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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.
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Source | PLoS One (2016). Figure 6. AS-604850 |
| Method | CCRF-CEM cells | |
| Cell Lines | resazurin reduction assay | |
| Concentrations | 50 μM | |
| Incubation Time | 3 days | |
| Results | We treated these cells with a p110γ-specific inhibitor, AS-604850, at dosing appropriate for in vitro cell based assays, both alone and in combination with CP-751,871 antibody on the premise that AS-604850 would block p110γ and CP-751,871 would block IGF1R-dependent p110α/β/δ |
| 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 |
| Molecular Weight | 285.22 |
| Formula | C11H5F2NO4S |
| CAS Number | 648449-76-7 |
| Solubility (25°C) | DMSO 47 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PI3K Products |
|---|
| AS605240
AS-605240 is a potent and selective inhibitor of PI 3-kinase γ (PI3Kγ) with an IC50 of 8 nM. |
| BEZ235
BEZ235 (NVP-BEZ235) is a potent dual PI3K and mTOR inhibitor of p110α, p110γ, p110δ and p110β with IC50 of 4 nM, 5 nM, 7 nM and 75 nM, respectively. |
| BKM120 (Buparlisib)
BKM120 (NVP-BKM120) is a potent and highly specific oral pan-class I PI3K inhibitor. |
| GDC-0941 (Pictilisib)
GDC-0941 is a selective and potent inhibitor of Class I PI3K, p110a IC50=0.003uM, U87MG IC50=0.95μM. |
| AS-252424
AS-252424 is a furan-2-ylmethylene thiazolidinedione as a selective ATP-competitive PI3Kγ inhibitor with IC50 with 33 nM. |
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