DEL-22379

Catalog No.S7921 Batch:S792101

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Technical Data

Formula

C26H28N4O3
Molecular Weight 444.53 CAS No. 181223-80-3
Solubility (25°C)* In vitro DMSO 89 mg/mL (200.21 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description DEL-22379 is a water-soluble ERK dimerization inhibitor with IC50 of ∼0.5 μM.
Targets
ERK [1]
(in HEK293 cells)
0.5 μM
In vitro 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. [1]
In vivo DEL-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). [1]

Protocol (from reference)

Kinase Assay:[1]
  • ERK dimerization 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:[1]
  • Cell lines

    A panel of human cell lines harboring mutant BRAF (V600E) or RAS (Q61L or G12V)

  • Concentrations

    ~10 μM

  • Incubation Time

    48 h

  • Method

    Cellular proliferation is analyzed by Alamar blue assays. Briefly, Cells 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.
Animal Study:[1]
  • Animal Models

    Nude mice bearing A375 (BRAF mutant), CHL (WT/WT) or HCT116 (KRAS mutant) tumors

  • Dosages

    15 mg/kg, bid

  • Administration

    i.p.

Selleck's DEL-22379 has been cited by 4 publications

Epiregulin as an Alternative Ligand for Leptin Receptor Alleviates Glucose Intolerance without Change in Obesity [ Cells, 2022, 11(3)425] PubMed: 35159237
Epiregulin as an Alternative Ligand for Leptin Receptor Alleviates Glucose Intolerance without Change in Obesity [ Cells, 2022, 11(3)425] PubMed: 35159237
ERK phosphorylation disrupts the intramolecular interaction of capicua to promote cytoplasmic translocation of capicua and tumor growth [ Front Mol Biosci, 2022, 9:1030725] PubMed: 36619173
Systems Modeling Identifies Divergent Receptor Tyrosine Kinase Reprogramming to MAPK Pathway Inhibition [Claas AM, et al. Cell Mol Bioeng, 2018, 11(6):451-469] PubMed: 30524510

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.