KDBwMkSg{txONg>?	NXHuTo4zRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke2OlA3QTJpPkK3OlYxPjl{PD;hQi=>
SKOV-3	MXTGeY5kfGmxbjDhd5NigQ>?	M4fWZlMxKG2rboO=	M{\aUGlvcGmkaYTpc44hd2ZiUFmzT4FteGijIHnuJIh2dWGwIGPLU3YuOyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gRWtVKHCqb4PwbI9zgWyjdHnvckBifCCVNEezJIFnfGW{IEOwJI1qdnNiYomgSWxKW0FuIFnDOVAhRSByLkK1JO69VS5?	NYTEV4F{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMke2OlA3QTJpPkK3OlYxPjl{PD;hQi=>
Sf9	M1vydWZ2dmO2aX;uJIF{e2G7	NXnuUHRnOTVibXnudy=>	NWLoR4hZUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDmeYxtKGynbnf0bEBPNXSncn3pcoFtKEirc{[teIFo\2WmIGDJN2sheDFzMHHsdIhiN3B6NXHsdIhiKGOxZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{KGmwZnXjeIVlKFOoOTDpcpNm[3RiY3XscJMhfXOrbneg[IlEQFCLUEKgZZMhe3Wkc4TyZZRmKGmwY4XiZZRm\CCob4KgNVUhdWmwczDmc4xtd3enZDDifUB{fWK\|dILheIUh[WSmaYTpc44hdWWjc4Xy[YQh[W[2ZYKgNkBpeiCkeTDBSHAuT2yxLDDJR\|UxKD1iMz6yJO69VS5?	M3jKcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5Nk[wOlkzLz5{N{[2NFY6OjxxYU6=
Sf9	MWnGeY5kfGmxbjDhd5NigQ>?	MnvHNVUhdWmwcx?=	M2PBe2lvcGmkaYTpc44hd2ZiaIXtZY4hemWlb33ibY5idnRiZoXscEBt\W6pdHigUk11\XKvaX7hcEBJcXN4LYTh[4dm\CCSSUPLJJAyOTCkZYThM5A5PWGucHjhJINw\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJHNnQSCrboPlZ5Qh[2WubIOgeZNqdmdiZHnDPHBKWDJiYYOgd5Vje3S{YYTlJIlv[3WkYYTl[EBnd3JiMUWgcYlveyCob3zsc5dm\CCkeTDzeYJ{fHKjdHWgZYRlcXSrb36gcYVie3W{ZXSgZYZ1\XJiMjDodkBjgSCDRGCtS4xwKCxiSVO1NEA:KDNwNTFOwG0v	MonjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjd4NkC2PVIoRjJ5Nk[wOlkzRC:jPh?=

Click to View More Cell Line Experimental Data

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.

References

[1] Evans CA, et al. ACS Med Chem Lett. 2016, 7(9):862-7.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	528.56
Formula	C₃₀H₂₄N₈O₂
CAS No.	1693758-51-8
Storage	3 years	-20°C	powder
Storage	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

Download Eganelisib (IPI-549) SDF

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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
=	×	×

Dilution Calculator Molecular Weight Calculator

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 2022-08-01)

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

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):