ChemicalBook Product Catalog Biochemical Engineering Inhibitors PI3K / Akt / mTOR PDK-1 inhibitors OSU-03012

OSU-03012

OSU-03012 Basic information
Product Name:OSU-03012
Synonyms:OSU-03012, >=98%;OSU-03012 (AR-12);AR-12;2-amino-N-(4-(5-(phenanthren-2-yl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)acetamide;2-Amino-N-[4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]acetamide OSU-03012;N/AAR-12;OSU-03012;2-Amino-N-[4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]acetamide
CAS:742112-33-0
MF:C26H19F3N4O
MW:460.45
EINECS:
Product Categories:Inhibitors;Inhibitor of phosphoinositide-dependent kinase-1.;Akt;mTOR;PI3K
Mol File:742112-33-0.mol
OSU-03012 Structure
OSU-03012 Chemical Properties
storage temp. Store at -20°C
solubility ≥23 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
form solid
CAS DataBase Reference742112-33-0
Safety Information
MSDS Information
OSU-03012 Usage And Synthesis
DescriptionCyclooxygenase-2 (COX-2) appears to play a significant role in the development and progression of cancer and COX-2 inhibitors such as celecoxib exhibit anti-cancer activity. OSU03012 is an analog of celecoxib that exhibits anti-cancer activity in a COX-2-independent manner via inhibition of the phosphatidyl inositol-3-kinase/Akt pathway. It has an IC50 value of 5 μM for inhibition of 3-phosphoinositide-dependent kinase-1, and therefore Akt activation, with no measurable COX-2 inhibition up to 50 μM. OSU03012 is a potent inhibitor of tumor cell growth with an average inhibitory concentration of 1.1 μM across a panel of 60 cancer cell lines. It does not inhibit signal transduction through the mitogen-activated protein kinase (MAPK) pathway. OSU03012 induces apoptosis of chronic lymphocytic leukemia cells independent of bcl-2 overexpression using both caspase-dependent and independent pathways.
UsesOSU 03012 is a PDK1 inhibitor and inducer of caspase and p53-independent apoptosis, also used in the development of anticancer agents by modification of novel immunosuppressant FTY720 and PDK1 inhibitor OSU-03012, compound for treating Alzheimers diseases.
DefinitionChEBI: A member of the class of pyrazoles that is N-[4-(pyrazol-1-yl)phenyl]glycinamide in which the pyrazole ring is substituted at positions 3 and 5 by trifluoromethyl and phenanthrene-2-yl groups respectively.
storageStore at -20°C
references[1] zhu j1, huang jw, tseng ph, yang yt, fowble j, shiau cw, shaw yj, kulp sk, chen cs. from the cyclooxygenase-2 inhibitor celecoxib to a novel class of 3-phosphoinositide-dependent protein kinase-1 inhibitors. cancer res. 2004 jun 15;64(12):4309-18.
[2] lee tx1, packer md, huang j, akhmametyeva em, kulp sk, chen cs, giovannini m, jacob a, welling db, chang ls. growth inhibitory and anti-tumour activities of osu-03012, a novel pdk-1 inhibitor, on vestibular schwannoma and malignant schwannoma cells. eur j cancer. 2009 jun;45(9):1709-20.
OSU-03012 Preparation Products And Raw materials
BEZ235 (NVP-BEZ235, Dactolisib) 1H-Imidazole-4-carboxylicacid,2-amino-,ethylester(9CI) (2R,3S/2S,3R)-3-(4-Chloro-5-fluoro-6-pyrimidinyl)-2-(2,4-difluorophenyl)butan-2-ol hydrochloride 2-AMino-4-chloro-6-MethylpyriMidine-5-carbonitrile L-Alanyl-L-Glutamine impurity 25 2-AMINO-4-TRIFLUOROPYRIMIDINE-5-BORONIC ACID PINACOL ESTER BX-795 Dasatinib 2-AMino-6-broMo-5,6-dihydro-7(4H)-benzothiazolone Axitinib 2-Amino-3-bromo-6-chloropyrazine BX-912 Sildenafil citrate
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