Art. -Nr.: HY-100716

Eganelisib

(Synonyms: IPI-549)

24 Cited Publications

Kundenbewertung

Based on 24 publication(s) in Google Scholar

Eganelisib (IPI549) is a potent and selective PI3Kγ inhibitor with an IC₅₀ of 16 nM. Eganelisib shows >100-fold selectivity over other lipid and protein kinases.

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Reinheit: 99.68%
CAS. Nr.: 1693758-51-8
Formel: C₃₀H₂₄N₈O₂
Molecular Weight:528.56

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Eganelisib Chemical Structure

CAS. Nr.: 1693758-51-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (24)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Eganelisib (IPI549) is a potent and selective PI3Kγ inhibitor with an IC₅₀ of 16 nM. Eganelisib shows >100-fold selectivity over other lipid and protein kinases^[1].

IC₅₀ & Target^[1]

PI3Kγ

16 nM (IC₅₀)

PI3Kα

3.2 μM (IC₅₀)

PI3Kβ

3.5 μM (IC₅₀)

Alle PI3K Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Raji	IC₅₀	180 nM Compound: 26	Inhibition of PI3Kdelta in IgM-stimulated human Raji cells assessed as reduction in AKT phosphorylation at S473 incubated for 30 mins followed by stimulation with IgM for 30 mins by ELISA Inhibition of PI3Kdelta in IgM-stimulated human Raji cells assessed as reduction in AKT phosphorylation at S473 incubated for 30 mins followed by stimulation with IgM for 30 mins by ELISA	[PMID: 27660692]
RAW264.7	IC₅₀	1.2 nM Compound: 26	Inhibition of PI3Kgamma in C5a-stimulated mouse RAW264.7 cells assessed as reduction in AKT phosphorylation at S473 incubated for 30 mins followed by stimulation with C5a for 3 mins by ELISA Inhibition of PI3Kgamma in C5a-stimulated mouse RAW264.7 cells assessed as reduction in AKT phosphorylation at S473 incubated for 30 mins followed by stimulation with C5a for 3 mins by ELISA	[PMID: 27660692]
Sf9	IC₅₀	>8400 nM Compound: 26	Inhibition of human recombinant full length N-terminal GST-tagged PI3K p110delta/p85alpha coexpressed in baculovirus infected Sf9 insect cells using diC8PIP2 as substrate incubated for 15 mins followed by substrate addition measured after 2 hr by ADP-Glo Inhibition of human recombinant full length N-terminal GST-tagged PI3K p110delta/p85alpha coexpressed in baculovirus infected Sf9 insect cells using diC8PIP2 as substrate incubated for 15 mins followed by substrate addition measured after 2 hr by ADP-Glo	[PMID: 27660692]
Sf9	IC₅₀	16 nM Compound: 26	Inhibition of human recombinant full length N-terminal His-tagged PI3Kgamma expressed in Sf9 insect cells using diC8PIP2 as substrate incubated for 15 mins followed by substrate addition measured after 2 hr by ADP-Glo luminescence assay Inhibition of human recombinant full length N-terminal His-tagged PI3Kgamma expressed in Sf9 insect cells using diC8PIP2 as substrate incubated for 15 mins followed by substrate addition measured after 2 hr by ADP-Glo luminescence assay	[PMID: 27660692]
Sf9	IC₅₀	3200 nM Compound: 26	Inhibition of human recombinant full length N-terminal His6-tagged PI3K p110alpha/p85alpha coexpressed in baculovirus infected Sf9 insect cells using diC8PIP2 as substrate incubated for 15 mins followed by substrate addition measured after 2 hr by ADP-Glo Inhibition of human recombinant full length N-terminal His6-tagged PI3K p110alpha/p85alpha coexpressed in baculovirus infected Sf9 insect cells using diC8PIP2 as substrate incubated for 15 mins followed by substrate addition measured after 2 hr by ADP-Glo	[PMID: 27660692]
Sf9	IC₅₀	3500 nM Compound: 26	Inhibition of human recombinant full length N-terminal His6-tagged PI3K p110beta/p85alpha coexpressed in baculovirus infected Sf9 insect cells using diC8PIP2 as substrate incubated for 15 mins followed by substrate addition measured after 2 hr by ADP-Glo Inhibition of human recombinant full length N-terminal His6-tagged PI3K p110beta/p85alpha coexpressed in baculovirus infected Sf9 insect cells using diC8PIP2 as substrate incubated for 15 mins followed by substrate addition measured after 2 hr by ADP-Glo	[PMID: 27660692]
SK-OV-3	IC₅₀	250 nM Compound: 26	Inhibition of PI3Kalpha in human SKOV-3 cells assessed as reduction in AKT phosphorylation at S473 after 30 mins by ELISA Inhibition of PI3Kalpha in human SKOV-3 cells assessed as reduction in AKT phosphorylation at S473 after 30 mins by ELISA	[PMID: 27660692]

