ERK-IN-3

Names

[ CAS No. ]:
2055597-12-9

[ Name ]:
ERK-IN-3

Biological Activity

[Description]:

ERK-IN-3 is a potent and oral inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 has the potential to be used to study cancers driven by RAS mutations.[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> MAPK/ERK Pathway >> ERK

Signaling Pathways >> Stem Cell/Wnt >> ERK

[Target]

ERK1

ERK2

[In Vitro]

ERK-IN-3 inhibits the phosphorylation of ERK1/2 substrates such as RSK1, FRA1, and Elk1 in various cell lines[1]. ERK-IN-3 showes single-digit nanomolar antiproliferative activity that is selective for MAPK-pathway dependent cancer cell lines[1].

[In Vivo]

ERK-IN-3 (daily p.o.) inhibits tumor growth in multiple BRAF and KRAS mutant xenograft models in mice and was well tolerated at efficacious doses[1].

[References]

[1]. Sanjeeva PR, et, al. Abstract B150: ASN007, a novel oral ERK inhibitor, shows robust antitumor activity in RAS mutant cancer models. Molecular Cancer Therapeutics. 2018 Jan; 17(1).

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₅ClFN₇O₂

[ Molecular Weight ]:
473.93

ERK-IN-3

Names

Biological Activity

Chemical & Physical Properties

Related Compounds