N-(3-溴-4-甲基苯基)-4-(4-吡啶甲基)-1-酞嗪胺
| 中文名称 | N-(3-溴-4-甲基苯基)-4-(4-吡啶甲基)-1-酞嗪胺 |
|---|---|
| 中文同义词 | N-(3-溴-4-甲基苯基)-4-(4-吡啶甲基)-1-酞嗪胺;化合物NVP-ACC789;N-(3-溴-4-甲基苯基)-4-(吡啶-4-基甲基)酞嗪-1-胺 |
| 英文名称 | N-(3-Bromo-4-methylphenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine |
| 英文同义词 | N-(3-Bromo-4-methylphenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine;Acc-789;ZK 202650;NVP-ACC-789;ACC-789 (NVP-ACC789);ACC-789; ZK-202650; NVP-ACC-789;ACC789;ACC 789;N-(3-Bromo-4-methylphenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine;NVP ACC789,Platelet-derived growth factor receptor,inhibit,ZK 202650,PDGFR,NVPACC789,Inhibitor,ZK-202650,ACC789,NVP-ACC789,VEGFR,ACC 789,NVP-ACC-789,Vascular endothelial growth factor receptor |
| CAS号 | 300842-64-2 |
| 分子式 | C21H17BrN4 |
| 分子量 | 405.29 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 300842-64-2.mol |
| 结构式 |  |
N-(3-溴-4-甲基苯基)-4-(4-吡啶甲基)-1-酞嗪胺 性质
| 沸点 | 607.7±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.441 |
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO:13.0(最大浓度 mg/mL);32.08(最大浓度 mM) DMF:0.5(最大浓度 mg/mL);1.23(最大浓度 mM) DMF:PBS ( pH 7) (1:10):0.09(最大浓度 mg/mL);0.22(最大浓度 mM) 乙醇:0.2(最大浓度 mg/mL);0.49(最大浓度 mM) |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 5.46±0.10(Predicted) |
|
VEGFR-2 0.02 μM (IC 50 ) |
VEGFR-1 0.38 μM (IC 50 ) |
mVEGFR-2 0.23 μM (IC 50 ) |
VEGFR-3 0.18 μM (IC 50 ) |
PDGFR-β 1.4 μM (IC 50 ) |
The enzymatic kinase assays demonstrate that NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC 50 s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively. In VEGF-treated cultures, addition of the VEGFR-2 inhibitor NVP-ACC789 reduces BME cell number to baseline levels from 1 μM. Likewise, bFGF-induced BME cell proliferation is reduced markedly by NVP-ACC789 from 1 to 10 μM, without however reaching basal levels. NVP-ACC789 is found to be a potent inhibitor of VEGF-induced HUVE cell proliferation with an IC 50 of 1.6 nM. NVP-ACC789 also completely inhibits VEGF-induced BME and BAE cell invasion and VEGF-C-induced BAE cell invasion. The inhibition is dose-dependent in both cell types with a maximal effect from 1 μM.
NVP-ACC789 which is given in daily oral doses for 6 days blocks VEGF-induced angiogenesis in a dose-dependent manner. NVP-ACC789 also inhibits the response to bFGF to some extent, but the dose-response curve is not linear for NVP-ACC789.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-19624 | NVP-ACC789 | 1 mg | 200元 | |
| 2024/01/25 | HY-19624 | N-(3-溴-4-甲基苯基)-4-(4-吡啶甲基)-1-酞嗪胺 NVP-ACC789 | 300842-64-2 | 5mg | 500元 |