In Vitro

Eganelisib (IPI549) inhibits PI3Kγ with IC₅₀ of 16 nM, with >100-fold selectivity over other lipid and protein kinases (PI3Kα IC₅₀=3.2 μM, PI3Kβ IC₅₀=3.5 μM, PI3Kδ IC₅₀>8.4 μM). Eganelisib is evaluated for activity across all Class I PI3K isoforms. The binding affinity of Eganelisib for PI3K-γ is determined by measuring the individual rates constants and for PI3K-α, β and δ using equilibrium fluorescent titration. Eganelisib is a remarkably tight binder to PI3Kγ with a K_d of 290 pM and >58-fold weaker affinity for other Class I PI3K isoforms (PI3Kα K_d=17 nM, PI3Kβ K_d=82 nM, PI3Kδ K_d=23 M). In PI3K-α, -β, -γ, and -δ dependent cellular phospho-AKT assays, Eganelisib demonstrates excellent PI3K-γ potency (IC₅₀=1.2 nM) and selectivity against other Class I PI3K isoforms (>146-fold). Cellular IC₅₀s for Class I PI3Kα (250 nM), PI3Kβ (240 nM), PI3Kγ (1.2 nM), PI3Kδ (180 nM) are determined in SKOV-3, 786-O, RAW 264.7, and RAJI cells, respectively, by monitoring inhibition of pAKT S473 by ELISA. Furthermore, Eganelisib dose dependently inhibits PI3Kγ dependent bone marrow-derived macrophage (BMDM) migration. Eganelisib is selective against a panel of 80 GPCRs, ion channels, and transporters at 10 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Eganelisib (IPI549) demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-γ mediated neutrophil migration. In vivo (mice, rats, dog, and monkeys), Eganelisib has excellent oral bioavailability, low clearance, and distributed into tissues with a mean volume of distribution of 1.2 L/kg. Overall, Eganelisib has a favorable pharmacokinetic profile to allow potent and selective inhibition of PI3K-γ in vivo. The t_1/2 of IPI-549 for mouse, rat, dog and monkey is 3.2, 4.4, 6.7 and 4.3 h, respectively. Eganelisib significantly reduces neutrophil migration in a dose dependent manner in this model when administered orally at all of the tested doses^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1693758-51-8
Appearance Solid
Molecular Weight 528.56
Formel C₃₀H₂₄N₈O₂
Color Light yellow to yellow
SMILES

O=C(C1=C2N=CC=CN2N=C1N)N[C@H](C3=CC4=C(C(N3C5=CC=CC=C5)=O)C(C#CC6=CN(C)N=C6)=CC=C4)C
Synonyms

IPI-549
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (24)

All RT-PCRCell Imaging/StainingIn Vivo Efficacy StudyWB

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Journal Impact Factor

Nature

Collagenolysis-dependent DDR1 signalling dictates pancreatic cancer outcome. [Abstract]

2022 Oct;610(7931):366-372. PMID: 36198801
Cancer Cell

Activating a collaborative innate-adaptive immune response to control metastasis. [Abstract]

2021 Oct 11;39(10):1361-1374.e9. PMID: 34478639

Eganelisib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Oct 11;39(10):1361-1374.e9. [Abstract]

Eganelisib (1 μM; 24 h) increased H2-Q2 and inhibited Il10 expression in macrophages and cancer cells from the metastatic pleural effusions of breast cancer patients.

Eganelisib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Oct 11;39(10):1361-1374.e9. [Abstract]

Eganelisib (1 μM; 48 h) did not activate TAMs to kill PyMT tumor-derived macrophages.

