Cobimetinib (GDC-0973, XL518, RG7420, GDC0973, XL-518, RG-7420),又称考比替尼、克吡替尼、卡吡替尼或可美替尼,是可口服的MEK1抑制剂,IC50为4.2 nM,通过抑制MEK1/2下游信号传导来诱导细胞凋亡,具有抗癌活性,临床上用于治疗BRAF V600E或V600K突变的黑色素瘤患者。
参考文献
[1] Hoeflich KP, et al. Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition. Cancer Res. 2012 Jan 1;72(1):210-9.
[2] Choo EF, et al. PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts. Cancer Chemother Pharmacol. 2013 Jan;71(1):133-43.
[3] Corazao-Rozas P, et al. Mitochondrial oxidative phosphorylation controls cancer cell's life and death decisions upon exposure to MAPK inhibitors. Oncotarget. 2016 Jun 28;7(26):39473-39485.
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。