An inhibitor of ERK dimerization
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Product Categories

Product Type

Biochemicals

Research Area

Cancer
Cell Signaling
ERK/MAPK Signaling

DEL-22379

Item No. 22433

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2,3-dihydro-3-[(5-methoxy-1H-indol-3-yl)methylene]-2-oxo-1H-indol-5-yl]-1-piperidinepropanamide
CAS Number
181223-80-3
Molecular Formula
C26H28N4O3
Formula Weight
444.5
Purity
≥98% (mixture of rotamers)
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:3): 0.25 mg/mlEthanol: slightly soluble
λmax
224, 276, 405 nm
SMILES
O=C(NC1=CC(/C(C(N2)=O)=C/C3=CNC4=C3C=C(OC)C=C4)=C2C=C1)CCN5CCCCC5
InChi Code
InChI=1S/C26H28N4O3/c1-33-19-6-8-23-20(15-19)17(16-27-23)13-22-21-14-18(5-7-24(21)29-26(22)32)28-25(31)9-12-30-10-3-2-4-11-30/h5-8,13-16,27H,2-4,9-12H2,1H3,(H,28,31)(H,29,32)/b22-13-
InChi Key
INQUULPXCZAKMS-XKZIYDEJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $107

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    10 mg

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    25 mg

    $424

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    50 mg

    $794

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    Cayman Chemical
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    Product Description

    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).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Herrero, A., Pinto, A., Colón-Bolea, P., et al. Small molecule inhibition of ERK dimerization prevents tumorigenesis by RAS-ERK pathway oncogenes. Cancer Cell 28(2), 170-182 (2015).