DEL-22379
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1390 | Check With Us |
| 500mg | $1850 | Check With Us |
| 1g | $2775 | Check With Us |
: Cat #: V0469 CAS #: 181223-80-3 Purity ≥ 98%
Description: DEL-22379 is a novel, potent, selective, and water-soluble ERK (extracellular signal-related kinase 2) dimerization inhibitor with potential antitumor activity.
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| Molecular Weight (MW) | 444.53 |
|---|---|
| Molecular Formula | C26H28N4O3 |
| CAS No. | 181223-80-3 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 89 mg/mL (200.2 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| SMILES Code | O=C(NC1=CC2=C(NC(/C2=C/C3=CNC4=C3C=C(OC)C=C4)=O)C=C1)CCN5CCCCC5 |
| Synonyms | DEL 22379; DEL22379; DEL-22379. |
| Protocol | 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. |
|---|---|---|
| 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). |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.2496 mL | 11.2478 mL | 22.4957 mL | 44.9913 mL |
| 5mM | 0.4499 mL | 2.2496 mL | 4.4991 mL | 8.9983 mL |
| 10mM | 0.2250 mL | 1.1248 mL | 2.2496 mL | 4.4991 mL |
| 20mM | 0.1125 mL | 0.5624 mL | 1.1248 mL | 2.2496 mL |
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Method for preparing in vivo formulation:
Take
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PEG300, mix and clarify, next add
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Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
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