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Eganelisib

Catalog No. T5432 CAS 1693758-51-8

Synonyms: IPI-549

Eganelisib (IPI-549) is an inhibitor of PI3Kγ (IC50 = 16, 3,200, 3,500, and <8,400 nM for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively)

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Eganelisib, CAS 1693758-51-8

Pack Size	Availability	Price/USD
5 mg	In stock	$ 40.00
10 mg	In stock	$ 64.00
25 mg	In stock	$ 113.00
50 mg	In stock	$ 197.00
100 mg	In stock	$ 357.00
500 mg	In stock	$ 855.00
1 mL * 10 mM (in DMSO)	In stock	$ 46.00

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Purity: 99.56%

Purity: 99.04%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Eganelisib (IPI-549) is an inhibitor of PI3Kγ (IC50 = 16, 3,200, 3,500, and >8,400 nM for PI3Kγ, PI3Kα, PI3Kβ, and PI3Kδ, respectively)
Targets&IC50	PI3Kγ:16 nM
In vitro	IPI-549 sensitizes doxorubicin-resistant SW620/Ad300 cells to P-glycoprotein (P-gp) substrates, such as paclitaxel (IC50s = 710 and 6.7 nM for paclitaxel alone and in combination with IPI-549, respectively), and increases the level of intracellular paclitaxel in SW620/Ad300 cells[1].
In vivo	IPI-549 demonstrates favorable pharmacokinetic properties and robust inhibition of PI3K-γ mediated neutrophil migration in vivo[2].
Animal Research	SW620 (4 X 10^6 ) and SW620/Ad300 (5 X 10^6 ) cells were injected subcutaneously at the flank near the armpits of athymic nude mice.?When the subcutaneous tumors were approximately 0.5 x 0.5 cm in size (day 0), the mice were randomized into four treatment groups.?The vehicle used to deliver the IPI-549 and paclitaxel by intraperitoneal (i.p.) injection was ethanol/Cremophor ELP/saline (10%/10%/80%).?Group one received the vehicle only;?group two received vehicle plus 3 mg/kg IPI-549;?group three received vehicle plus 15 mg/kg paclitaxel;?group four, the combination group, received vehicle plus 3 mg/kg IPI-549 one h prior to administration of vehicle plus 15 mg/kg paclitaxel.?The drug doses were administered every 3 days with a total of 4 doses.?Tumor volume was measured using calipers, and body weights were recorded prior to each dosing.

Synonyms	IPI-549
Molecular Weight	528.56
Formula	C30H24N8O2
CAS No.	1693758-51-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 15 mg/mL (28.38 mM)

References and Literature

1. De Vera AA1, Gupta P.et al.Immuno-oncology agent IPI-549 is a modulator of P-glycoprotein (P-gp, MDR1, ABCB1)-mediated multidrug resistance (MDR) in cancer: In vitro and in vivo.Cancer Lett. 2019 Feb 1;442:91-103 2. 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.

Citations

1. Jiang Y, Xiong W, Jia L, et al. Developing a Naïve Bayesian Classification Model with PI3Kγ structural features for virtual screening against PI3Kγ: Combining molecular docking and pharmacophore based on multiple PI3Kγ conformations. European Journal of Medicinal Chemistry. 2022: 114824. 2. Xiong W, Jia L, Liang J, et al. Investigation into the anti-airway inflammatory role of the PI3Kγ inhibitor JN-PK1: An in vitro and in vivo study. International Immunopharmacology. 2022, 111: 109102 3. Xiong W, Jia L, Liang J, et al.Investigation into the anti-airway inflammatory role of the PI3Kγ inhibitor JN-PK1: An in vitro and in vivo study.International Immunopharmacology.2022, 111: 109102. 4. Xiong W, Jia L, Cai Y, et al.Evaluation of the anti-inflammatory effects of PI3Kδ/γ inhibitors for treating acute lung injury.Immunobiology.2023: 152753.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Inhibitor Library Kinase Inhibitor Library Highly Selective Inhibitor Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library Antidepressant Compound Library Anti-Aging Compound Library Antioxidant Compound Library

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Keywords

Eganelisib 1693758-51-8 PI3K/Akt/mTOR signaling PI3K inhibit Inhibitor IPI-549 IPI 549 IPI549 Phosphoinositide 3-kinase inhibitor

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