產(chǎn)品屬性：
產(chǎn)品名稱 | Pz-1 |
規(guī)格 | 5mg、10mg、25mg、50mg、100mg |
貨號(hào) | EY-01Y12908 |
Cas No.: 1800505-64-9
別名: N/A
化學(xué)名: N/A
分子式: C26H26N6O2
分子量: 454.52
溶解度: Soluble in DMSO
儲(chǔ)存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述：
Pz-1 is a potent RET and VEGFR2 inhibitor with IC50s of less than 1 nM for both wild type kinases.IC50: < 1 nM (RET and VEGFR2)[1]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 (RETV804M and RETV804L)[1].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[1].[1]. Frett B, et al. Fragment-Based Discovery of a Dual pan-RET/VEGFR2 Kinase Inhibitor Optimized for Single-Agent Polypharmacology. Angew Chem Int Ed Engl. 2015 Jul 20;54(30):8717-21.
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