Brigatinib (AP-26113, AP26113),又称布格替尼,是有效的ALK选择性抑制剂,IC50为0.6 nM;也是ROS1抑制剂,IC50为0.9 nM。Brigatinib是新一代酪氨酸激酶抑制药,常与EGFR联用用于治疗癌症,在临床试验显示出对肺癌有治疗前景。
参考文献
1.Zhang S, et al. The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models. Clin Cancer Res. 2016 Nov 15;22(22):5527-5538.
2.Siaw JT, et al. Brigatinib, an anaplastic lymphoma kinase inhibitor, abrogates activity and growth in ALK-positive neuroblastoma cells, Drosophila and mice. Oncotarget. 2016 May 17;7(20):29011-22.
3.Uchibori K, et al. Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer.Nat Commun. 2017 Mar 13;8:14768.
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。