181223-80-3 | 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
英文名称
DEL-22379
分子式
C26H28N4O3
分子量
444.53
结构式
中文别名
英文别名
| 属性 | 值 |
|---|---|
| 密度 | 1.313±0.06 g/cm3(Predicted) |
| 形态 | 粉末 |
| 沸点 | 763.9±60.0 °C(Predicted) |
| 颜色 | Yellow to orange |
| 溶解度 | 溶于二甲基亚砜 |
| 储存条件 | Sealed in dry,Store in freezer, under -20°C |
| 酸度系数(pKa) | 11.84±0.20(Predicted) |
| 属性 | 值 |
|---|---|
| 警示词 | 警告 |
| 海关编码 | 2933790090 |
| 防范说明 | P305+P351+P338 |
| 危险性描述 | H315-H319 |
| 危险性符号(GHS) | GHS07 |
| 标题 | 内容 |
|---|---|
| 靶点 | ERK2 0.5 μM (IC 50 ) |
| 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). |
| 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. |
| 生物活性 | DEL-22379 是一种 ERK 二聚化抑制剂。DEL-22379 易与 ERK2 结合，Kd 为低微摩尔水平，即使在低纳摩尔浓度下也可检测到 EL-22379 与 ERK2 结合。DEL-22379 抑制 ERK2 二聚化，IC50 约为 0.5 μM。 |