Article
CH5424802, a selective ALK inhibitor capable of blocking the resistant gatekeeper mutant.
Cancer cell - 17 May 2011
Sakamoto Hiroshi, Tsukaguchi Toshiyuki, Hiroshima Sayuri, Kodama Tatsushi, Kobayashi Takamitsu, Fukami Takaaki A, Oikawa Nobuhiro, Tsukuda Takuo, Ishii Nobuya, Aoki Yuko
Abstract excerpt
Anaplastic lymphoma kinase (ALK) is a tyrosine kinase that is constitutively activated in certain cancers, following gene alterations such as chromosomal translocation, amplification, or point mutation. Here, we identified CH5424802, 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...
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