ERK2-IN-6

ERK2-IN-6 (Compound 20) is a highly selective ERK1/2 inhibitor with an IC50 value of 7.9 nM for ERK2. ERK2-IN-6 inhibits the proliferation of BRAFV600E mutant cells (IC50=250 nM in A375 cells) . ERK2-IN-6 is promising for research of solid tumors, such as BRAF-mutated melanoma[1].

Product Specifications

CAS Number

[2095713-33-8]

UNSPSC

12352005

Target

ERK

Related Pathways

MAPK/ERK Pathway; Stem Cell/Wnt

Field of Research

Cancer

Smiles

O=C1C2=C(CN1CC(NC(C)(C)C3=CC=CC=C3)=O)C=CC(C4=NC(NC5CCOCC5)=NC=C4Cl)=C2

Molecular Formula

C28H30ClN5O3

Molecular Weight

520.02

References & Citations

[1]Heightman TD, et al. Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2. J Med Chem. 2018 Jun 14;61 (11) :4978-4992.