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Version: 17.06d (Release date: 2017-06-26)
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pan-PI3K/mTOR Inhibitor PQR309 (Code C111898)

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Terms & Properties

Preferred Name: pan-PI3K/mTOR Inhibitor PQR309

Definition: An orally bioavailable pan inhibitor of phosphoinositide-3-kinases (PI3K) and inhibitor of the mammalian target of rapamycin (mTOR), with potential antineoplastic activity. PI3K/mTOR kinase inhibitor PQR309 inhibits the PI3K kinase isoforms alpha, beta, gamma and delta and, to a lesser extent, mTOR kinase, which may result in tumor cell apoptosis and growth inhibition in cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to both chemotherapy and radiotherapy. As mTOR, a serine/threonine kinase downstream of PI3K, may also be activated independent of PI3K, this agent may potentially be more potent than an agent that inhibits either PI3K kinase or mTOR kinase. By inhibiting mTOR to a lesser extent than PI3K, PQR309 does not interfere with the mTOR-mediated negative feedback loop on PI3K signaling. Blocking the negative feedback loop would potentially increase PI3K signaling and decrease therapeutic efficacy.

Label: pan-PI3K/mTOR Inhibitor PQR309

NCI Thesaurus Code: C111898 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: CL454230  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
pan-PI3K/mTOR Inhibitor PQR309

External Source Codes: 
PDQ Closed Trial Search ID 753407
PDQ Open Trial Search ID 753407 (check for NCI PDQ open clinical trial info)

Other Properties:
     Name Value (qualifiers indented underneath)
code C111898
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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