1403258-26-3Relevant articles and documents
EPZ011989, A potent, orally-available EZH2 inhibitor with robust in vivo activity
Campbell, John E.,Kuntz, Kevin W.,Knutson, Sarah K.,Warholic, Natalie M.,Keilhack, Heike,Wigle, Tim J.,Raimondi, Alejandra,Klaus, Christine R.,Rioux, Nathalie,Yokoi, Akira,Kawano, Satoshi,Minoshima, Yukinori,Choi, Hyeong-Wook,Porter Scott, Margaret,Waters, Nigel J.,Smith, Jesse J.,Chesworth, Richard,Moyer, Mikel P.,Copeland, Robert A.
, p. 491 - 495 (2015)
Inhibitors of the protein methyltransferase Enhancer of Zeste Homolog 2 (EZH2) may have significant therapeutic potential for the treatment of B cell lymphomas and other cancer indications. The ability of the scientific community to explore fully the spectrum of EZH2-associated pathobiology has been hampered by the lack of in vivo-active tool compounds for this enzyme. Here we report the discovery and characterization of EPZ011989, a potent, selective, orally bioavailable inhibitor of EZH2 with useful pharmacokinetic properties. EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma. Hence, this compound represents a powerful tool for the expanded exploration of EZH2 activity in biology.
SUBSTITUTED BENZENE COMPOUNDS
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, (2012/11/06)
The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.