PI3Kδ/γ-IN-2
PI3Kδ/γ-IN-2 is a potent PI3Kδ and PI3Kγ dual inhibitor with IC50s of 1 nM and 4.3 nM, respectively. PI3Kδ/γ-IN-2 has favorable oral bioavailability. PI3Kδ/γ-IN-2 has potential for battling B-cell malignancies.
For research use only. We do not sell to patients.
- CAS No.: 2412195-89-0
- Formula: C25H21ClN8O
- Molecular Weight:484.94
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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 1 nM (IC50) |
PI3Kγ 4.3 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SU-DHL-6 | GI50 |
33 nM
Compound: 26
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Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
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[PMID: 32078865] |
PI3Kδ/γ-IN-2 (compound 26) (0-5 μM; 72 hours) exhibits remarkable anti-proliferative activity against SU-DHL-6 cell line[1].
PI3Kδ/γ-IN-2 (10-100 nM; 2 hours) down-regulates both phos-Akt (Ser473) and phos-S6K1 (Thr389), and decreases the phosphoration of Akt and S6K1 at 30 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SU-DHL-6[1]
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Concentration:0-5 μM
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Incubation Time:72 hours
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Result:Exhibited remarkable anti-proliferative activity against SU-DHL-6 cell line with GI50 value of 33 nM.
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Cell Line:SU-DHL-6[1]
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Concentration:10, 30 and 100 nM
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Incubation Time:2 hours
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Result:Down-regulated both phos-Akt (Ser473) and phos-S6K1 (Thr389) in a dose-dependent manner, and exhibited a more significant decrease in the phosphoration of Akt and S6K1 at 30 nM.
Pharmacokinetic Parameters of PI3Kδ/γ-IN-2 in male Sprague-Dawley rats[1].
| IV (5 mg/kg) | PO (5 mg/kg) | |
| T1/2 (h) | 3.0 ± 0.3 | 14.3 ± 4.4 |
| AUC0-t (h·μg/L) | 5576 ± 606 | 4878 ± 694 |
| VSS (L/kg) | 3.9 ± 0.6 | |
| CL (L/h/kg) | 0.9 ± 0.1 | |
| F (%) | 87.5 ± 12.5 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats[1]
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Dosage:5 mg/kg
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Administration:PO or IV; single (Pharmacokinetics Analysis)
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Result:Exhibited a high plasma exposure (AUC0-t = 4878 ± 694 h μg/L), an attractive oral bioavailability (F% = 87.5 ± 12.5), and an acceptable clearance (CL = 0.9 ± 0.1 L/h/kg).
Chemical Information
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CAS No. 2412195-89-0
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Molecular Weight 484.94
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Formula C25H21ClN8O
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SMILES
N#CC1=C(N=C(N=C1N2CC3(C[C@H]2C4=NC5=CC=CC(Cl)=C5C(N4C6=CC=CC=C6)=O)CC3)N)N
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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/γ-IN-2 Related Classifications
HY-146789 Related Classifications
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