Ontology highlight
ABSTRACT:
SUBMITTER: Zou HY
PROVIDER: S-EPMC4504786 | biostudies-literature | 2015 Jul
REPOSITORIES: biostudies-literature
Zou Helen Y HY Friboulet Luc L Kodack David P DP Engstrom Lars D LD Li Qiuhua Q West Melissa M Tang Ruth W RW Wang Hui H Tsaparikos Konstantinos K Wang Jinwei J Timofeevski Sergei S Katayama Ryohei R Dinh Dac M DM Lam Hieu H Lam Justine L JL Yamazaki Shinji S Hu Wenyue W Patel Bhushankumar B Bezwada Divya D Frias Rosa L RL Lifshits Eugene E Mahmood Sidra S Gainor Justin F JF Affolter Timothy T Lappin Patrick B PB Gukasyan Hovhannes H Lee Nathan N Deng Shibing S Jain Rakesh K RK Johnson Ted W TW Shaw Alice T AT Fantin Valeria R VR Smeal Tod T
Cancer cell 20150702 1
We report the preclinical evaluation of PF-06463922, a potent and brain-penetrant ALK/ROS1 inhibitor. Compared with other clinically available ALK inhibitors, PF-06463922 displayed superior potency against all known clinically acquired ALK mutations, including the highly resistant G1202R mutant. Furthermore, PF-06463922 treatment led to regression of EML4-ALK-driven brain metastases, leading to prolonged mouse survival, in a superior manner. Finally, PF-06463922 demonstrated high selectivity and ...[more]