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ERK-IN-3 benzenesulfonate

ERK-IN-3 benzenesulfonate
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 IC 50 values. ERK-IN-3 benzenesulfonate can be used for the research of cancers driven by RAS mutations.
Catalog No. T39453Cas No. 2055597-39-0

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ERK-IN-3 benzenesulfonate

Catalog No. T39453Cas No. 2055597-39-0

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 IC 50 values. ERK-IN-3 benzenesulfonate can be used for the research of cancers driven by RAS mutations.
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Product Introduction

Bioactivity
Description
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 IC 50 values. ERK-IN-3 benzenesulfonate can be used for the research of cancers driven by RAS mutations.
In vitro
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].
In vivo
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].
Chemical Properties
Molecular Weight632.11
FormulaC28H31ClFN7O5S
Cas No.2055597-39-0
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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