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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

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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	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?=

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	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
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)

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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.

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Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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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)

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