Astex ERK inhibitor X

Names

[ CAS No. ]:
2095719-90-5

[ Name ]:
Astex ERK inhibitor X

Biological Activity

[Description]:

ERK1/2 inhibitor 1 is a potent, orally bioavailable ERK1/2 inhibitor, showing 60% inhibition at 1 nM and an IC50 of 3.0 nM against ERK1 and ERK2, respectively[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> MAPK/ERK Pathway >> ERK

Signaling Pathways >> Stem Cell/Wnt >> ERK

[Target]

ERK2:3.0 nM (IC50)

ERK1

[In Vitro]

ERK1/2 inhibitor 1 (Compound 27) shows excellent antiproliferative potency with IC50s of 4.9 and 7.5 nM in A375 and Colo205 cells, respectively[1].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₉H₃₂ClN₅O₄

[ Molecular Weight ]:
550.05

[ Storage condition ]:
-20°C

Astex ERK inhibitor X

Names

Biological Activity

Chemical & Physical Properties

Related Compounds