1800505-64-9
1800505-64-9 结构式
基本信息
Pz-1 >=98% (HPLC)
Benzeneacetamide, N-[5-(1,1-dimethylethyl)-3-isoxazolyl]-4-[5-(1-methyl-1H-pyrazol-4-yl)-1H-benzimidazol-1-yl]-
| 报价日期 | 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 |
| 2024/08/19 | HY-U00437 | 1800505-64-9 Pz-1 | 1800505-64-9 | 10mg | 1050元 |
常见问题列表
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.