An inhibitor of ERK dimerization (IC50 = ~0.5 μM for disruption of EGF-induced co-immunoprecipitation of ERK); has no effect on ERK phosphorylation or kinase activity (IC50s = >10 μM); inhibits cell growth in a panel of melanoma and colorectal cancer cell lines (IC50s = 150-400 nM); inhibits ERK dimerization in liver extract and tumor tissue and inhibits tumor progression in an A375 mouse xenograft model at 15 mg/kg; reduces tumor growth in a BRAF mutant colorectal cancer PDX mouse model

DEL-22379 – 5 mg

Brand:
Cayman
CAS:
181223-80-3
Storage:
-20
UN-No:
Non-Hazardous - /

DEL-22379 is an inhibitor of ERK dimerization that disrupts EGF-induced co-immunoprecipitation of ERK tagged with hemagglutinin (HA) or FLAG epitopes with an IC50 value of approximately 0.5 μM without affecting ERK phosphorylation or kinase activity (IC50s = >10 μM).{37660} It inhibits cell growth in a panel of melanoma and colorectal cancer cell lines (IC50s = 150-400 nM). DEL-22379 (15 mg/kg, i.p.) inhibits ERK dimerization in liver extract and tumor tissue and inhibits tumor progression in an A375 mouse xenograft model. It also reduces tumor growth in a BRAF mutant colorectal cancer patient-derived xenograft (PDX) mouse model.  

 

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Description

An inhibitor of ERK dimerization (IC50 = ~0.5 μM for disruption of EGF-induced co-immunoprecipitation of ERK); has no effect on ERK phosphorylation or kinase activity (IC50s = >10 μM); inhibits cell growth in a panel of melanoma and colorectal cancer cell lines (IC50s = 150-400 nM); inhibits ERK dimerization in liver extract and tumor tissue and inhibits tumor progression in an A375 mouse xenograft model at 15 mg/kg; reduces tumor growth in a BRAF mutant colorectal cancer PDX mouse model

Formal name: N-[2,3-dihydro-3-[(5-methoxy-1H-indol-3-yl)methylene]-2-oxo-1H-indol-5-yl]-1-piperidinepropanamide

Synonyms: 

Molecular weight: 444.5

CAS: 181223-80-3

Purity: ≥98% (mixture of rotamers)

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling

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