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Items: 6

1.

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.

Clin Cancer Res. 2013 Apr 1;19(7):1760-72. doi: 10.1158/1078-0432.CCR-12-3072. Epub 2013 Jan 3.

2.

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.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7653-8. doi: 10.1016/j.bmcl.2012.10.007. Epub 2012 Oct 16.

PMID:
23127890
3.

Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions.

Choo EF, Belvin M, Boggs J, Deng Y, Hoeflich KP, Ly J, Merchant M, Orr C, Plise E, Robarge K, Martini JF, Kassees R, Aoyama RG, Ramaiya A, Johnston SH.

Drug Metab Dispos. 2012 May;40(5):919-27. doi: 10.1124/dmd.111.043778. Epub 2012 Feb 7.

PMID:
22315332
4.

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.

Mol Cancer Ther. 2011 Dec;10(12):2426-36. doi: 10.1158/1535-7163.MCT-11-0446. Epub 2011 Oct 13.

5.

Navitoclax enhances the efficacy of taxanes in non-small cell lung cancer models.

Tan N, Malek M, Zha J, Yue P, Kassees R, Berry L, Fairbrother WJ, Sampath D, Belmont LD.

Clin Cancer Res. 2011 Mar 15;17(6):1394-404. doi: 10.1158/1078-0432.CCR-10-2353. Epub 2011 Jan 10.

6.

Nuclear phospho-Akt increase predicts synergy of PI3K inhibition and doxorubicin in breast and ovarian cancer.

Wallin JJ, Guan J, Prior WW, Edgar KA, Kassees R, Sampath D, Belvin M, Friedman LS.

Sci Transl Med. 2010 Sep 8;2(48):48ra66. doi: 10.1126/scitranslmed.3000630.

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