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Soluble in DMSO.. Alectinib, also known as CH 5424802, is a potent, selective, and orally available ALK inhibitor (IC50 = 1.9 nM) and has weak or no inhibition against 24 other tested protein kinases. It has selective antitumor activity against cancers with ALK gene alterations, including non-small cell lung cancer (NSCLC) cells expressing EML4-ALK fusion and anaplastic large-cell lymphoma (ALCL) cells expressing NPM-ALK fusion in vitro and in vivo. It also blocked ALK L1196M, which corresponds to the gatekeeper mutation giving common resistance to kinase inhibitors, and prevented EML4-ALK L1196M-driven cell growth. Sakamoto H., et al. 'CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant.' Cancer Cell 19: 679-690 (2011). Alectinib reduced the tumor size in EML4-ALK-positive xenograft tumors that was not able to regress fully during treatment with crizotinib. Alectinib also inhibited the growth of some EML4-ALK mutant-driven tumors, such as the G1269A model. Kodama T., et al. 'Selective ALK inhibitor alectinib with potent antitumor activity in models of crizotinib resistance.' Cancer Lett. 351: 215-221 (2014). Two ALK mutations, a V1180L gatekeeper mutation from the cell line model and I1171T mutation from a patient, were found to develop resistance to alectinib and to crizotinib, but were sensitive to ceritinib and other next-generation ALK-TKIs. Katayama R., et al. 'Two novel ALK mutations mediate acquired resistance to the next-generation ALK inhibitor alectinib.' Clin. Cancer Res. 20: 5686-5696 (2014). This research compound is the free acid form of alectinib, we also offer the HCl salt form of alectinib, please see Cat. No. A-2311, Alectinib, Hydrochloride Salt. The free base form of alectinib is used for some or all alectinib formulations for use in humans.
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