AbMole|Everolimus 依维莫斯；依维莫司(CAS号：159351-69-6；目录号M1709)

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.