RG7112 (RO5045337, RO-5045337, RG-7112)是一种可口服、可透过血脑屏障的p53-MDM2选择性抑制剂,IC50为18 nM,结合到MDM2的p53口袋,Kd值为11 nM,对多种肿瘤细胞表现出抗肿瘤活性,目前处于I期临床研究。
参考文献
1.Obrador-Hevia A, et al. RG7112, a small-molecule inhibitor of MDM2, enhances trabectedin response in soft tissue sarcomas. Cancer Invest. 2015;33(9):440-50.
2.Tovar C, et al. MDM2 small-molecule antagonist RG7112 activates p53 signaling and regresses human tumors in preclinical cancer models. Cancer Res. 2013 Apr 15;73(8):2587-97.
3.Verreault M, et al. Preclinical Efficacy of the MDM2 Inhibitor RG7112 in MDM2-Amplified and TP53 Wild-type Glioblastomas. Clin Cancer Res. 2016 Mar 1;22(5):1185-96.
4.Makii C, et al. MDM2 is a potential therapeutic target and prognostic factor for ovarian clear cell carcinomas with wild type TP53. Oncotarget. 2016 Nov 15;7(46):75328-75338.
冰袋运输。粉末直接保存于-20℃,有效期3年。建议分装后-20℃干燥保存,避免反复冻融。