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PI3Kδ-IN-25
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Catalog No. T212311
PI3Kδ-IN-25 is an orally active and selective PI3Kδ inhibitor with an IC50 of 2.1 nM. It exhibits IC50 values of 272, 285, and 1171 nM for PI3Kα, PI3Kγ, and PI3Kβ, respectively. In B16F10 cells, PI3Kδ-IN-25 inhibits the phosphorylation of AKTSer473, suppresses Treg cell proliferation, and downregulates the expression of PD-L1. In mouse models of B16F10 melanoma and Lewis lung cancer, PI3Kδ-IN-25 demonstrates anticancer activity by reducing tumor-infiltrating Treg cells and enhancing immune responses. This compound is applicable for research on cancers such as melanoma and lung cancer.
PI3Kδ-IN-25
PI3Kδ-IN-25
Copy Product Info😃Good
Catalog No. T212311
PI3Kδ-IN-25 is an orally active and selective PI3Kδ inhibitor with an IC50 of 2.1 nM. It exhibits IC50 values of 272, 285, and 1171 nM for PI3Kα, PI3Kγ, and PI3Kβ, respectively. In B16F10 cells, PI3Kδ-IN-25 inhibits the phosphorylation of AKTSer473, suppresses Treg cell proliferation, and downregulates the expression of PD-L1. In mouse models of B16F10 melanoma and Lewis lung cancer, PI3Kδ-IN-25 demonstrates anticancer activity by reducing tumor-infiltrating Treg cells and enhancing immune responses. This compound is applicable for research on cancers such as melanoma and lung cancer.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | PI3Kδ-IN-25 is an orally active and selective PI3Kδ inhibitor with an IC50 of 2.1 nM. It exhibits IC50 values of 272, 285, and 1171 nM for PI3Kα, PI3Kγ, and PI3Kβ, respectively. In B16F10 cells, PI3Kδ-IN-25 inhibits the phosphorylation of AKTSer473, suppresses Treg cell proliferation, and downregulates the expression of PD-L1. In mouse models of B16F10 melanoma and Lewis lung cancer, PI3Kδ-IN-25 demonstrates anticancer activity by reducing tumor-infiltrating Treg cells and enhancing immune responses. This compound is applicable for research on cancers such as melanoma and lung cancer. |
| Targets&IC50 | PI3Kδ:2.1 nM |
| In vitro | PI3Kδ-IN-25 (Compound 18) at 1 μM effectively inhibits PIK3CD (93.37%), PIK3CG (87.63%), and PIK3CA (107.38%), while showing moderate activity against RIPK2 (58.65%) and PIK3CB (42.68%). After a 96-hour exposure, PI3Kδ-IN-25 demonstrates anti-proliferative effects on Ramos, DOHH2, Hela, BxPC3, SGC7901, BGC823, MX-1, A375, and B16F10 cells with IC50 values of 18.11, 14.39, 29.51, 22.13, 15.81, 13.06, 25.43, 21.95, and 11.42 μM respectively, while exhibiting weaker activity on K562, HepG2, and MCF-7 cells with IC50 values greater than 50 μM. Additionally, PI3Kδ-IN-25 (1-10 μM, 5-30 minutes) inhibits AKT Ser473 phosphorylation, indicating blockage of the PI3K signaling pathway in B16F10 cells. At concentrations of 1-10 μM over 72 hours, PI3Kδ-IN-25 reduces the proportion of CD4/CD25/FOXP3+++ as well as IL-10 concentration in mIL-2 and hTGFβ-induced Treg cells; at 10 μM, it downregulates PD-L1 expression in B16F10 cells. |
| In vivo | PI3Kδ-IN-25 (Compound 18) administered orally at doses of 1-30 mg/kg twice daily, suppresses tumor growth by modulating the tumor microenvironment in both B16F10 and Lewis xenograft mouse models. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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