Thursday, May 7, 2015

Drugs in Clinical Pipeline: Pimasertib

Pimasertib [N-[(2S)-2,3-dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)amino] isonicotinamide] is a novel, orally bioavailable small molecule inhibitor that binds to an allosteric site in close proximity to the adenosine triphosphate binding site of MEK1/2 with IC50 value of 5.2 nM.

The activity of Pimasertib is as follows:

IC50 (MAP2K1/K2 enzyme assay) = 5.2 nM

Common Name: Pimasertib
Synonyms:  SAR245509; SAR-245509; SAR 245509; MSC1936369B; AS-703026; AS 703026; AS703026
IUPAC Name: (S)-N-(2,3-dihydroxypropyl)-3-((2-fluoro-4-iodophenyl)amino)isonicotinamide
CAS Number: 1236699-92-5
Mechanism of Action: Kinase Inhibitor; MEK 1/2 Inhibitors; MAP2K1/K2 Inhibitors
Indication: Various Cancers; Solid Tumors
Development Stage: Phase I
Company: Merck Serono