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Discovery of KIN-3248, An Irreversible, Next Generation FGFR Inhibitor for the Treatment of Advanced Tumors Harboring FGFR2 and/or FGFR3 Gene Alterations.
Tyhonas JS, Arnold LD, Cox JM, Franovic A, Gardiner E, Grandinetti K, Kania R, Kanouni T, Lardy M, Li C, Martin ES, Miller N, Mohan A, Murphy EA, Perez M, Soroceanu L, Timple N, Uryu S, Womble S, Kaldor SW. Tyhonas JS, et al. Among authors: li c. J Med Chem. 2024 Feb 8;67(3):1734-1746. doi: 10.1021/acs.jmedchem.3c01819. Epub 2024 Jan 24. J Med Chem. 2024. PMID: 38267212
The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition.
Chen YK, Kanouni T, Arnold LD, Cox JM, Gardiner E, Grandinetti K, Jiang P, Kaldor SW, Lee C, Li C, Martin ES, Miller N, Murphy EA, Timple N, Tyhonas JS, Vassar A, Wang TS, Williams R, Yuan D, Kania RS. Chen YK, et al. Among authors: li c. J Med Chem. 2024 Feb 8;67(3):1747-1757. doi: 10.1021/acs.jmedchem.3c01830. Epub 2024 Jan 17. J Med Chem. 2024. PMID: 38230963
The pan-RAF-MEK non degrading molecular glue NST-628 is a potent and brain penetrant inhibitor of the RAS-MAPK pathway with activity across diverse RAS- and RAF-driven cancers.
Ryan MB, Quade B, Schenk N, Fang Z, Zingg M, Cohen SE, Swalm BM, Li C, Ozen A, Ye C, Ritorto MS, Huang X, Dar AC, Han Y, Hoeflich KP, Hale M, Hagel M. Ryan MB, et al. Among authors: li c. Cancer Discov. 2024 Apr 8. doi: 10.1158/2159-8290.CD-24-0139. Online ahead of print. Cancer Discov. 2024. PMID: 38588399
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