目录号：A2003 别名: IMC-1121B, LY3009806, IMC-1121 中文名称：雷莫芦单抗
For research use only.
Not for use in humans.
Ramucirumab (anti-VEGFR2) 是IgG1类的单克隆抗体，可与 VEGF-R2 结合并阻止其激活，其阻断KDR与VEGF结合的 IC50 值为0.8 nM；MW: 143.6 KD。
|产品描述||Ramucirumab (anti-VEGFR2) 是IgG1类的单克隆抗体，可与 VEGF-R2 结合并阻止其激活，其阻断KDR与VEGF结合的 IC50 值为0.8 nM；MW: 143.6 KD。|
Ramucirumab is direct inhibitor of VEGF-R2, where it binds to the extracellular VEGF-binding domain with high degree of specificity and affinity, at picomolar dose range. It thus prevents the binding of the VEGF ligand to the VEGF-R2 receptor. Ramucirumab has potential advantages over bevacizumab as it is selective for VEGF-R2, whereas bevacizumab by targeting VEGF-A affects VEGF-R1, -R2, and the noncatalytic coreceptors neuropilin-1and -2. Ramucirumab prevents the binding of VEGFR ligands: VEGF-A, VEGF-C, and VEGF-D to its receptors. Thus, ramucirumab inhibits the angiogenesis pathways involved in the development and progression of gastric cancer. ramucirumab demonstrates inhibition of VEGF-stimulated VEGFR-2 activation, proliferation of human endothelial cells, VEGF migration of human leukemia cells, and VEGF induced phosphorylation of VEGFR-2 in human umbilical vein and porcine aortic endothelial cells overexpressing VEGFR-2. Preclinical in vitro data revealed that ramucirumab has a high affinity for VEGFR-2, showing a half-maximal effective concentration (EC50) of 0.15 nM, 8- to 9-fold higher than its natural ligand VEGFA. Ramucirumab binds VEGFR-2 in domain 3 near the N-terminus, both as a soluble protein and as a cell-surface receptor, with a IC50 of 1-2 nM.
|体内研究||In preclinical studies, ramucirumab concentrations of >20 μg/mL were associated with anticancer activity. And ramucirumab potently inhibited VEGF binding to VEGFR-2 with a binding affinity constant of ramucirumab to VEGFR-2 of 5 × 10-11 M. Pharmacokinetic evaluation has demonstrated a nonlinear pharmacokinetic, with incremental doses of this agent being associated with a decrease in clearance. Ramucirumab has a half-life of 200-300 h. Preclinical studies were also to be conducted in mice, but interspecies receptor differences made ramucirumab inactive in preclinical mouse models.|
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|配制||PBS buffer, pH 7.2|
|储存条件||Store the undiluted solution at 4°C in the dark to avoid freeze-thaw cycles|