| CAS: | 1800505-64-9 | ||
| 分子式: | C26H26N6O2 | ||
| 分子量: | 454.52 | ||
| 英文名称: |
| ||
| 用途: | Pz-1 is a potent RET and VEGFR2 inhibitor with IC50s of less than 1 nM for both wild type kinases. |
| 货号 | 品牌 | 产品名称 | 规格 | 包装、参考价格 | 详情 | ||||||||||||||||||||||||||||||
| P911131 | MACKLIN | Pz-1 | 98% | 2916元/5mg; | 展开 | ||||||||||||||||||||||||||||||
储存：-20°C，密闭，干燥 | |||||||||||||||||||||||||||||||||||
| SML1693 | Sigma-Aldrich | Pz-1 | ≥98% (HPLC) | 1117.23元/5 MG; | 展开 | ||||||||||||||||||||||||||||||
产品说明 包装 5, 25 mg in glass bottle 生化/生理作用 Pz-1 is a cell-permeable, non-cytotoxic (up to 0.1 μM and 6 days; NIH/3T3 cells), and highly potent type II kinase inhibitor that potently inhibits RET and VEGFR2 tyrosine kinase activity (IC50 <1 nM; [ATP] = 190 μM) by targeting the kinases in their inactive DFG-out conformation, displaying significant affinity (Kd <50 nM) toward only TRKB, TRKC, GKA, FYN, SRC, TAK1, MUSK from a panel of 96 other kinases. Pz-1 inhibits cellular RET mutants (C634R, C634Y, V804L, V804M, M918T) and VEGFR2 phosphorylations, and selectively inhibits the growth of RET C634Y- than HRas G12V-transformed NIH/3T3 cultures (IC50 = 0.5 vs. 34.4 nM). Likewise, Pz-1 completely abrogated tumor formation from RET C634Y-transformed NIH/3T3 cells in mice in vivo (1 mg/kg/d, p.o.), while only up to 70% tumor suppression of HRas G12V-transformed cells was achieved with 10 mg/kg daily oral dosage. 基本信息
产品性质
安全信息
| |||||||||||||||||||||||||||||||||||
m.cnreagent.com