1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. ERK
  3. ERK-IN-3

ERK-IN-3 

Cat. No.: HY-136579
Handling Instructions

ERK-IN-3 is a potent and oral inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 has the potential to be used to study cancers driven by RAS mutations.

For research use only. We do not sell to patients.

ERK-IN-3 Chemical Structure

ERK-IN-3 Chemical Structure

CAS No. : 2055597-12-9

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Description

ERK-IN-3 is a potent and oral inhibitor of ERK. ERK-IN-3 inhibits ERK1/2 with low single-digit nM IC50 values. ERK-IN-3 has the potential to be used to study cancers driven by RAS mutations.[1]

IC50 & Target[1]

ERK1

 

ERK2

 

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].

Molecular Weight

473.93

Formula

C₂₂H₂₅ClFN₇O₂

CAS No.

2055597-12-9

SMILES

O=C(C1=CN(C2=NC(NC3CCOCC3)=NC=C2C)C=N1)N[[email protected]@H](C4=CC(F)=CC(Cl)=C4)CN

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

ERK-IN-3ERKExtracellular signal regulated kinasesERK1/2cancerRASInhibitorinhibitorinhibit

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