amuvatinib

Ligand id: 7932

Name: amuvatinib

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 1
Rotatable bonds 5
Topological polar surface area 107.98
Molecular weight 447.14
XLogP 3.92
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
A Phase II clinical trial for small cell lung cancer (in combination with platinum-etoposide chemotherapy) was registered with ClinicalTrials.gov, but details have not been updated since 2012.
Mechanism Of Action and Pharmacodynamic Effects
Amuvatinib binds to and inhibits the activity of mutant forms of the stem cell factor receptor (c-Kit, mutant forms of which are often associated with tumor chemoresistance [2]), AXL [2] and other receptor tyrosine kinases, such as c-Met, Ret oncoprotein, and mutant forms of Flt3 and PDGFRα, which are frequently dysregulated in variety of tumours. In addition, this compound suppresses the induction of the DNA repair protein RAD51 recombinase (HGNC ID 9817), thereby potentiating the activities of DNA damage-inducing agents [3-4].