Drug intelligence / Profile preview

KU63794

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

Overview

KU63794 is a potent and selective ATP-competitive inhibitor of the mechanistic target of rapamycin (mTOR). Unlike allosteric inhibitors such as rapamycin, KU63794 targets the active site of the kinase, allowing it to inhibit both mTOR complex 1 (mTORC1) and mTOR complex 2 (mTORC2). This dual inhibition results in the suppression of p70S6K phosphorylation and the complete abrogation of Akt phosphorylation at Ser473. Developed by KuDOS Pharmaceuticals, KU63794 is widely used as a pharmacological tool to study mTOR signaling and its role in various cancers, including pancreatic ductal adenocarcinoma. Research indicates that while it effectively blocks mTOR signaling, it may trigger compensatory feedback loops, such as the activation of the ERK pathway.

02

Targets

PI3K (Phosphoinositide-3-kinase regulatory subunit 6)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)p38 mitogen-activated protein kinase (p38 MAPK)mTOR (Mammalian target of rapamycin kinase)

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