Alectinib

CAT#: H205799

CAS#: 1256580-46-7

Description: Alectinib, also known as AF802, or CH5424802 or RO5424802, is a potent, selective, and orally available ALK inhibitor with a unique chemical scaffold, showing preferential antitumor activity against cancers with gene alterations of ALK, such as nonsmall 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. CH5424802 inhibited ALK L1196M, which corresponds to the gatekeeper mutation conferring common resistance to kinase inhibitors, and blocked EML4-ALK L1196M-driven cell growth. Alectinib was approved in Dec. 2015.

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Alectinib - Synthetic Route 1

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Kinoshita, Kazutomo; Asoh, Kohsuke; Furuichi, Noriyuki; Ito, Toshiya; Kawada, Hatsuo; Hara, Sousuke; Ohwada, Jun; Miyagi, Takuho; Kobayashi, Takamitsu; Takanashi, Kenji; Tsukaguchi, Toshiyuki; Sakamoto, Hiroshi; Tsukuda, Takuo; Oikawa, Nobuhiro. Design and synthesis of a highly selective, orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802). Bioorganic & Medicinal Chemistry. Volume 20. Issue 3. Pages 1271-1280. 2012.