网站主页 >> CAS数据库列表 >> 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
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
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- CAS号:
- 181223-80-3
- 英文名:
- DEL-22379
- 英文别名:
- CS-2171;DEL-22379;DEL-22379 >=98% (HPLC);DEL22379;DEL 22379;DEL-22379;DEL-22379, 98%, an ERK dimerization inhibitor;N-(3-((5-methoxy-1H-indol-3-yl)methylene)-2-oxoindolin-5-yl)-3-(piperidin-1-yl)propanamide;ERK,Inhibitor,DEL-22379,Extracellular signal regulated kinases,inhibit,DEL 22379,Apoptosis;(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
- 中文名:
- 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
- 中文别名:
- 化合物DEL22379;DEL 22379,ERK二聚化抑制剂;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
- CBNumber:
- CB33049203
- 分子式:
- C26H28N4O3
- 分子量:
- 444.53
- MOL File:
- 181223-80-3.mol
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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-哌啶丙酰胺化学性质
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沸点:
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763.9±60.0 °C(Predicted)
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密度:
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1.313±0.06 g/cm3(Predicted)
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储存条件:
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Sealed in dry,Store in freezer, under -20°C
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溶解度:
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Soluble in DMSO
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形态:
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Powder
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酸度系数(pKa):
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11.84±0.20(Predicted)
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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-哌啶丙酰胺性质、用途与生产工艺
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。
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.
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).
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
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下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-18932 | 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
DEL-22379 | 181223-80-3 | 5mg | 750元 |
| 2024/01/25 | HY-18932 | 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
DEL-22379 | 181223-80-3 | 10mM * 1mLin DMSO | 825元 |
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
生产厂家
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 相关搜索:
- 药靶配体
- 抑制剂
- DEL 22379,ERK二聚化抑制剂
- 化合物DEL22379
- 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
- 181223-80-3
- ERK,Inhibitor,DEL-22379,Extracellular signal regulated kinases,inhibit,DEL 22379,Apoptosis
- DEL-22379 >=98% (HPLC)
- 1-Piperidinepropanamide, N-[2,3-dihydro-3-[(5-methoxy-1H-indol-3-yl)methylene]-2-oxo-1H-indol-5-yl]-
- (E)-N-(3-((5-methoxy-1H-indol-3-yl)methylene)-2-oxoindolin-5-yl)-3-(piperidin-1-yl)propanamide
- DEL22379;DEL 22379;DEL-22379
- CS-2171
- N-{3-[(5-methoxyindol-3-yl)methylene]-2-oxo(1H-benzo[3,4-d]azolidin-5-yl)}-3-piperidylpropanamide
- DEL-22379, 98%, an ERK dimerization inhibitor
- N-(3-((5-methoxy-1H-indol-3-yl)methylene)-2-oxoindolin-5-yl)-3-(piperidin-1-yl)propanamide
- N-[2,3-Dihydro-3-[(5-methoxy-1H-indol-3-yl)methylene]-2-oxo-1H-indol-5-yl]-1-piperidinepropanamide
- DEL-22379