ERK-IN-3 是一种有效的口服活性 ERK 抑制剂，以低 IC50 值抑制 ERK1/2，可用于研究由 Ras 突变驱动的癌症。

ERK-IN-3 is a potent and orally active inhibitor of ERK. It inhibits ERK1/2 with low single-digit nM IC50 values. It can be used for the research of cancers driven by RAS mutations.

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

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

2055597-12-9

C22H25ClFN7O2

473.94

ASN007 free base

DMSO:250 mg/mL (527.50 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years