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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 (<a href="/target/PDK" style="display: inline; color: #c13a36">PDK</a>1) with potential antineoplastic activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Osu03012, CAS 742112-33-0

Pack Size	Availability	Price/USD
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

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Purity: 98.47%

Purity: 97.95%

Purity: 99.22%

Purity: 98.52%

Purity: 98.47%

Biological Description

Chemical Properties

Storage & Solubility Information

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

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

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 )

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. Zhang Yajuan, et al. Macrophage-Associated PGK1 Phosphorylation Promotes Aerobic Glycolysis and Tumorigenesis[J]. Molecular cell. 2018 Jul 19;71(2):201-215.e7.

Citations

1. Zhang Y, Yu G, Chu H, et al. Macrophage-Associated PGK1 Phosphorylation Promotes Aerobic Glycolysis and Tumorigenesis. Molecular Cell. 2018, 71(2): 201-215. e7

Related compound libraries

This product is contained In the following compound libraries：

Orally Active Compound Library Autophagy Compound Library Anti-Liver Cancer Compound Library Apoptosis Compound Library Glycometabolism Compound Library Antidepressant Compound Library Anti-Cancer Active Compound Library Target-Focused Phenotypic Screening Library Anti-Breast Cancer Compound Library Anti-Cancer Compound Library

Related Products

Related compounds with same targets

δ-Tocotrienol BX517 PS 48 PS47 Osu03012 GSK2334470 Dehydroabiethylamine VER-246608

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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.

Keywords

Osu03012 742112-33-0 PI3K/Akt/mTOR signaling PDK Osu-03012 Osu 03012 AR-12 Inhibitor inhibitor inhibit

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