ERK-IN-3 benzenesulfonate 是一种有效和具有口服活性的 ERK 抑制剂。 ERK-IN-3 benzenesulfonate 以较低的 IC50 值抑制 ERK1/2。 ERK-IN-3 benzenesulfonate 可用于研究由 RAS 突变驱动的癌症。
货号:ajcx35722
CAS:2055597-39-0
分子式:C28H31ClFN7O5S
分子量：632.11
溶解度:DMSO : 320 mg/mL (506.24 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

ERK-IN-3 benzenesulfonate is a potent and orally active inhibitor of ERK. ERK-IN-3 benzenesulfonate inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 benzenesulfonate can be used for the research of cancers driven by RAS mutations[1].

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].

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].

[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).