Eganelisib
Based on 28 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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.68%
- No. CAS: 1693758-51-8
- Fòrmula: C30H24N8O2
- Peso molecular:528.56
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Eganelisib
More- Nature. 2022 Oct;610(7931):366-372. [Abstract]
- Cancer Cell. 2021 Oct 11;39(10):1361-1374.e9. [Abstract]
- Cancer Discov. 2021 May;11(5):1286-1305. [Abstract]
- Nat Cancer. 2024 Jul;5(7):1082-1101. [Abstract]
- Nat Immunol. 2024 Aug;25(8):1422-1431. [Abstract]
- Nat Commun. 2024 Jan 31;15(1):950. [Abstract]
- Nat Commun. 2022 May 20;13(1):2834. [Abstract]
- Nat Commun. 2019 Sep 25;10(1):4364. [Abstract]
- ACS Nano. 2025 Sep 2;19(34):31077-31091. [Abstract]
- ACS Nano. 2021 Dec 28;15(12):20414-20429. [Abstract]
- Adv Sci (Weinh). 2021 Jul;8(14):e2100712. [Abstract]
- Cell Rep Med. 2026 Jun 16;7(6):102833. [Abstract]
- Asian J Pharm Sci. 2022 Jul;17(4):557-570. [Abstract]
- J Control Release. 2024 May 15:370:677-690. [Abstract]
- Phytomedicine. 2026 Oct:160:158639.
- J Transl Med. 2023 Aug 14;21(1):544. [Abstract]
- Oncogene. 2026 Oct;45(40):4330-4344.
- Phytother Res. 2026 Apr 27. [Abstract]
- Cell Rep. 2024 Apr 23;43(5):114132. [Abstract]
- J Ethnopharmacol. 2026 Oct 28:369:121888. [Abstract]
- Cell Rep Methods. 2026 Jun 15;6(6):101339. [Abstract]
- ACS Appl Bio Mater. 2025 Jun 16;8(6):5239-5251. [Abstract]
- Brain Res Bull. 2019 Aug:150:272-280. [Abstract]
- FASEB J. 2026 Jun 15;40(11):e71954. [Abstract]
- BMC Cancer. 2026 Jul 16.
- Int J Parasitol Drugs Drug Resist. 2024 Aug:25:100539. [Abstract]
- bioRxiv. 2026 Aug 12.
- bioRxiv. 2023 Dec 15:2023.12.15.571909. [Abstract]
Customer Validation & Images
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WB
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WB
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RT-PCR
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Cell Imaging/Staining
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In Vivo Efficacy Study
Actividad biológica
Descripciòn
IC50 & Target
[1]|
PI3Kγ 16 nM (IC50) |
PI3Kα 3.2 μM (IC50) |
PI3Kβ 3.5 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Raji | IC50 |
180 nM
Compound: 26
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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
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[PMID: 27660692] |
| RAW264.7 | IC50 |
1.2 nM
Compound: 26
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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
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[PMID: 27660692] |
| Sf9 | IC50 |
>8400 nM
Compound: 26
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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
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[PMID: 27660692] |
| Sf9 | IC50 |
16 nM
Compound: 26
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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
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[PMID: 27660692] |
| Sf9 | IC50 |
3200 nM
Compound: 26
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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
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[PMID: 27660692] |
| Sf9 | IC50 |
3500 nM
Compound: 26
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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
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[PMID: 27660692] |
| SK-OV-3 | IC50 |
250 nM
Compound: 26
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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
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[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 Kd of 290 pM and >58-fold weaker affinity for other Class I PI3K isoforms (PI3Kα Kd=17 nM, PI3Kβ Kd=82 nM, PI3Kδ Kd=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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1693758-51-8
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Appearance Solid
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Peso molecular 528.56
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Fòrmula C30H24N8O2
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Color Light yellow to yellow
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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
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Synonyms
IPI-549
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (28)
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Journal Impact Factor
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Most Recent
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Nature
2022 Oct;610(7931):366-372. PMID: 36198801 -
Cancer Cell
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.
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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.
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Nat Immunol
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 -
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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 -
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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 -
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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 -
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bioRxiv
2023 Dec 15:2023.12.15.571909. PMID: 38328043
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (282 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
Eganelisib Related Classifications
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