Everolimus (RAD001)是一种mTOR的大环类抑制剂,作用于FKBP12,IC50为1.6-2.4 nM。
1生物活性
Everolimus (RAD001)是一种mTOR抑制剂,作用于FKBP12,IC50为1.6-2.4 nM。体外, 与Rapamycin相比,Everolimus 具有抑制免疫活性。Everolimus与固定化的FK 506竞争性结合到生物素化的FKBP12上,IC50为1.6 nM-2.4 nM,且作用于BALB/c和CBA小鼠脾脏细胞,抑制双向MLR,IC50为0.12 nM-1.8 nM。Everolimus 作用于VEGF诱导的HUVEC增殖和bFGF诱导的 HUVEC增殖,具有抗血管生成/血管效果,IC50分别为0.12 nM和 0.8 nM。
2实验参考
3化学性质
分子量 958.22
分子式 C53H83NO14
CAS号 159351-69-6
溶解性(25°C) DMSO 30 mg/mL
储存条件 粉末型式 -20°C 3年;4°C 2年
溶于溶剂 -80°C 6个月;-20°C 1个月
运输方式 冰袋运输,根据产品的不同,可能会有相应调整。
4储备液配置
5参考文献
[1] Manzia et al. Transplant Proc. Everolimus and enteric-coated mycophenolate sodium ab initio after liver transplantation: midterm results.
[2] Caroti et al. Transplant Proc. Conversion from calcineurin inhibitors to everolimus with low-dose cyclosporine in renal transplant recipients with squamous cell carcinoma of the skin.
[3] Papadimitrakopoulou et al. J Thorac Oncol. Everolimus and Erlotinib as Second- or Third-Line Therapy in Patients with Advanced Non-Small-Cell Lung Cancer.
[4] Jensen et al. Am J Cardiol. Comparison of Outcomes in Patients With Versus Without Diabetes Mellitus After Revascularization With Everolimus- and Sirolimus-Eluting Stents (from the SORT OUT IV Trial).
[5] Arora et al. Am J Transplant. Virtual Histology Assessment of Cardiac Allograft Vasculopathy Following Introduction of Everolimus-Results of a Multicenter Trial.
[6] Saito et al. J Invasive Cardiol. Mid-Term Results of Everolimus-Eluting Stent in a Japanese Population Compared With a US Randomized Cohort: SPIRIT III Japan Registry With Harmonization by Doing.
[7] Holdaas et al. Expert Opin Drug Saf. A drug safety evaluation of everolimus in kidney transplantation.