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Version: 17.06d (Release date: 2017-06-26)
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PI3K Delta/Gamma Inhibitor RP6530 (Code C113433)

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Terms & Properties

Preferred Name: PI3K Delta/Gamma Inhibitor RP6530

Definition: An orally active, highly selective, small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities. Upon administration, PI3K delta/gamma inhibitor RP6530 inhibits the PI3K delta and gamma isoforms and prevents the activation of the PI3K/AKT-mediated signaling pathway. This may lead to a reduction in cellular proliferation in PI3K delta/gamma-expressing tumor cells. In addition, this agent modulates inflammatory responses through various mechanisms, including the inhibition of both the release of reactive oxygen species (ROS) from neutrophils and tumor necrosis factor (TNF)-alpha activity. Unlike other isoforms of PI3K, the delta and gamma isoforms are overexpressed primarily in hematologic malignancies and in inflammatory and autoimmune diseases. By selectively targeting these isoforms, PI3K signaling in normal, non-neoplastic cells is minimally impacted or not affected at all, which minimizes the side effect profile for this agent.

Display Name: PI3K Delta/Gamma Inhibitor RP6530

Label: PI3K Delta/Gamma Inhibitor RP6530

NCI Thesaurus Code: C113433 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: CL458227  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
PI3K Delta/Gamma Inhibitor RP6530
RP-6530
RP6530
RP 6530

External Source Codes: 
PDQ Closed Trial Search ID 756264
PDQ Open Trial Search ID 756264 (check for NCI PDQ open clinical trial info)
NCI META CUI CL458227

Other Properties:
     Name Value (qualifiers indented underneath)
code C113433
Contributing_Source CTRP
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=C113433

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