Activity of the Type II JAK2 Inhibitor CHZ868 in B Cell Acute Lymphoblastic Leukemia.

  title={Activity of the Type II JAK2 Inhibitor CHZ868 in B Cell Acute Lymphoblastic Leukemia.},
  author={Shuo-Chieh Wu and Loretta S Li and Nadja Kopp and Joan Montero and Bjoern Chapuy and Akinori Yoda and Amanda L. Christie and Huiyun Liu and Alexandra Christodoulou and Diederik van Bodegom and Jordy van der Zwet and Jacob V. Layer and Trevor R. Tivey and Andrew A. Lane and Jeremy A Ryan and Samuel Yao-Ming Ng and Daniel J. Deangelo and Richard M Stone and David P Steensma and Martha Wadleigh and Marian H. Harris and Emeline Mandon and Nicolas Ebel and Rita Andraos and Vincent Romanet and Arno Doelemeyer and Dario Sterker and Michael Zender and Scott J Rodig and Masato Murakami and Francesco Hofmann and Frank Kuo and Michael J. Eck and Lewis B. Silverman and Stephen E. Sallan and Anthony Letai and Fabienne Baffert and Eric Vangrevelinghe and Thomas Radimerski and Christoph Gaul and David M. Weinstock},
  journal={Cancer cell},
  volume={28 1},
A variety of cancers depend on JAK2 signaling, including the high-risk subset of B cell acute lymphoblastic leukemias (B-ALLs) with CRLF2 rearrangements. Type I JAK2 inhibitors induce paradoxical JAK2 hyperphosphorylation in these leukemias and have limited activity. To improve the efficacy of JAK2 inhibition in B-ALL, we developed the type II inhibitor CHZ868, which stabilizes JAK2 in an inactive conformation. CHZ868 potently suppressed the growth of CRLF2-rearranged human B-ALL cells… CONTINUE READING
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