1800505-64-9
| 中文名称 | 1800505-64-9 |
|---|---|
| 中文同义词 | 化合物 T12598;化合物PZ-1;N-(5-(叔丁基)异恶唑-3-基)-2-(4-(5-(1-甲基-1H-吡唑-4-基)-1H-苯并[D]咪唑-1-基)苯基)乙酰胺 |
| 英文名称 | PZ-1 |
| 英文同义词 | PZ-1;Benzeneacetamide, N-[5-(1,1-dimethylethyl)-3-isoxazolyl]-4-[5-(1-methyl-1H-pyrazol-4-yl)-1H-benzimidazol-1-yl]-;Pz-1 >=98% (HPLC);Pz 1,Vascular endothelial growth factor receptor,inhibit,RET,Pz-1,VEGFR,Inhibitor,Pz1;N-(5-(tert-Butyl)isoxazol-3-yl)-2-(4-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)phenyl)acetamide , Pz-1 |
| CAS号 | 1800505-64-9 |
| 分子式 | C26H26N6O2 |
| 分子量 | 454.52 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 1800505-64-9.mol |
| 结构式 |  |
1800505-64-9 性质
| 密度 | 1.28±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | 2-8°C |
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 粉末 |
| 酸度系数(pKa) | 12?+-.0.70(Predicted) |
| 颜色 | 白色至米色 |
IC50: < 1 nM (RET and VEGFR2)
Pz-1 is a Type-II tyrosine kinase inhibitor, able to bind the DFG-out conformation of the kinase. In cell-based assays, 1.0 nM of Pz-1 strongly inhibits tyrosine phosphorylation of VEGFR2 and clinically relevant RET mutants, including those refractory to vandetanib and cabozantinib (RET V804M and RET V804L ).
Pz-1 is shown active on VEGFR2, which can block blood supply required for RET-stimulated growth. At 1.0 mg/kg/day per os, Pz-1 abrogates formation of tumors induced by RET-mutant fibroblasts and blocks phosphorylation of both RET and VEGFR2 in tumor tissue. Pz-1 features no detectable toxicity up to 100.0 mg/kg, which indicates a large therapeutic window.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/08/19 | HY-U00437 | 1800505-64-9 Pz-1 | 1800505-64-9 | 5mg | 650元 |
| 2024/08/19 | HY-U00437 | 1800505-64-9 Pz-1 | 1800505-64-9 | 10 mM * 1 mLin DMSO | 720元 |