AM-8508
AM-8508 is an orally bioactive PI3Kδ inhibitor with an IC50 of 0.016 μM. AM-8508 selectively inhibits PI3Kδ, thereby blocking AKT phosphorylation mediated by the B cell receptor. AM-8508 suppresses the formation of antigen-specific IgG and IgM in rats immunized with keyhole limpet hemocyanin. AM-8508 can be used for the research of inflammatory diseases.
For research use only. We do not sell to patients.
- CAS No.: 1338483-67-2
- Formula: C19H15FN8
- Molecular Weight:374.38
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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 0.016 μM (IC50) |
PI3Kα 58.2 μM (IC50) |
PI3Kβ 1.78 μM (IC50) |
PI3Kγ 5.8 μM (IC50) |
AM-8508 (Compound 1) potently and selectively inhibits the PI3Kδ subtype with an IC50 of 0.016 μM, exhibiting 3638-fold, 111-fold and 363-fold selectivity over PI3Kα (IC50 = 58.2 μM), PI3Kβ (IC50 = 1.78 μM) and PI3Kγ (IC50 = 5.8 μM), respectively[1].
AM-8508 potently inhibits anti-IgM/CD40L-induced proliferation of human B cells, with an IC50 of 0.0064 μM[1].
AM-8508 potently inhibits anti-IgM-induced AKT phosphorylation in mouse splenic B cells, with an IC50 of 0.0046 μM[1].
AM-8508 potently inhibits anti-IgD-induced AKT phosphorylation in human whole blood, with a total IC50 of 0.0027 μM and a free IC50 of 1.0 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AM-8508 (0.003-0.3 mg/kg, p.o., once daily for 10 consecutive days) dose-dependently suppresses the keyhole limpet hemocyanin (KLH)-induced humoral immune response in female Lewis rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:IgMₘ transgenic mice[1]
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Dosage:0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
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Administration:p.o.; single dose
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Result:Showed dose-dependent inhibition of AKT phosphorylation in anti-IgM stimulated B cells isolated from whole blood and spleen compartments.
Calculated ED50 values for inhibition of pAKT were <0.03 mg/kg in whole blood and <0.03 mg/kg in splenocytes.
Observed statistically significant inhibition relative to the control group at all tested doses.
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Animal Model:Lewis rats (female)[1]
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Dosage:0.003 mg/kg; 0.01 mg/kg; 0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg
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Administration:p.o.; once daily; 10 days
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Result:Inhibited KLH-specific IgG in a dose-dependent manner, with statistically significant inhibition relative to the control group at the 0.1 mg/kg (67% reduction) and 0.3 mg/kg (77% reduction) doses.
Showed a dose-dependent reduction in KLH-specific IgM, but this effect was not statistically significant.
Calculated ED50 values were 0.08 mg/kg for IgG inhibition and 0.12 mg/kg for IgM inhibition.
Chemical Information
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CAS No. 1338483-67-2
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Molecular Weight 374.38
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Formula C19H15FN8
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SMILES
[C@H](NC=1C(C#N)=C(N)N=CN1)(C)C=2N(C=3C(N2)=CC=C(F)C3)C=4C=CC=NC4
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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)
AM-8508 Related Classifications
HY-120116 Related Classifications
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