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SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.
Forsyth T, Kearney PC, Kim BG, Johnson HW, Aay N, Arcalas A, Brown DS, Chan V, Chen J, Du H, Epshteyn S, Galan AA, Huynh TP, Ibrahim MA, Kane B, Koltun ES, Mann G, Meyr LE, Lee MS, Lewis GL, Noguchi RT, Pack M, Ridgway BH, Shi X, Takeuchi CS, Zu P, Leahy JW, Nuss JM, Aoyama R, Engst S, Gendreau SB, Kassees R, Li J, Lin SH, Martini JF, Stout T, Tong P, Woolfrey J, Zhang W, Yu P. Forsyth T, et al. Among authors: kassees r. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7653-8. doi: 10.1016/j.bmcl.2012.10.007. Epub 2012 Oct 16. Bioorg Med Chem Lett. 2012. PMID: 23127890
Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models.
Lin J, Sampath D, Nannini MA, Lee BB, Degtyarev M, Oeh J, Savage H, Guan Z, Hong R, Kassees R, Lee LB, Risom T, Gross S, Liederer BM, Koeppen H, Skelton NJ, Wallin JJ, Belvin M, Punnoose E, Friedman LS, Lin K. Lin J, et al. Among authors: kassees r. Clin Cancer Res. 2013 Apr 1;19(7):1760-72. doi: 10.1158/1078-0432.CCR-12-3072. Epub 2013 Jan 3. Clin Cancer Res. 2013. PMID: 23287563
GDC-0980 is a novel class I PI3K/mTOR kinase inhibitor with robust activity in cancer models driven by the PI3K pathway.
Wallin JJ, Edgar KA, Guan J, Berry M, Prior WW, Lee L, Lesnick JD, Lewis C, Nonomiya J, Pang J, Salphati L, Olivero AG, Sutherlin DP, O'Brien C, Spoerke JM, Patel S, Lensun L, Kassees R, Ross L, Lackner MR, Sampath D, Belvin M, Friedman LS. Wallin JJ, et al. Among authors: kassees r. Mol Cancer Ther. 2011 Dec;10(12):2426-36. doi: 10.1158/1535-7163.MCT-11-0446. Epub 2011 Oct 13. Mol Cancer Ther. 2011. PMID: 21998291