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AS-604850

Cat. No. M3368
AS-604850 Structure
Size Price Availability Quantity
5mg USD 80 In stock
25mg USD 230 In stock
100mg USD 750 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

AS-604850  is a selective, ATP-competitive PI3Kγ inhibitor with IC50 of 0.25, >20, >20, and 4.5 µM for the human recombinant γ, δ, β, and α isoforms, respectively. AS-604850  shows no notable activity against a wide array of protein kinases at 1 μM. AS-604850  inhibited MCP-1-mediated monocyte chemotaxis with an IC50 value of 21 µM and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 42.4 mg/kg.

Protocol
Cell Experiment
Cell lines HepG2 Ntcp and Huh7-Ntcp cells
Preparation method Treating hepatocyte cultures with diluent (DMSO), 25 μM TLC, 250 μM TCDC, 50 μM GCDC, or 50 ng/ml Fas for 2-4 hours HepG2-Ntcp and treating Huh7-Ntcp cells with DMSO, 20 μM TLC, 75 μM TCDC or GCDC, 200 μM etoposide or 200 ng/ml TNFa plus 28 ng/ml actinomycin D for 2-4 hours. Using fluorescent staining to determine morphologically the number of apoptotic cells expressing as % of cells . Apoptosis is confirmed in human cell lines by determination of caspase-3/-7 activity and in rat hepatocytes by detection of the 17 kDa proteolytic cleavage fragment of caspase-3 by immunoblotting; equal protein loading is monitored by immunoblotting for actin.
Concentrations 2.5 μM
Incubation time 2 - 4 hours
Animal Experiment
Animal models RANTES (0.5 mg/kg in 200 ml saline) or thioglycollate (40 ml/kg) are intraperitoneally injected to C3H mice to induce peritonitis mouse models
Formulation AS-604850 is dissolved in vehicle (0.5% carboxymethylcellulose/0.25% Tween-20) and adjusted the solution to 10 mL/kg of body weight.
Dosages 0, 1, 3, 10 or 30 mg/kg for RANTES, 10 mg/kg for thioglycollate
Administration Oral administration 30 or 15 minutes before injection of RANTES or thioglycollate
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 285.22
Formula C11H5F2NO4S
CAS Number 648449-76-7
Purity >99%
Solubility DMSO 50 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AS-604850 supplier, PI3K, inhibitors

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