DS03090629

DS03090629 is an orally active MEK inhibitor that inhibits MEK activity in an ATP-competitive manner. DS03090629 exhibits high affinity for both MEK and phosphorylated MEK, with Kd values of 0.11 and 0.15 nM, respectively. It effectively inhibits the proliferation of BRAF-mutant overexpressing melanoma cell lines, with IC50 values of 74.3 and 97.8 nM for BRAF V600E and MEK1 F53L transfected A375 cells, respectively. DS03090629 holds potential value in the field of anti-melanoma therapy[1].

Product Specifications

UNSPSC

12352005

Target

MEK

Type

Reference compound

Related Pathways

MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ds03090629.html

Smiles

CC1=NNC2=CC(C3=CC=C(OC4=NC=CC(C)=N4)C=C3Cl)=CC(O[C@@H]5C[C@H](N)CCC5)=C21

Molecular Formula

C25H26ClN5O2

Molecular Weight

463.96

References & Citations

[1]Takano K, et al. Discovery of a Novel ATP-Competitive MEK Inhibitor DS03090629 that Overcomes Resistance Conferred by BRAF Overexpression in BRAF-Mutated Melanoma. Mol Cancer Ther. 2023 Mar 2;22 (3) :317-332.