ERK-IN-3 is a potent and orally active inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 can be used for the research of cancers driven by RAS mutations.
IC50&Target
ERK1
ERK2
体外研究
ERK-IN-3 inhibits the phosphorylation of ERK1/2 substrates such as RSK1, FRA1, and Elk1 in various cell lines.
ERK-IN-3 showes single-digit nanomolar antiproliferative activity that is selective for MAPK-pathway dependent cancer cell lines.
体内研究
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.
分子式
C22H25ClFN7O2
分子量
473.93
CAS号
2055597-12-9
运输条件
Room temperature in continental US; may vary elsewhere.