PF-376304
PF-376304 is an orally active non-specific class I phosphoinositide 3-kinase (PI3K) inhibitor with an IC50 of 0.197 μM against PI3Kγ. PF-376304 induces dose-dependent glucose and lipid metabolic disorders in rats, causes rapid death at high doses, and leads to metabolic abnormalities that are self-reversible at low doses. PF-376304 is applicable to the research of metabolic and inflammatory diseases.
For research use only. We do not sell to patients.
- CAS No.: 851757-93-2
- Formula: C17H24N8O3
- Molecular Weight:388.43
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
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PI3Kγ 0.197 μM (IC50) |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley [Crl:CD(SD)BR] rats (6-8 weeks old; males 194-228 g, females 164-182 g)[1]
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Dosage:0, 30, 100, 300, 1000 mg/kg
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Administration:i.g.; daily; once daily for up to 7 consecutive days
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Result:Caused dose-dependent hyperglycemia, hyperinsulinemia, elevated serum corticosterone, reduced triglycerides, profound transient glucosuria, increased urinary β-hydroxybutyrate and creatine, and decreased citrate.
Led to rapid mortality within 72 h at doses ≥300 mg/kg , while metabolic effects mostly reversed within 72 h despite continued dosing at 100 mg/kg.
Chemical Information
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CAS No. 851757-93-2
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Molecular Weight 388.43
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Formula C17H24N8O3
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SMILES
O=C(NC1=NN=NN1)C2=CN=C(N=C2OC3CCCCCC3)N4CCOCC4
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
[1]. Robertson DG, et al. Metabonomic evaluation of metabolic dysregulation in rats induced by PF 376304, a novel inhibitor of phosphoinositide 3-kinase. Chem Res Toxicol. 2007;20(12):1871-1877. [Content Brief]
[2]. Ameriks MK, et al. Small molecule inhibitors of phosphoinositide 3-kinase (PI3K) delta and gamma. Curr Top Med Chem. 2009;9(8):738-53. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PF-376304 Related Classifications
HY-107387 Related Classifications
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