Eganelisib (Synonyms: IPI-549)

Name: Eganelisib
Brand: MedChemExpress
SKU: HY-100716
Rating: 5.0 (17 reviews)

Cat. No.: HY-100716 Purity: 99.68%: FAQs
Data Sheet SDS COA Handling Instructions

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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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Eganelisib Chemical Structure

CAS No. : 1693758-51-8

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10 mM * 1 mL in DMSO ready for reconstitution	USD 58	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 58	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 17 publication(s) in Google Scholar

17 Publications Citing Use of MCE Eganelisib

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View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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)

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

Molecular Weight

528.56

Formula

C₃₀H₂₄N₈O₂

CAS No.

1693758-51-8

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.68%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (254 KB) HNMR (298 KB) LCMS (94 KB) Elemental Analysis Report (111 KB)

Handling Instructions (2659 KB)

References

[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]

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].

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

References

[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

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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Eganelisib1693758-51-8IPI-549IPI549IPI 549PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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Eganelisib (Synonyms: IPI-549)

Customer Review

Eganelisib Related Antibodies

17 Publications Citing Use of MCE Eganelisib

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Eganelisib Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Eganelisib Related Classifications

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