An analog of celecoxib that inhibits PDK-1 (IC50 = 5 µM)

OSU03012 – 5 mg

Brand:
Cayman
CAS:
742112-33-0
Storage:
-20
UN-No:
Non-Hazardous - /

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.{11047} 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.{13637,13638,13639} 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.{13638} 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.{13638} It does not inhibit signal transduction through the mitogen-activated protein kinase (MAPK) pathway.{13639} OSU03012 induces apoptosis of chronic lymphocytic leukemia cells independent of bcl-2 overexpression using both caspase-dependent and independent pathways.{13637}  

 

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SKU: 10008005 - 5 mg Category:

Description

An analog of celecoxib that inhibits PDK-1 (IC50 = 5 µM), and therefore Akt activation, with no measurable COX-2 inhibition up to 50 µM; inhibits tumor cell growth (IC50s ~ 1.1 µM) across a panel of 60 cancer cell lines and induces apoptosis of chronic lymphocytic leukemia cells independent of bcl-2 overexpression using both caspase-dependent and independent pathways

Formal name: 2-amino-N-[4-[5-(2-phenanthrenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-acetamide

Synonyms: 

Molecular weight: 460.5

CAS: 742112-33-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Lipids|Fatty Acids||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway||Research Area|Lipid Biochemistry|Glycerophospholipids|Phosphatidyl Inositol Kinases & Phosphatases

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