PI3Kδ-IN-25
PI3Kδ-IN-25 is an orally active selective PI3Kδ inhibitor (IC50 = 2.1 nM). PI3Kδ-IN-25 has IC50s of 272, 285, and 1171 nM for PI3Kα, PI3Kγ, and PI3Kβ, respectively. PI3Kδ-IN-25 inhibits AKT Ser473 phosphorylation, suppresses Treg cell proliferation, and downregulates PD-L1 expression in B16F10 cells. PI3Kδ-IN-25 exhibits anticancer effects in B16F10 melanoma and Lewis lung cancer mouse models by reducing tumor-infiltrating Treg cells and enhancing immune responses. PI3Kδ-IN-25 is potentially useful in the study of melanoma, lung cancer, and other cancers.
For research use only. We do not sell to patients.
- Formula: C26H28N6O4S2
- Molecular Weight:552.67
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PI3Kδ 2.1 nM (IC50) |
PI3Kδ-IN-25 (Compound 18) (1 μM) inhibits PIK3CD (93.37%), PIK3CG (87.63%) and PIK3CA (107.38%) while showing only moderate activity against RIPK2 (58.65%) and PIK3CB (42.68%)[1].
PI3Kδ-IN-25 (96 h) shows antiproliferative activities against Ramos, DOHH2, Hela, BxPC3, SGC7901, BGC823, MX-1, A375, B16F10 cells, with IC50s of 18.11, 14.39, 29.51, 22.13, 15.81, 13.06, 25.43, 21.95, 11.42 μM, respectively, shows weak antiproliferative activities against K562, HepG2, MCF-7 cells, with IC50s > 50 μM[1].
PI3Kδ-IN-25 (1-10 μM, 5-30 min) inhibits the phosphorylation of AKT at Ser473, suggesting an effective blockade of the PI3K signaling pathway in B16F10 cells[1].
PI3Kδ-IN-25 (1-10 μM, 72 h) reduces the ratio of CD4/CD25/FOXP3+++, the concentration of IL-10 in mIL-2 and hTGFβ induced Treg cells[1].
PI3Kδ-IN-25 (1-10 μM, 72 h) down-regulates of PD-L1 expression in B16F10 cells at 10 μΜ[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:B16F10 cells
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Concentration:1 μM, 3 μM, 10 μM
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Incubation Time:5 min, 15min, 30 min
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Result:Inhibited AKT phosphorylation at Ser473.
| Species | Dose | Route | Cmax | T1/2 | MRT0-t | MRT0-∞ | AUC0-t | AUC0-∞ | F |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 2128 ng/mL | 1.21 h | 0.45 h | 0.6 h | 432 ng·h/mL | 442 ng·h/mL | / |
| Mice[1] | 10 mg/kg | p.o. | 618 ng/mL | 1.68 h | 1.69 h | 1.99 h | 996 ng·h/mL | 1030 ng·h/mL | 23.3 % |
| Rat[1] | 1 mg/kg | i.v. | 3838 ng/mL | 0.77 h | 0.75 h | 0.81 h | 1387 ng·h/mL | 1404 ng·h/mL | / |
| Rat[1] | 10 mg/kg | p.o. | 1550 ng/mL | 1.87 h | 2.13 h | 2.46 h | 4433 ng·h/mL | 4598 ng·h/mL | 32.7 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B16F10 xenograft (1.8 × 106) mouse (male C57BL/6J) melanoma model [1]
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Dosage:1 mg/kg, 3 mg/kg, 30 mg/kg
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Administration:o.p., twice daily
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Result:Resulted significant inhibition of pAKT(S473) levels at a single oral dose of 30 mg/kg. Inhibited tumor growth, increased level of leukocytes, T cells, and especially CD8 T cells, elevated the expression of CD3, suppressed the expression of PD-1 and PD-L1.
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Animal Model:Lewis xenograft (1 × 106) mouse (male C57BL/6J) model[1]
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Dosage:1 mg/kg, 3 mg/kg, 30 mg/kg
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Administration:o.p., twice daily
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Result:Inhibited tumor growth, increased level of leukocytes, T cells, and especially CD8 T cells, decreased tumor-infiltrating Treg cells.
Chemical Information
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Molecular Weight 552.67
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Formula C26H28N6O4S2
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SMILES
O=C(N1CC[C@H](NC2=NC=NC3=C2C=C(C4=CC(NS(C5=CC=C(C=C5)C)(=O)=O)=C(N=C4)OC)S3)C1)CC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PI3Kδ-IN-25 Related Classifications
HY-175369 Related Classifications
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