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PI3K/Akt/mTOR signaling PDK Osu03012

Osu03012

Catalog No. T2466   CAS 742112-33-0
Synonyms: Osu 03012, Osu-03012, AR-12

AR-12 is an orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (PDK1) with potential antineoplastic activity.

Osu03012, CAS 742112-33-0
Pack Size Availability Price/USD Quantity
2 mg In stock 40.00
5 mg In stock 53.00
10 mg In stock 102.00
25 mg In stock 163.00
50 mg In stock 308.00
100 mg In stock 554.00
200 mg In stock 888.00
1 mL * 10 mM (in DMSO) In stock 53.00
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Biological Description
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Description AR-12 is an orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (PDK1) with potential antineoplastic activity.
Targets&IC50 PDK1 : ic50 5μM,  
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)
Cell lines: PC-3 cells
Animal Research
Animal Model: Huh7 tumor xenografts in BALB/c nude mice
Synonyms Osu 03012 , Osu-03012 , AR-12
Purity 99.22%
Molecular Weight 460.45
Formula C26H19F3N4O
CAS No. 742112-33-0

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 9 mg/mL (19.5 mM)

Ethanol: <1 mg/mL

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

0.5% methylcellulose+0.2% Tween 80: 30 mg/mL

Citations

References and Literature
1. Zhu J, et al. Cancer Res, 2004, 64(12), 4309-4318. 2. Yacoub A, et al. Mol Pharmacol, 2006, 70(2), 589-603. 3. Porchia LM, et al. Mol Pharmacol, 2007, 72(5), 1124-1131. 4. Gao M, et al. Cancer Res, 2008, 68(22), 9348-9357. 5. Tseng PH, et al. Blood, 2005, 105(10), 4021-4027. 6. To K, et al. Mol Pharmacol, 2007, 72(3), 641-652. 7. Lee TX, et al. Eur J Cancer, 2009, 45(9), 1709-1720.

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library PI3K-AKT-mTOR Compound Library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Fluorochemical Library Anti-cancer Metabolism Compound Library

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