ERK-IN-3 benzenesulfonate (Synonyms: ERK-IN-3 benzenesulfonate) |
Catalog No.GC63459 |
Le benzènesulfonate ERK-IN-3 est un inhibiteur puissant et oralement actif de l'ERK. Le benzènesulfonate ERK-IN-3 inhibe ERK1/2 avec de faibles valeurs IC50 nM À un chiffre. Le benzènesulfonate ERK-IN-3 peut être utilisé pour la recherche sur les cancers provoqués par des mutations RAS.
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Cas No.: 2055597-39-0
Sample solution is provided at 25 µL, 10mM.
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).
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