AMG319

SKU: orb1300494

Description

AMG319 is a potent and selective PI3Kδ inhibitor (IC50 = 18 nM) with >47-fold selectivity against other PI3K isoforms. This compound has been utilized in Phase 2 clinical studies and preclinical research for investigating hematological malignancies and immune disorders in both cellular and animal models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1608125-21-8
• MW: 385.4
• Purity: 99.24% (May vary between batches)
• Formula: C₂₁H₁₆FN₇
• SMILES: C[C@H](Nc1ncnc2[nH]cnc12)c1cc2ccc(F)cc2nc1-c1ccccn1
• Target: PI3K
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.19 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:71 mg/mL (184.22 mM);Ethanol:71 mg/mL (184.22 mM)

Bioactivity

• Target IC50:
  PI3Kα:33 μM|PI3Kβ:2.7 μM|PI3Kγ:850 nM|PI3Kδ:18 nM
• In Vivo:
  In female Lewis rats, AMG319 (3 mg/kg, p.o.) inhibits the KLH-induced inflammatory response by 88%. In the transgenic (IgMm) mice, AMG319 (, p.o.) inhibits in vivo pAKT with IC50 of 1.9 nM.
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• In Vitro:
  AMG319 inhibits anti-IgM/CD40L-induced B cell proliferation with IC50 of 8.6 nM and reduces pAkt level with IC50 of 1.5 nM. AMG319 also inhibits anti-IgD-induce CD-69 expression in HWB.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PI3K, PI3Kβ, PI3Kα, PI3Kγ, PI3Kδ, Phosphoinositide 3-kinase, Inhibitor, inhibit, AMG319, AMG-319, AMG 319

Compound Identifiers

PubChem CID

68947304