RO5068760

RO5068760 is a potent, orally active and selective non-ATP-competitive MEK1/2 inhibitor with an IC50 of 0.025 μM for MEK1. RO5068760 significantly inhibits MAPK pathway activity, thereby inducing G1 cell cycle arrest and apoptosis to inhibit cancer cell growth. RO5068760 exhibits significant efficacy in a broad spectrum of tumors with aberrant MAPK pathway activation. RO5068760 can be used for melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer research[1].

Product Specifications

CAS Number

[947182-25-4]

UNSPSC

12352005

Target

Apoptosis; CDK; ERK; MEK; p38 MAPK; PARP

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics; MAPK/ERK Pathway; Stem Cell/Wnt

Field of Research

Cancer

Smiles

C[C@@H](C1=CC=CC=C1)[C@H](N2C([C@@H](C3=CC=C(C=C3)OC[C@H](O)CO)NC2=O)=O)C(NC4=C(C=C(C=C4)I)F)=O

Molecular Formula

C28H27FIN3O6

Molecular Weight

647.43

References & Citations

[1]Daouti S, et al. Preclinical in vivo evaluation of efficacy, pharmacokinetics, and pharmacodynamics of a novel MEK1/2 kinase inhibitor RO5068760 in multiple tumor models. Mol Cancer Ther. 2010 Jan;9 (1) :134-44.