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

OSU-03012

OSU-03012 Structure
  • ₹0
  • Product name: OSU-03012
  • CAS: 742112-33-0
  • MF: C26H19F3N4O
  • MW: 460.45
  • EINECS:-0
  • MDL Number:MFCD12912272
  • Synonyms:OSU-03012, >=98%;OSU-03012 (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;OSU-03012 (AR-12);N/AAR-12; OSU03012; OSU 03012
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Properties

storage temp. :Store at -20°C
solubility :≥23 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
form :solid
color :White to off-white
CAS DataBase Reference :742112-33-0

Safety Information

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Description

Cyclooxygenase-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.

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