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In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials.
DePinto W, Chu XJ, Yin X, Smith M, Packman K, Goelzer P, Lovey A, Chen Y, Qian H, Hamid R, Xiang Q, Tovar C, Blain R, Nevins T, Higgins B, Luistro L, Kolinsky K, Felix B, Hussain S, Heimbrook D. DePinto W, et al. Among authors: higgins b. Mol Cancer Ther. 2006 Nov;5(11):2644-58. doi: 10.1158/1535-7163.MCT-06-0355. Mol Cancer Ther. 2006. PMID: 17121911
Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6- methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity.
Chu XJ, DePinto W, Bartkovitz D, So SS, Vu BT, Packman K, Lukacs C, Ding Q, Jiang N, Wang K, Goelzer P, Yin X, Smith MA, Higgins BX, Chen Y, Xiang Q, Moliterni J, Kaplan G, Graves B, Lovey A, Fotouhi N. Chu XJ, et al. Among authors: higgins bx. J Med Chem. 2006 Nov 2;49(22):6549-60. doi: 10.1021/jm0606138. J Med Chem. 2006. PMID: 17064073
Characterization of a novel mitogen-activated protein kinase kinase 1/2 inhibitor with a unique mechanism of action for cancer therapy.
Daouti S, Wang H, Li WH, Higgins B, Kolinsky K, Packman K, Specian A Jr, Kong N, Huby N, Wen Y, Xiang Q, Podlaski FJ, He Y, Fotouhi N, Heimbrook D, Niu H. Daouti S, et al. Among authors: higgins b. Cancer Res. 2009 Mar 1;69(5):1924-32. doi: 10.1158/0008-5472.CAN-08-2627. Epub 2009 Feb 24. Cancer Res. 2009. PMID: 19244124
Preclinical in vivo evaluation of efficacy, pharmacokinetics, and pharmacodynamics of a novel MEK1/2 kinase inhibitor RO5068760 in multiple tumor models.
Daouti S, Higgins B, Kolinsky K, Packman K, Wang H, Rizzo C, Moliterni J, Huby N, Fotouhi N, Liu M, Goelzer P, Sandhu HK, Li JK, Railkar A, Heimbrook D, Niu H. Daouti S, et al. Among authors: higgins b. Mol Cancer Ther. 2010 Jan;9(1):134-44. doi: 10.1158/1535-7163.MCT-09-0601. Epub 2010 Jan 6. Mol Cancer Ther. 2010. PMID: 20053779
462 results