1350549-22-2Relevant academic research and scientific papers
UNC1062, a new and potent Mer inhibitor
Liu, Jing,Zhang, Weihe,Stashko, Michael A.,DeRyckere, Deborah,Cummings, Christopher T.,Hunter, Debra,Yang, Chao,Jayakody, Chatura N.,Cheng, Nancy,Simpson, Catherine,Norris-Drouin, Jacqueline,Sather, Susan,Kireev, Dmitri,Janzen, William P.,Earp, H. Shelton,Graham, Douglas K.,Frye, Stephen V.,Wang, Xiaodong
, p. 83 - 93 (2013/10/01)
Abnormal activation of Mer kinase has been implicated in the oncogenesis of many human cancers including acute lymphoblastic and myeloid leukemia, non-small cell lung cancer, and glioblastoma. We have discovered a new family of small molecule Mer inhibitors, pyrazolopyrimidine sulfonamides, that potently inhibit the kinase activity of Mer. Importantly, these compounds do not demonstrate significant hERG activity in the PatchXpress assay. Through structure-activity relationship studies, 35 (UNC1062) was identified as a potent (IC50 = 1.1 nM) and selective Mer inhibitor. When applied to live tumor cells, UNC1062 inhibited Mer phosphorylation and colony formation in soft agar. Given the potential of Mer as a therapeutic target, UNC1062 is a promising candidate for further drug development.
PYRAZOLOPYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER
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Page/Page column 59; 76, (2011/12/04)
Compound of Formula (I): are described, along with pharmaceutically acceptable salts thereof, compositions containing the same, and methods of use thereof in the treatment of cancer.
