中文名 | DEL-22379 |
英文名 | DEL-22379 |
别名 | DEL-22379, 一种ERK二聚化抑制剂 N-[2,3-二氢-3-[(5-甲氧基-1H-吲哚-3-基)亚甲基]-2-氧代-1H-吲哚-5-基]-1-哌啶丙酰胺 |
英文别名 | CS-2171 DEL22379 DEL 22379 DEL-22379 N-(3-((5-methoxy-1H-indol-3-yl)methylene)-2-oxoindolin-5-yl)-3-(piperidin-1-yl)propanamide (E)-N-(3-((5-methoxy-1H-indol-3-yl)methylene)-2-oxoindolin-5-yl)-3-(piperidin-1-yl)propanamide N-{3-[(5-methoxyindol-3-yl)methylene]-2-oxo(1H-benzo[3,4-d]azolidin-5-yl)}-3-piperidylpropanamide N-[2,3-Dihydro-3-[(5-methoxy-1H-indol-3-yl)methylene]-2-oxo-1H-indol-5-yl]-1-piperidinepropanamide |
CAS | 181223-80-3 |
化学式 | C26H28N4O3 |
分子量 | 444.53 |
密度 | 1.313±0.06 g/cm3(Predicted) |
沸点 | 763.9±60.0 °C(Predicted) |
溶解度 | DMSO: ≥ 30 mg/mL |
酸度系数 | 11.84±0.20(Predicted) |
存储条件 | Sealed in dry,Store in freezer, under -20°C |
体外研究 | 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. |
体内研究 | 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). |
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 |
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