Drug intelligence / Profile preview

IC87114

Development stage
Preclinical
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Non-clinical (preclinical Research)
01

Overview

IC87114 is a **selective small molecule inhibitor of phosphoinositide 3-kinase delta (PI3Kδ)**, a class I phosphatidylinositol 3-kinase primarily expressed in leukocytes. It is an ATP-competitive, purine-quinazolin-based compound that displays strong selectivity for PI3Kδ, with an IC50 of approximately 0.5 μM and over 60-fold selectivity compared to other PI3K isoforms. IC87114 blocks PI3Kδ-mediated signaling, impacting cellular processes such as neutrophil chemotaxis, T cell function, and cytokine production. Preclinical studies demonstrate that IC87114 reduces inflammatory responses in models of asthma and allergic inflammation by lowering leukocyte recruitment, cytokine release (e.g., IL-4, IL-5, IL-13), and downstream Akt phosphorylation. IC87114 has also shown efficacy in vitro against cancer cell migration, including thyroid cancer, by inhibiting the PI3K/Akt pathway[1][3][4][7][10].

Other names
2-[(6-aminopurin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)quinazolin-4-one371242-69-2CHEMBL1213082CHEMBL-1213082CHEMBL 1213082UNII-9HC746B1KFUNII9HC746B1KFUNII 9HC746B1KF
02

Targets

PIK3CD (Phosphatidylinositol 3-kinase delta)

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