Ligand id: 7952

Name: BMS-754807

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 10
Hydrogen bond donors 3
Rotatable bonds 7
Topological polar surface area 116.13
Molecular weight 461.21
XLogP 3.26
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
BMS-754807 has been assessed in Phase II clinical trials for HER2+ve breast cancer, alone or in combination with either trastuzumab or letrozole. A Phase II study for various other solid tumours in combination with cetuximab was terminated.
Mechanism Of Action and Pharmacodynamic Effects
IGF-1R is a receptor tyrosine kinase expressed on most tumour cells and is involved in mitogenesis, angiogenesis, and tumor cell survival. BMS-7548077 prevents IGF-1 binding to and signalling through the IGF-1R. Inhibition of IGF-1R-mediated signaling pathways may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis.