AMG319

Catalog No.S7813

AMG319 Chemical Structure

Molecular Weight(MW): 385.4

AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.

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Biological Activity

Description AMG319 is a potent and selective PI3Kδ inhibitor with IC50 of 18 nM, >47-fold selectivity over other PI3Ks. Phase 2.
Targets
PI3Kδ [1]
()
PI3Kγ [1]
18 nM 850 nM
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. [1]

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. [1]

Protocol

Kinase Assay:[1]
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PI3K Enzyme Assays:

A PI3K Alphascreen assay is used to measure the activity of a panel of four phosphoinositide 3-kinases: PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ. Enzyme reaction buffer is prepared using sterile water and 50 mM Tris-HCl, pH 7, 14 mM MgCl2, 2 mM sodium cholate, and 100 mM NaCl. 2 mM DTT is added fresh on the day of the experiment. The Alphascreen buffer is made using sterile water and 10 mM Tris-HCl, pH 7.5, 150 mM NaCl, 0.10% Tween 20, and 30 mM EDTA. Then 1 mM DTT is added fresh on the day of the experiment. Compound source plates used for this assay are 384-well Greiner clear polypropylene plates containing test compounds at 5 mM and diluted 1:2 over 22 concentrations. Columns 23 and 24 contained only DMSO, as these wells comprised the positive and negative controls, respectively. Source plates are replicated by transferring 0.5 μL per well into 384-well Optiplates. Each PI3K isoform is diluted in enzyme reaction buffer to 2× working stocks. PI3Kα is diluted to 1.6 nM, PI3Kβ is diluted to 0.8 nM, PI3Kγ is diluted to 15 nM, and PI3Kδ is diluted to 1.6 nM. PI(4,5)P2 is diluted to 10 μM, and ATP was diluted to 20 μM. This 2× stock is used in the assays for PI3Kα and PI3Kβ. For assay of PI3Kγ and PI3Kδ, PI(4,5)P2 is diluted to 10 μM and ATP was diluted to 8 μM to prepare a similar 2× working stock. Alphascreen reaction solutions are made using beads from the anti-GST Alphascreen kit. Two 4× working stocks of the Alphascreen reagents are made in Alphascreen reaction buffer. In one stock, biotinylated-IP4 is diluted to 40 nM and streptavadin-donor beads are diluted to 80 μg/mL. In the second stock, PIP3-binding protein is diluted to 40 nM and anti-GST-acceptor beads were diluted to 80 μg/mL. As a negative control, a reference inhibitor at a concentration ≫Ki (40 μM) is included in column 24 as a negative (100% inhibition) control. Using a 384-well Multidrop, 10 μL/well of 2× enzyme stock is added to columns 1–24 of the assay plates for each isoform. An amount of 10 μL/well of the appropriate substrate 2× stock (containing 20 μM ATP for the PI3Kα and -β assays and containing 8 μM ATP for the PI3Kγ and -δ assays) is then added to columns 1–24 of all plates. Plates are then incubated at room temperature for 20 min. In the dark, 10 μL/well of the donor bead solution is added to columns 1–24 of the plates to quench the enzyme reaction. The plates are incubated at room temperature for 30 min. Still in the dark, 10 μL/well of the acceptor bead solution is added to columns 1–24 of the plates. The plates are then incubated in the dark for 1.5 h. The plates are read on an Envision multimode plate reader using a 680 nm excitation filter and a 520–620 nm emission filter.
Animal Research:[1]
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  • Animal Models: Female Lewis rats
  • Formulation: 2% HPMC, 1% Pluronic F68, 10% Captisol, pH 2.0
  • Dosages: ~3 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 77 mg/mL (199.79 mM)
Ethanol 77 mg/mL (199.79 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 385.4
Formula

C21H16FN7

CAS No. 1608125-21-8
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02540928 Recruiting Human Papillomavirus (HPV)|Positive or Negative Head and Neck Squamous Cell Carcinoma (HNSCC) of the Hypopharynx, Oropharynx, Oral Cavity, Supraglottis or Larynx Cancer Research UK October 2015 Phase 2
NCT01300026 Completed Cancer|Chronic Lymphocytic Leukemia|Diffuse Large Cell Lymphoma|Hematologic Malignancies|Hematology|Leukemia|Low Grade Lymphoma|Lymphoma|Mantle Cell Lymphoma|Non-Hodgkins Lymphoma|Oncology|Oncology Patients|T Cell Lymphoma|Tumors Amgen April 2011 Phase 1

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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