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    DEL-22379
    DEL-22379

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0469
    CAS #: 181223-80-3Purity ≥98%

    Description: DEL-22379 is a novel, potent, selective, and water-soluble ERK (extracellular signal-related kinase 2) dimerization inhibitor with potential antitumor activity. It inhibits ERK with an IC50 of 0.5 μM. Unregulated RAS-ERK signaling is observed in nearly 50% of human malignancies and thus is an excellent target for intervention by antineoplasticagents. DEL-22379 inhibits ERK dimerization without affecting ERK phosphorylation, forestalls tumorigenesis driven by RAS-ERK pathway oncogenes. DEL-22379 readily binds to ERK2 with a Kd estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations. 

    References: Cancer Cell. 2015 Aug 10;28(2):170-82.

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    Molecular Weight (MW)444.53
    FormulaC26H28N4O3
    CAS No.181223-80-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 89 mg/mL (200.2 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: (E)-N-(3-((5-methoxy-1H-indol-3-yl)methylene)-2-oxoindolin-5-yl)-3-(piperidin-1-yl)propanamide

    InChi Key: INQUULPXCZAKMS-LPYMAVHISA-N

    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+

    SMILES Code: O=C(NC1=CC2=C(NC(/C2=C/C3=CNC4=C3C=C(OC)C=C4)=O)C=C1)CCN5CCCCC5

    SynonymsDEL 22379; DEL22379; DEL-22379.


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    In Vitro

    In vitro activity: DEL-22379 inhibits ERK dimerization without affecting its phosphorylation. In a panel of human cell lines harboring mutant BRAF (V600E) or RAS (Q61L or G12V), DEL-22379 shows potent anti-proliferative effects, and induces apoptosis.


    Kinase Assay: Compound screening is performed in HEK293T cells treated with the potential inhibitors (10 μM) for 30 min before EGF stimulation. Cellular lysates are tested for ERK dimerization by native PAGE and p-ERK evaluation of the potential positives. In vitro ERK dimerization is assayed using GST-MEK1 ΔN EE purified from bacteria, bound to glutathione sepharose beads, and incubated with 25 μg/ml of purified His-ERK2 plus increasing concentrations of DEL-22379. Western blotting, kinase assays, and luciferase assays are also performed. In silico docking of the DEL-22379 compound is carried out with the modeling tools provided by the OpenEye package (v. 2.1).


    Cell Assay: Cellular proliferation is analyzed by Alamar blue assays. Briefly, Cells (A panel of human cell lines harboring mutant BRAF (V600E) or RAS (Q61L or G12V)) are plated in 96-well plates at a density of 1000-2000 cells per well. Cells are treated with drug concentrations prepared by serial dilution ranging from 0.1 nM to 10 μM. 48 hr after drug treatment cells are exposed to Alamar Blue and the colorimetric change is measured at 570 and 600 nm. GI50 is estimated by nonlinear regression using GraphPad5 Prism Software.

    In VivoDEL-22379 (15 mg/kg, i.p.) prevents tumor growth and metastasis in mice bearing A375 (BRAF mutant) and HCT116 (KRAS mutant) tumors, but fails to prevent the formation of tumors in mice injected with CHL cells (WT/WT).
    Animal modelNude mice bearing A375 (BRAF mutant), CHL (WT/WT) or HCT116 (KRAS mutant) tumors
    Formulation & DosageDissolved in  1% DMSO; 15 mg/kg; i.p.
    References

    Cancer Cell. 2015 Aug 10;28(2):170-82.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    DEL-22379

    Identification and Validation of DEL-22379 as an ERK Dimerization Inhibitor. Cancer Cell. 2015 Aug 10;28(2):170-82.


    DEL-22379

    Antitumor Effects of DEL-22379 in Mice. Cancer Cell. 2015 Aug 10;28(2):170-82.


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