2055597-12-9

2055597-12-9 structure
2055597-12-9 structure
  • Name: ERK-IN-3
  • Chemical Name: ERK-IN-3
  • CAS Number: 2055597-12-9
  • Molecular Formula: C22H25ClFN7O2
  • Molecular Weight: 473.93
  • Catalog: Signaling Pathways MAPK/ERK Pathway ERK
  • Create Date: 2020-08-07 12:48:16
  • Modify Date: 2024-01-01 18:26:18
  • 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].

Name ERK-IN-3
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
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).

Molecular Formula C22H25ClFN7O2
Molecular Weight 473.93