181223-80-3
DEL-22379
CAS: 181223-80-3
Molecular Formula: C26H28N4O3
181223-80-3 - Names and Identifiers
181223-80-3 - Physico-chemical Properties
| Molecular Formula | C26H28N4O3 |
| Molar Mass | 444.53 |
| Density | 1.313±0.06 g/cm3(Predicted) |
| Boling Point | 763.9±60.0 °C(Predicted) |
| Solubility | DMSO: ≥ 30 mg/mL |
| pKa | 11.84±0.20(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| In vitro study | 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 (IC 50 ) 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 (GI 50 ). 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 (IC 50 of 150-400 nM) regardless of the genotype. |
| In vivo study | 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). |
181223-80-3 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.25 ml | 11.248 ml | 22.496 ml |
| 5 mM | 0.45 ml | 2.25 ml | 4.499 ml |
| 10 mM | 0.225 ml | 1.125 ml | 2.25 ml |
| 5 mM | 0.045 ml | 0.225 ml | 0.45 ml |
Last Update：2024-01-02 23:10:35
181223-80-3 - Reference Information
| biological activity | DEL-22379 is an ERK dimerization inhibitor. DEL-22379 is easy to bind to ERK2, Kd is a low micromolar level, and EL-22379 binding to ERK2 can be detected even at low nanomolar concentrations. DEL-22379 inhibit ERK2 dimerization, IC50 is about 0.5 μM. |
| target | ERK2 0.5 μM (IC 50 ) |
| in vitro study | 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 (IC 50 ) 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 (GI 50 ). 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 mutcells 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 (IC 50 of 150-400 nM) regardless of the genotype. |
| in vivo study | 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). |
Last Update：2024-04-09 15:16:38
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Product Name: DEL-22379 Visit Supplier Webpage Request for quotation
CAS: 181223-80-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 181223-80-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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