IPI549 (Eganelisib)
IPI549
CAS: 1693758-51-8
Molecular Formula: C30H24N8O2
IPI549 (Eganelisib) - Names and Identifiers
IPI549 (Eganelisib) - Physico-chemical Properties
| Molecular Formula | C30H24N8O2 |
| Molar Mass | 528.56 |
| Density | 1.37±0.1 g/cm3(Predicted) |
| Solubility | DMSO: 15 mg/mL |
| Appearance | solid |
| Color | Pale yellow |
| pKa | 10.81±0.46(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month. |
| In vitro study | IPI-549 and PI3Kγ can bind tightly with a Kd value of 290 pM, and the affinity for other I-type PI3K subtypes is more than 58 times weaker. In experiments on 48 mutant and non-mutant protein kinases and lipid kinases, IPI-549 at a concentration of 1 μm had no significant inhibitory effect on them. IPI-549 effectively inhibited PI3Kγ(IC50 = 1.2 nM) in PI3K-α, -β, -γ, and-δ-dependent intracellular p-AKT experiments, it is more than 146 times selective for other class I subtypes. In addition, IPI-549 inhibited the migration of PI3Kγ-dependent bone marrow-derived cells in vitro. Among the 80 GPCRs, ion channels, and transporters, IPI-549 at a concentration of 10 μm has high selectivity. It has moderate cell permeability and can penetrate through Caco-2x single cell layers. In hepatocytes, metabolism is slow (t1/2 > 360 min). The IC50 for the CYP subtypes tested (1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4) was greater than 20 μm. |
| In vivo study | In in vivo models (mouse, rat, canine, and monkey),IPI-549 has good oral bioavailability, low clearance, and an average volume of distribution in tissues of 1.2 L/kg. It has good pharmacokinetic characteristics in vivo and can effectively and selectively inhibit PI3Kγ. Oral administration of IPI549 significantly and dose-dependently reduced neutrophil migration in a mouse model. In addition, in a mouse homologous model, IPI-549 inhibited tumor growth by altering immune cells in the tumor microenvironment. |
IPI549 (Eganelisib) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.892 ml | 9.46 ml | 18.919 ml |
| 5 mM | 0.378 ml | 1.892 ml | 3.784 ml |
| 10 mM | 0.189 ml | 0.946 ml | 1.892 ml |
| 5 mM | 0.038 ml | 0.189 ml | 0.378 ml |
Last Update：2024-01-02 23:10:35
IPI549 (Eganelisib) - Reference Information
| Introduction | IPI-549 is produced by Infinity Pharmaceuticals by blocking PI3 kinase-gamma (PI3Kγ) in suppressor cells. Molecules. The related research was published in the journal Nature in 2016. The experimental results show that blocking this molecule changes the balance of such immunosuppressive cells and promotes the activation of anti-tumor immunity. |
| Use | IPI-549 is a selective phosphoinositide 3 kinase (PI3Kγ) inhibitor. PI3Kγ inhibitors can be used to develop potential treatments for inflammatory and autoimmune diseases. |
| Application | IPI-549 is produced by Infinity Pharmaceuticals by blocking PI3 kinase-gamma (PI3Kγ) in suppressor cells. Molecules that can be used as reagents for Cell Biology. |
| biological activity | Eganelisib (IPI-549) is a potent inhibitor of PI3K-γ, the selectivity was more than 100-fold over other lipids and protein kinases. The biochemical IC50 was 16 nM. |
| Target | Value |
| PI3Kγ (Cell-free assay) | 16 nM |
Last Update：2024-04-10 22:29:15
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CAS: 1693758-51-8
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Product Name: IPI549 Visit Supplier Webpage Request for quotation
CAS: 1693758-51-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 1693758-51-8
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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