Eganelisib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Oct 11;39(10):1361-1374.e9. [Abstract]

Eganelisib (IPI-549; 15 mg/kg; dailly; po; from day 13 to day 34) in MMTV-PyMT mice shows anti-tumor activity.

Eganelisib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Oct 11;39(10):1361-1374.e9. [Abstract]

Eganelisib (IPI-549; 15 mg/kg; dailly; po; from day 21 to day 42) in ID8-p53^−/−tumor-bearing mice shows anti-tumor activity.
Cancer Discov

Direct and Indirect Regulators of Epithelial-Mesenchymal Transition-Mediated Immunosuppression in Breast Carcinomas. [Abstract]

2021 May;11(5):1286-1305. PMID: 33328216
Nat Cancer

Targeting a lineage-specific PI3Kɣ-Akt signaling module in acute myeloid leukemia using a heterobifunctional degrader molecule. [Abstract]

2024 Jul;5(7):1082-1101. PMID: 38816660

Eganelisib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2024 Jul;5(7):1082-1101. [Abstract]

AKT phosphorylation levels by western blot in OCI-AML2 cells either infected with PIK3CG- and PIK3R5-directed sgRNAs for 72 hours or treated with 500nM Eganelisib (IPI-549), AZ2, or the AKT inhibitor, MK-2206, for one and 72 hours.

Eganelisib purchased from MedChemExpress. Usage Cited in: Nat Cancer. 2024 Jul;5(7):1082-1101. [Abstract]

AKT phosphorylation levels by western blot of OCI-AML2 cells treated for one hour, 72 hours, or 72 hours followed by fresh addition of 500 nM Eganelisib (IPI-549), AZ2, or MK-2206 for one hour.
Nat Immunol

PI3Kγ in B cells promotes antibody responses and generation of antibody-secreting cells. [Abstract]

2024 Aug;25(8):1422-1431. PMID: 38961274
Nat Commun

Bacterial protoplast-derived nanovesicles carrying CRISPR-Cas9 tools re-educate tumor-associated macrophages for enhanced cancer immunotherapy. [Abstract]

2024 Jan 31;15(1):950. PMID: 38296939
Nat Commun

Nanoparticle-enhanced radiotherapy synergizes with PD-L1 blockade to limit post-surgical cancer recurrence and metastasis. [Abstract]

2022 May 20;13(1):2834. PMID: 35595770
Nat Commun

Human PI3Kγ deficiency and its microbiota-dependent mouse model reveal immunodeficiency and tissue immunopathology. [Abstract]

2019 Sep 25;10(1):4364. PMID: 31554793
ACS Nano

Reprogramming Macrophage via an Antigen Phagocytosis-Presentation Nanoenhancer for Improved Cancer Immunotherapy. [Abstract]

2025 Sep 2;19(34):31077-31091. PMID: 40835579
ACS Nano

Tailoring Chemoimmunostimulant Bioscaffolds for Inhibiting Tumor Growth and Metastasis after Incomplete Microwave Ablation. [Abstract]

2021 Dec 28;15(12):20414-20429. PMID: 34881574
Adv Sci (Weinh)

Multifunctional Nanodrug Mediates Synergistic Photodynamic Therapy and MDSCs-Targeting Immunotherapy of Colon Cancer. [Abstract]

2021 Jul;8(14):e2100712. PMID: 34021727
Cell Rep Med

Fungal metabolite-based immunotherapy overcomes tumor-associated macrophage immunosuppression. [Abstract]

2026 Jun 16;7(6):102833. PMID: 42173096
Asian J Pharm Sci

Non-cytotoxic nanoparticles re-educating macrophages achieving both innate and adaptive immune responses for tumor therapy. [Abstract]

2022 Jul;17(4):557-570. PMID: 36101893
J Control Release

Electrically activated polymetallic nanocrystals for long-term tumor suppression via oxygen-independent ROS generation and electro-immunotherapy. [Abstract]

2024 May 15:370:677-690. PMID: 38740093
J Transl Med

TNFSF14/LIGHT promotes cardiac fibrosis and atrial fibrillation vulnerability via PI3Kγ/SGK1 pathway-dependent M2 macrophage polarisation. [Abstract]

