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Ref Type Journal Article
PMID (20797855)
Authors Venkatesan AM, Chen Z, dos Santos O, Dehnhardt C, Santos ED, Ayral-Kaloustian S, Mallon R, Hollander I, Feldberg L, Lucas J, Yu K, Chaudhary I, Mansour TS
Title PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor.
Journal Bioorganic & medicinal chemistry letters
Vol 20
Issue 19
Date 2010 Oct 1
URL
Abstract Text A series of mono-morpholino 1,3,5-triazine derivatives (8a-8q) bearing a 3-oxa-8-azabicyclo[3.2.1]octane were prepared and evaluated for PI3-kinase/mTOR activity. Replacement of one of the bis-morpholines in lead compound 1 (PKI-587) with 3-oxa-8-azabicyclo[3.2.1]octane and reduction of the molecular weight yielded 8m (PKI-179), an orally efficacious dual PI3-kinase/mTOR inhibitor. The in vitro activity, in vivo efficacy, and PK properties of 8m are discussed.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
PKI-179 PKI-179 1 0
Drug Name Trade Name Synonyms Drug Classes Drug Description
PKI-179 mTOR Inhibitor 51 PI3K Inhibitor (Pan) 40 PKI-179 is a dual PI3K/mTORC1/2 inhibitor that inhibits the PI3K/mTOR signaling pathway, thereby inducing apoptosis and inhibiting tumor growth (PMID: 20797855, PMID: 26500112).
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
PIK3CA mut PTEN loss prostate cancer sensitive PKI-179 Preclinical - Cell culture Actionable In a preclinical study, PKI-179 inhibited growth of prostate cancer cells harboring PIK3CA mutations and PTEN loss in culture (PMID: 20797855). 20797855