dactolisib

Ligand id: 7950

Name: dactolisib

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 6
Hydrogen bond donors 0
Rotatable bonds 3
Topological polar surface area 73.12
Molecular weight 469.19
XLogP 5.89
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Dactolisib (as BEZ235) is currently in Phase II clinical trial for pancreatic neuroendocrine tumors (NCT01628913; comparing with everolimus) and other advanced solid tumours (NCT01508104; in combination with everolimus).
Mechanism Of Action and Pharmacodynamic Effects
Dactolisib specifically inhibits PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway [1]. This action may trigger the translocation of cytosolic Bax (a proapoptotic Bcl2 family member) to the mitochondrial outer membrane, increasing mitochondrial membrane permeability, the result of which is apoptotic cell death.