ASN007 (ERK-IN-3) is a potent and orally active inhibitor of ERK . ASN007 inhibits ERK1/2 with low single-digit nM IC 50 values. ASN007 can be used for the research of cancers driven by RAS mutations
In Vitro
ASN007 (ERK-IN-3) inhibits the phosphorylation of ERK1/2 substrates such as RSK1, FRA1, and Elk1 in various cell lines. ASN007 showes single-digit nanomolar antiproliferative activity that is selective for MAPK-pathway dependent cancer cell lines. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
ASN007 (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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.