2023 Aug 14;21(1):544. PMID: 37580750
Phytother Res

(+)-Matairesinol, Derived From Olive Oil, Enhanced T-Cell Anti-Tumor Immune via JAK3-STAT1 Signal and Synergized With Anti-PD-1 Efficacy. [Abstract]

2026 Apr 27. PMID: 42037203
Cell Rep

Adipocyte PI3K links adipostasis with baseline insulin secretion at fasting through an adipoincretin effect. [Abstract]

2024 Apr 23;43(5):114132. PMID: 38656871
J Ethnopharmacol

"Shihu" promote T-cell immunity against breast cancer through bioactive constituent THMB enhancing JAK3-STAT1 signal. [Abstract]

2026 Oct 28:369:121888. PMID: 42202911
Cell Rep Methods

Tumor immune microenvironment reconstitution in patient-derived organoids enables therapy modeling for NSCLC. [Abstract]

2026 Jun 15;6(6):101339. PMID: 42134319
ACS Appl Bio Mater

Hybrid Nanocarrier Delivers Immuno-Photothermal Therapy to Modulate Pancreatic Tumor Microenvironment. [Abstract]

2025 Jun 16;8(6):5239-5251. PMID: 40390390
Brain Res Bull

Anxiolytic and panicolytic-like effects of environmental enrichment seem to be modulated by serotonin neurons located in the dorsal subnucleus of the dorsal raphe. [Abstract]

2019 Aug:150:272-280. PMID: 31220551
FASEB J

Polyphosphates Attenuate Interleukin-12 Production in Macrophages Infected With Legionella pneumophila. [Abstract]

2026 Jun 15;40(11):e71954. PMID: 42219888
Int J Parasitol Drugs Drug Resist

Oral administration of IPI549 protects mice from neuropathology and an overwhelming inflammatory response during experimental cerebral malaria. [Abstract]

2024 Aug:25:100539. PMID: 38621317
bioRxiv

Targetable leukemia dependency on noncanonical PI3Kγ signaling. [Abstract]

2023 Dec 15:2023.12.15.571909. PMID: 38328043

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (47.30 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8919 mL

9.4597 mL

18.9193 mL

5 mM

0.3784 mL

1.8919 mL

3.7839 mL

10 mM

0.1892 mL

0.9460 mL

1.8919 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.25 mg/mL (2.36 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.25 mg/mL (2.36 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Animal Administration^[2]

C57BL/6J and Balb/c mice (6 to 8 weeks old) are used in this study. On day 0 of the experiments, tumor cells are injected intradermally (i.d.) in the right flank. Eganelisib is administered by oral gavage once a day at 15 mg/kg. Treatment is initiated on day 7 ending on day 21 post tumor implant. Control groups receive vehicle (5% NMP, 95% PEG). Tumors are measured every second or third day with a caliper, and the volume (length×width×height) is calculated. Animals are euthanized for signs of distress or when the total tumor volume reaches 2500 mm³. Finally, Tumors are isolated, and frozen until needed^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Evans CA, et al. Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate. ACS Med Chem Lett. 2016 Jul 22;7(9):862-7. [Content Brief]

[2]. De Henau O, et al. Overcoming resistance to checkpoint blockade therapy by targeting PI3Kγ in myeloid cells. Nature. 2016 Nov 17;539(7629):443-447. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8919 mL	9.4597 mL	18.9193 mL	47.2983 mL
	5 mM	0.3784 mL	1.8919 mL	3.7839 mL	9.4597 mL
	10 mM	0.1892 mL	0.9460 mL	1.8919 mL	4.7298 mL
	15 mM	0.1261 mL	0.6306 mL	1.2613 mL	3.1532 mL
	20 mM	0.0946 mL	0.4730 mL	0.9460 mL	2.3649 mL
	25 mM	0.0757 mL	0.3784 mL	0.7568 mL	1.8919 mL
	30 mM	0.0631 mL	0.3153 mL	0.6306 mL	1.5766 mL
	40 mM	0.0473 mL	0.2365 mL	0.4730 mL	1.1825 mL

Keywords

Eganelisib

24 Cited Publications

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Eganelisib

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Publications Citing Use of MedChemExpress (MCE) Eganelisib

Alle PI3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (24)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Eganelisib Related Classifications

HY-100716 Related Classifications