Powder: -20°C for 3 years
In solvent: -80°C for 2 years
AR-12 is an orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (<a href="/target/PDK" style="display: inline; color: #c13a36">PDK</a>1) with potential antineoplastic activity.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | $ 40.00 | |
5 mg | In stock | $ 47.00 | |
10 mg | In stock | $ 91.00 | |
25 mg | In stock | $ 146.00 | |
50 mg | In stock | $ 277.00 | |
100 mg | In stock | $ 498.00 | |
200 mg | In stock | $ 799.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 47.00 |
Description | AR-12 is an orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (PDK1) with potential antineoplastic activity. |
Targets&IC50 | PDK-1:5 μM |
Kinase Assay | PDK-1 Kinase Assay: This in vitro assay is performed using a PDK-1 kinase assay kit. This cell-free assay is based on the ability of recombinant PDK-1, in the presence of DMSO vehicle or OSU-03012, to activate its downstream serum- and glucocorticoid-regulated kinase which, in turn, phosphorylates the Akt/serum- and glucocorticoid-regulated kinase-specific peptide substrate RPRAATF with [γ-32P]ATP. The 32P-phosphorylated peptide substrate is then separated from the residual [γ-32P]-ATP by using P81 phosphocellulose paper and quantitated in a scintillation counter after three washes with 0.75% phosphoric acid. |
Cell Research | The effect of OSU-03012 on PC-3 cell viability is assessed by using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide assay in six replicates. Cells are grown in 10% FBS- supplemented RPMI 1640 in 96-well, flat-bottomed plates for 24 hours. They are exposed to various concentrations of OSU-03012 (0-10 μM) dissolved in DMSO (final concentration ≤0.1%) in 1% serum-containing RPMI 1640 for different time intervals (~72 hours). Controls receive DMSO vehicle at a concentration equal to that in OSU-03012-treated cells. The medium is removed and replaced by 200 μL of 0.5 mg/mL 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide in 10% FBS-containing RPMI 1640. The cells are incubated in the CO2 incubator at 37 °C for 2 hours. Supernatants are removed from the wells, and the reduced 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide dye is solubilized in 200 μL DMSO per well. Absorbance at 570 nm is determined by using a plate reader.(Only for Reference) |
Synonyms | Osu-03012, Osu 03012, AR-12 |
Molecular Weight | 460.46 |
Formula | C26H19F3N4O |
CAS No. | 742112-33-0 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
Ethanol: <1 mg/mL
H2O: <1 mg/mL
DMSO: 9 mg/mL (19.5 mM)
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Osu03012 742112-33-0 PI3K/Akt/mTOR signaling PDK Osu-03012 Osu 03012 AR-12 Inhibitor inhibitor inhibit