Ligand id: 5665

Name: selumetinib

Structure and Physico-chemical Properties

2D Structure
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Calculated Physico-chemical Properties
Hydrogen bond acceptors 4
Hydrogen bond donors 3
Rotatable bonds 7
Topological polar surface area 88.41
Molecular weight 456
XLogP 3.7
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Selumetinib is being investigated for the treatment of various types of cancer, such as non-small cell lung cancer (NSCLC) and AIDS-related Kaposi's sarcoma. Click here to view's list of registered selumetinib trials. In April 2015, the US FDA granted selumetinib orphan drug status as a treatment for uveal melanoma.
Mechanism Of Action and Pharmacodynamic Effects
Selumetinib inhibits the MAPK kinases, MEK1 and MEK2 [4]. These kinases act in the MAPK/ERK pathway, downstream of BRAF and KRAS, two additional kinases which have been shown to carry activating mutations in some cancers [1]. Inhibition of MEK1/2 reduces abberant signalling in the growth factor-responsive MAPK/ERK signalling pathway in such cancer cells, and thereby reduces tumour growth.