JTE-013
| 中文名称 | JTE-013 |
|---|---|
| 中文同义词 | 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;化合物JTE-013;N-(2,6-二氯吡啶-4-基)-2-(4-异丙基-1,3-二甲基-1H-吡唑并[3,4-B]吡啶-6-基)氨基甲酰肼;JTE 013,S1P2受体拮抗剂 |
| 英文名称 | JTE-013 |
| 英文同义词 | 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;CS-2553;N-(2,6-Dichloro-4-pyridinyl)-2-[1,3-dimethyl-4-(1-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]hydrazinecarboxamide;JTE-013;JTE 013;JTE013;1-(2,6-dichloropyridin-4-yl)-3-[(1,3-dimethyl-4-propan-2-ylpyrazolo[3,4-b]pyridin-6-yl)amino]urea;Hydrazinecarboxamide, N-(2,6-dichloro-4-pyridinyl)-2-[1,3-dimethyl-4-(1-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]- |
| CAS号 | 383150-41-2 |
| 分子式 | C17H19Cl2N7O |
| 分子量 | 408.29 |
| EINECS号 | |
| 相关类别 | 生物活性分子 |
| Mol文件 | 383150-41-2.mol |
| 结构式 |  |
JTE-013 性质
| 密度 | 1.50±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：≥20mg/mL |
| 酸度系数(pKa) | 9.32±0.43(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至类白色 |
JTE-013 是一种有效且选择性的 S1P2 (鞘氨醇1-磷酸2) 拮抗剂。JTE-013 抑制放射性标记的 S1P 与人和大鼠 S1P2 的特异性结合，IC50 分别为 17 nM 和 22 nM。
IC50: 17 nM (S1P 2 for human) and 22 nM (S1P 2 for rat)
JTE-013 (50-200 μM; 1-3 days) reduced cell viability.
JTE-013 (10-1000 nM; 30 mins) reverses S1P-induced Akt inhibition and inhibits S1P-induced ERK activation.
JTE-013 displays 4.2% inhibition of S1P
3
and does not antagonize S1P
1
at concentrations up to 10 μM.
Cell Viability Assay
| Cell Line: | SK-N-AS cells |
| Concentration: | 50, 100, 150, 200 μM |
| Incubation Time: | 1-3 days |
| Result: | Reduced cell viability. |
Western Blot Analysis
| Cell Line: | SK-N-AS cells |
| Concentration: | 10, 100, 1000 nM |
| Incubation Time: | 30 mins |
| Result: | Reversed S1P-induced Akt inhibition and inhibited S1P-induced ERK activation. |
JTE-013 (gavage; 30 mg/kg daily for 14 consecutive days) reduces tumor size and tumor weight.
| Animal Model: | Six-week-old female athymic NCr-nu/nu nude mice |
| Dosage: | 30 mg/kg |
| Administration: | Gavage; daily for 14 consecutive days |
| Result: | Reduced tumor size and tumor weight. |