1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. ERK

DEL-22379 

Cat. No.: HY-18932 Purity: 99.84%
Handling Instructions

DEL-22379 is an ERK dimerization Inhibitor. DEL-22379 readily binds to ERK2 with a Kd estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations. ERK2 dimerization is progressively inhibited with an IC50 of ~0.5 μM.

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

DEL-22379 Chemical Structure

DEL-22379 Chemical Structure

CAS No. : 181223-80-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 205 In-stock
Estimated Time of Arrival: December 31
5 mg USD 186 In-stock
Estimated Time of Arrival: December 31
10 mg USD 306 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1026 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

DEL-22379 is an ERK dimerization Inhibitor. DEL-22379 readily binds to ERK2 with a Kd estimated in the low micromolar range, though binding is detectable even at low nanomolar concentrations. ERK2 dimerization is progressively inhibited with an IC50 of ~0.5 μM.

IC50 & Target[1]

ERK2

0.5 μM (IC50)

In Vitro

DEL-22379 is an ERK dimerization inhibitor. DEL-22379 abolishes EGF-induced co-immunoprecipitation of ectopic ERK2 molecules tagged with hemagglutinin (HA) or FLAG epitopes, with an estimated half-maximal inhibitory concentration (IC50) of ~0.5 μM. DEL-22379 inhibits growth of tumor cells harboring RAS-ERK pathway oncogenes. The biological effects of DEL-22379 are investigated on tumor cells in culture. The cytostatic effects of DEL-22379 are compared to those of the MEK inhibitor PD-0325901 and the ERK kinase inhibitor SCH-772984, as reflected by their half-maximal growth inhibitory concentrations (GI50). Cell lines harboring mutant BRAF are the most sensitive to the three compounds. In comparison, wild-type (WT) cell lines for BRAF and RAS are the most resistant, and RAS mutant cells exhibit a range of sensitivities. In cells showing different oncogenic genotypes, distinct sensitivity to DEL-22379 can not be attributed to variations on its effects on dimerization, because DEL-22379 displays similar dimerization- and cytoplasmic signaling-inhibitory dose responses (IC50 of 150-400 nM) regardless of the genotype[1].

In Vivo

To test DEL-22379 antitumor effects, some of the aforementioned cell lines are xenografted into nude mice, and tumor growth is monitored after intra-peritoneal administration of DEL-22379 at 15 mg/kg. At such a dose, inhibition of ERK dimerization is evident in liver extracts and in xenografted tumors. DEL-22379 markedly inhibits tumor progression for A375 cells (BRAF mutant)[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (67.49 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2496 mL 11.2478 mL 22.4957 mL
5 mM 0.4499 mL 2.2496 mL 4.4991 mL
10 mM 0.2250 mL 1.1248 mL 2.2496 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

HEK293T cells are plated at a density of 1,000-2,000 cells/well and treated with DEL-22379 (0.2-1 μ M) for 48 hr, Alamar Blue is added, and the colorimetric change is measured at 570 and 600 nm. GI50 is estimated by nonlinear regression using GraphPad5 Prism Software. Apoptosis is analyzed by evaluating caspase 3 activity, either by western blotting or using the Caspase-Glo 3/7 luminogenic assay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Cancer cells are xenografted in female, athymic nu/nu mice of 8 weeks of age. 3×106 cells are injected subcutaneously in the lateral flank and allowed to develop for 10-15 days before treatment with DEL-22379 at 15 mg/kg every 12 hr for 2 weeks. patient-derived xenografts (PDXs) are performed using patient-derived colorectal cancer cells harboring BRAFV600E from non-necrotic areas of primary adenocarcinomas from patients that undergo surgical resection. Cells are grafted in both flanks or in the cecum of NOD-SCID mice. DEL-22379 is administered by intra-peritoneal injection at a concentration of 15 mg/kg every 12 hr for 30 days[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

444.53

Formula

C₂₆H₂₈N₄O₃

CAS No.

181223-80-3

SMILES

O=C(CCN1CCCCC1)NC2=CC=C(NC(/C3=C\C4=CNC5=C4C=C(OC)C=C5)=O)C3=C2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
DEL-22379
Cat. No.:
HY-18932
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DEL-22379

Cat. No.: HY-18932