Substance
ID:73432
Names and Identifiers
IUPAC name
5-bromo-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]benzamide
IUPAC Traditional name
C16H13BrF3IN2O4
Synonyms
PD318088
Registration numbers
CAS Number
Properties
Safety Information
Storage Condition
-20°C
Pharmacology Properties
Target
MEK
Product Information
Salt Data
Free Base
Molecule Details
Research Area
Description
Cancer
Biological Activity
Description
PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor.
Targets
MEK1/2
IC50
In Vitro
PD318088 is a small-molecule inhibitor of MEK1/2, which is an analog of PD184352, suggesting it might have substantial anti-proliferative activity against cancer cells, although no functional study of PD318088 is currently available. PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. Formation of the ternary complexes with PD318088 and MgATP results in moderate increases (to 140 nM) for the Kd monomer-dimer for both MEK1 and MEK2. The binding of PD318088 and MgATP to MEK1 also abolishes the formation of tetramers and higher-order aggregates. PD318088 and MgATP together increase the dimerization disassociation constant for MEK1 and MEK2 slightly from ~75 nM to ~140 nM, suggesting that the mechanism of inhibition for PD318088 is probably a result of localized conformational changes in the active site and not a global change in the overall structure. [1]
In Vivo
Clinical Trials
Features
Molecular Spectra
No Data Available
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References
• Ohren JF, et al. Nat Struct Mol Biol, 2004, 11(12), 1192-1197.