PI3K-IN-69
PI3K-IN-69 is an orally active PI3K inhibitor that inhibits class I PI3Kα/β/γ/δ and PI3K C2β kinase activity. PI3K-IN-69 has IC50 values of 0.87 nM, 0.70 nM, 1.6 nM, and 1.1 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ, respectively. PI3K-IN-69 blocks PI3K signaling and the phosphorylation of AKT, p70S6K, and S6RP, and is selective across a broad kinase panel. PI3K-IN-69 can be used for research on idiopathic pulmonary fibrosis and pulmonary fibrosis.
For research use only. We do not sell to patients.
- CAS No.: 2231399-62-3
- Formula: C26H24F2N4O5S
- Molecular Weight:542.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
PI3Kα 0.87 nM (IC50) |
PI3Kβ 0.7 nM (IC50) |
PI3Kγ 1.6 nM (IC50) |
PI3Kδ 1.1 nM (IC50) |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice (6-8 wk) were anesthetized with pentobarbital sodium (45 mg/kg) intraperitoneally. Then, inject 50 uL of Bleomycin
(3.0 U/kg) in to the trachea using a microsyringe and keep mice in orthostatic body position for 5 min.[1] -
Dosage:1 mg/kg
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Administration:p.o.; once daily; 18 consecutive days starting 10 days after Bleomycin
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Result:Decreased lung index and ameliorated bleomycin-induced deterioration in respiratory system resistance (Rrs), inspiratory capacity (IC), respiratory system elastance (Ers), and respiratory system compliance (Crs).
Suppressed bleomycin-induced elevations in α-SMA, hydroxyproline, and fibronectin in lung homogenates.
H&E staining showed attenuated inflammatory damage, and Masson staining showed reduced collagen fiber deposition.
Chemical Information
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CAS No. 2231399-62-3
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Molecular Weight 542.55
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Formula C26H24F2N4O5S
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SMILES
O=S(NC1=C(OC)N=CC(C2=CC(OCC3(COC3)C)=C4N=CN=C(C)C4=C2)=C1)(C5=CC=C(C=C5F)F)=O
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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)