SCH772984 (SCH-772984)是一种新型高选择性、ATP竞争性的ERK1/2抑制剂,IC50分别为4 nM和1 nM,强烈抑制含有RAS或BRAF突变的癌细胞的生长。此外,SCH772984对7种激酶(MAP4K4、MAPK1、CLK2、GSG2、FLT4、MINK1、PRKD1和TTK)具有高选择性,在1 μM浓度时抑制超过50%的活性。
参考文献
[1].Morris EJ, et al. Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. Cancer Discov. 2013;3(7):742-50.
[2].Wong DJL, et al. Antitumor activity of the ERK inhibitor SCH722984 against BRAF mutant, NRAS mutant and wild-type melanoma. Molecular cancer, 2014;13(1): 194.
[3].Hu C, et al. Combined inhibition of cyclin-dependent kinases (Dinaciclib) and AKT (MK-2206) or ERK (SCH772984) dramatically blocks pancreatic tumor growth and metastases in patient-derived orthotopic xenograft models. Mol Cancer Ther. 2015;14(7):1532-9.
冰袋运输。粉末直接保存于-25~-15℃,有效期2年。建议干燥避光保存,避免反复冻融。