barasertib

Ligand id: 7332

Name: barasertib

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 12
Hydrogen bond donors 5
Rotatable bonds 16
Topological polar surface area 184.63
Molecular weight 587.21
XLogP 2.78
No. Lipinski's rules broken 2

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
A Phase II/III trial assessing this compound in combination with low dose cytosine arabinoside (LDAC) in acute myeloid leukemia (AML) patients (NCT00952588) has been completed, as has a Phase I clinical trial in patients with advanced solid tumors [5]. Click here to see a full list of trials involving AZD1152 (barasertib) registered on ClinicalTrials.gov.
Mechanism Of Action and Pharmacodynamic Effects
Aurora B is required for the phosphorylation of histone H3, chromosome segregation and cytokinesis. Overexpression can lead to mitotic defects, making this a cogent cancer drug target [1-3]. Aurora B inhibition leads to aberrant mitosis and cell death [4].