Ligand id: 7954

Name: BMS-911543

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 9
Hydrogen bond donors 1
Rotatable bonds 7
Topological polar surface area 85.8
Molecular weight 432.24
XLogP 2.37
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
A multiple ascending dose Phase I/II clinical trial is underway in patients with myelofibrosis (NCT01236352).
Mechanism Of Action and Pharmacodynamic Effects
JAK2 is often upregulated or mutated in several types of cancer cells. This induces signal transducer and activator of transcription 3 (STAT3) activation and plays a key role in tumour cell proliferation and survival. Therfore, inhbition of JAK2 prevents this abberant activation of the JAK/STAT signaling cascade and may lead to an induction of tumour cell apoptosis and a decrease in cellular proliferation.