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Pz-1

品牌
Sigma-Aldrich
CAS
1800505-64-9
货号
SML1693
包装型号
规格纯度
≥98% (HPLC)
参考价格
1117.23 *本价格含增值税费
促销
数量
-+
产品介绍:

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

经验(实验)分子式C26H26N6O2
分子量454.52
PubChem化学物质编号329826021

产品性质

质量水平100
测定≥98% (HPLC)
形式powder
颜色 white to beige
溶解性DMSO: 1 mg/mL, clear (warmed)
储存温度2-8℃
SMILES stringCN1N=CC(C(C=C2)=CC3=C2N(C4=CC=C(CC(NC5=NOC(C(C)(C)C)=C5)=O)C=C4)C=N3)=C1

安全信息

储存分类代码13 - Non Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

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