- 英文名称
- N-(2,6-Dichloropyridin-4-yl)-2-(4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)hydrazine-1-carboxamide
- 分子式
- C17H19Cl2N7O
- 分子量
- 408.29
- 中文别名
- JTE-013; N-(2,6-二氯-4-吡啶基)-2-[1,3-二甲基-4-异丙基-1H-吡唑并[3,4-b]吡啶-6-基]肼基甲酰胺; JTE 013; JTE-013; 1-(2,6-dichloropyridin-4-yl)-3-[(1,3-dimethyl-4-propan-2-ylpyrazolo[3,4-b]pyridin-6-yl)amino]urea; N-(2,6-Dichloropyridin-4-yl)-2-(4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)hydrazinecarboxamide; N-(2,6-Dichloro-4-pyridinyl)-2-(4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)hydrazinecarboxamide; 1-[1,3-Dimethyl-4-(2-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]-4-(2,6-dichloro-4-pyridinyl)-semicarbazide; 1-(2,6-dichloro-4-pyridyl)-3-[(4-isopropyl-1,3-dimethyl-pyrazolo[3,4-b]pyridin-6-yl)amino]urea; 1-[1,3-Dimethyl-4-(2-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]-4-(3,5-dichloro-4-pyridinyl)-semicarbazide; N-(2,6-Dichloro-4-pyridinyl)-2-[1,3-dimethyl-4-(1-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]hydrazinecarboxamide; JTE 013; JTE013; Hydrazinecarboxamide, N-(2,6-dichloro-4-pyridinyl)-2-[1,3-dimethyl-4-(1-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]-
- 用途
- 化学合成；作为有效且选择性的S1P2（鞘氨醇1-磷酸2）拮抗剂，抑制放射性标记的S1P与人（IC50为17 nM）和大鼠（IC50为22 nM）S1P2的特异性结合；体外研究中，50-200 μM作用1-3天可降低SK-N-AS细胞活力，10-1000 nM作用30分钟可逆转S1P诱导的Akt抑制并抑制S1P诱导的ERK激活，对S1P3仅显示4.2%的抑制，在浓度高达10 μM时不拮抗S1P1；体内研究中，以30 mg/kg每日灌胃连续14天可减小裸鼠肿瘤大小和重量。
