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Altiratinib Inhibits Tumor Growth, Invasion, Angiogenesis, and Microenvironment-Mediated Drug Resistance via Balanced Inhibition of MET, TIE2, and VEGFR2.
Smith BD, Kaufman MD, Leary CB, Turner BA, Wise SC, Ahn YM, Booth RJ, Caldwell TM, Ensinger CL, Hood MM, Lu WP, Patt TW, Patt WC, Rutkoski TJ, Samarakoon T, Telikepalli H, Vogeti L, Vogeti S, Yates KM, Chun L, Stewart LJ, Clare M, Flynn DL. Smith BD, et al. Among authors: flynn dl. Mol Cancer Ther. 2015 Sep;14(9):2023-34. doi: 10.1158/1535-7163.MCT-14-1105. Epub 2015 Aug 18. Mol Cancer Ther. 2015. PMID: 26285778
The Selective Tie2 Inhibitor Rebastinib Blocks Recruitment and Function of Tie2Hi Macrophages in Breast Cancer and Pancreatic Neuroendocrine Tumors.
Harney AS, Karagiannis GS, Pignatelli J, Smith BD, Kadioglu E, Wise SC, Hood MM, Kaufman MD, Leary CB, Lu WP, Al-Ani G, Chen X, Entenberg D, Oktay MH, Wang Y, Chun L, De Palma M, Jones JG, Flynn DL, Condeelis JS. Harney AS, et al. Among authors: flynn dl. Mol Cancer Ther. 2017 Nov;16(11):2486-2501. doi: 10.1158/1535-7163.MCT-17-0241. Epub 2017 Aug 24. Mol Cancer Ther. 2017. PMID: 28838996 Free PMC article.
Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells.
Henry JR, Kaufman MD, Peng SB, Ahn YM, Caldwell TM, Vogeti L, Telikepalli H, Lu WP, Hood MM, Rutkoski TJ, Smith BD, Vogeti S, Miller D, Wise SC, Chun L, Zhang X, Zhang Y, Kays L, Hipskind PA, Wrobleski AD, Lobb KL, Clay JM, Cohen JD, Walgren JL, McCann D, Patel P, Clawson DK, Guo S, Manglicmot D, Groshong C, Logan C, Starling JJ, Flynn DL. Henry JR, et al. Among authors: flynn dl. J Med Chem. 2015 May 28;58(10):4165-79. doi: 10.1021/acs.jmedchem.5b00067. Epub 2015 May 12. J Med Chem. 2015. PMID: 25965804
Discovery of vimseltinib (DCC-3014), a highly selective CSF1R switch-control kinase inhibitor, in clinical development for the treatment of Tenosynovial Giant Cell Tumor (TGCT).
Caldwell TM, Ahn YM, Bulfer SL, Leary CB, Hood MM, Lu WP, Vogeti L, Vogeti S, Kaufman MD, Wise SC, Le Bourdonnec B, Smith BD, Flynn DL. Caldwell TM, et al. Among authors: flynn dl. Bioorg Med Chem Lett. 2022 Oct 15;74:128928. doi: 10.1016/j.bmcl.2022.128928. Epub 2022 Aug 10. Bioorg Med Chem Lett. 2022. PMID: 35961460 Free article.
Phase 1 dose-finding study of rebastinib (DCC-2036) in patients with relapsed chronic myeloid leukemia and acute myeloid leukemia.
Cortes J, Talpaz M, Smith HP, