Alectinib
ALK inhibitor / Alectinib is a potent (IC50 = 1.9 nM) and highly selective ALK inhibitor.1 It blocked phosphorylation of both native ALK and the L1196M, C1156Y, and F1174L mutants. Alectinib has also been shown to inhibit RET kinase (IC50 = 4.8 nM), the RET gatekeeper mutations V804L and V804M, and inhibited the growth of RET fusion positive cells.2 Alectinib is clinically useful in the treatment of ALK-positive Non-Small Cell Lung Cancer. It effectively suppressed cell proliferation and induced apoptosis in a mouse neuroblastoma xenograft.3
Biochemicals & reagents
1256580-46-7
CH5424802; RO5424802
1) Sakamoto et al. (2011), CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant; Cancer Cell, 19 679 2) Kodama et al. (2014), Alectinib Shows Potent Antitumor Activity against RET-Rearranged Non-Small Cell Lung Cancer., Mol. Cancer Ther. 13 2910 3) Lu et al. (2017), The second-generation ALK inhibitor alectinib effectively induces apoptosis in human neuroblastoma cells and inhibits tumor growth in a TH-MYCN transgenic neuroblastoma mouse model; Cancer Lett, 400 61
-20°C
TARGET: Kinase -- PATHWAY: Proliferation; PI3K; TGF-beta -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Cancer