Drug intelligence / Profile preview

PI-3065

Development stage
Preclinical
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral
01

Overview

PI-3065 is a potent and highly selective small molecule inhibitor of the p110δ isoform of phosphoinositide 3-kinase (PI3Kδ). It demonstrates an IC50 of 5 nM and a Ki of 1.5 nM for p110δ, maintaining over 70-fold selectivity against other PI3K family members, including the p110α, p110β, and p110γ isoforms. Developed as a research tool, PI-3065 has been utilized in preclinical oncology studies to investigate the role of PI3Kδ in tumor progression, apoptosis, and metastasis, particularly in hepatocellular carcinoma and breast cancer models. In research involving murine models of peripheral T-cell lymphoma (PTCL), PI-3065 was evaluated for therapeutic efficacy but failed to prolong survival, suggesting that PI3Kδ signaling may not be a primary driver in certain PTCL subtypes. The compound is currently available exclusively as a laboratory research chemical and is not approved for clinical use in humans.

Other names
CAS 955977-50-1CAS955977-50-1CAS-955977-50-1
02

Targets

PIK3CD (Phosphatidylinositol 3-kinase delta)

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