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
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