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Version: 17.06d (Release date: 2017-06-26)
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PDK1 Inhibitor AR-12 (Code C88271)

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Terms & Properties

Preferred Name: PDK1 Inhibitor AR-12

Definition: An orally bioavailable, small-molecule, celecoxib-derived inhibitor of phosphoinositide-dependent kinase-1 (PDK1) with potential antineoplastic activity. Devoid of any COX inhibiting activity, PDK1 inhibitor AR-12 binds to and inhibits the phosphorylation of 3-phosphoinositide-dependent kinase-1 (PDK-1).; subsequently, the phosphorylation and activation of the serine/threonine protein kinase Akt (protein kinase B or PKB) is inhibited, which may result in inhibition of the PI3K/Akt signaling pathway, inhibition of tumor cell proliferation, and the induction of tumor cell apoptosis. In addition, this agent appears to induce the activity of protein kinase R-like endoplasmic reticulum kinase (PERK), which plays a key role in the endoplasmic reticulum stress pathway. Activation and dysregulation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

Label: PDK1 Inhibitor AR-12

NCI Thesaurus Code: C88271 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C1569671  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
AR-12
PDK1 Inhibitor AR-12

External Source Codes: 
CAS Registry Number 742112-33-0 (see NLM ChemIDplus info)
FDA UNII Code EX3O2Q61UV
PDQ Closed Trial Search ID 655950
PDQ Open Trial Search ID 655950 (check for NCI PDQ open clinical trial info)
UMLS CUI C1569671

Other Properties:
     Name Value (qualifiers indented underneath)
code C88271
Contributing_Source FDA
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C88271

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