N4-(3-溴苯基)-N6-甲基-吡啶并[3,4-D]嘧啶-4,6-二胺
| 中文名称 | N4-(3-溴苯基)-N6-甲基-吡啶并[3,4-D]嘧啶-4,6-二胺 |
|---|---|
| 中文同义词 | N4-(3-溴苯基)-N6-甲基-吡啶并[3,4-D]嘧啶-4,6-二胺;化合物PD158780 |
| 英文名称 | PD158780 |
| 英文同义词 | N4-(3-Bromophenyl)-N6-methyl-pyrido[3,4-d]pyrimidine-4,6-diamine;Pyrido[3,4-d]pyriMidine-4,6-diaMine,N4-(3-broMophenyl)-N6-Methyl- (Related Reference);Pyrido[3,4-d]pyriMidine-4,6-diaMine,N4-(3-broMophenyl)-N6-Methyl-;PD 158780 solution;InSolution? PD 158780;PD 158780 - CAS 171179-06-9 - Calbiochem;InSolution PD 158780 - CAS 171179-06-9 - Calbiochem;PD 158780; PD-158780 |
| CAS号 | 171179-06-9 |
| 分子式 | C14H12BrN5 |
| 分子量 | 330.18 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 171179-06-9.mol |
| 结构式 | ![N4-(3-溴苯基)-N6-甲基-吡啶并[3,4-D]嘧啶-4,6-二胺 结构式](CAS/GIF/171179-06-9.gif) |
N4-(3-溴苯基)-N6-甲基-吡啶并[3,4-D]嘧啶-4,6-二胺 性质
| 熔点 | 174.0 to 178.0 °C |
|---|---|
| 沸点 | 499.6±45.0 °C(Predicted) |
| 密度 | 1.611±0.06 g/cm3 (20 ºC 760 Torr) |
| 储存条件 | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| 溶解度 | 二甲基亚砜：≥20mg/mL |
| 形态 | 黄色固体 |
| 酸度系数(pKa) | 5.80±0.30(Predicted) |
| 颜色 | 粘黄色 |
|
EGFR 8 μM (IC 50 , Cell Assay) |
ErbB2 49 nM (IC 50 , Cell Assay) |
ErbB3 52 nM (IC 50 , Cell Assay) |
ErbB4 52 nM (IC 50 , Cell Assay) |
PD158780 inhibits EGF receptor autophosphorylation in A431 human epidermoid carcinoma with IC 50 value of 13 nM. PD158780 is highly specific for the EGF receptor in Swiss 3T3 fibroblasts, inhibiting EGF-dependent receptor autophosphorylation and thymidine incorporation at low nanomolar concentrations while requiring micromolar levels for platelet-derived growth factor- and basic fibroblast growth factordependent processes. PD158780 inhibits heregulin-stimulated phosphorylation in the SK-BR-3 and MDAMB-453 breast carcinomas with IC 50 values of 49 and 52 nM, respectively, suggesting that the compound is active against other members of the EGF receptor family.
PD158780 is active against clone formation in several breast tumors having different expression patterns of the ErbB family. PD158780 shows good therapeutic effect against the A431 epidermoid carcinoma when administered either intraperitoneally or orally. PD158780 produces measurable, significant effects against a mouse fibroblast transfected with human EGFR. PD158780 produces a significant therapeutic effect against the estrogendependent MCF-7 breast carcinoma at equitoxic dose levels.
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | P2567 | PD 158780 PD 158780 | 171179-06-9 | 10mg | 420元 |
| 2024/04/30 | P2567 | PD 158780 PD 158780 | 171179-06-9 | 50mg | 1730元 |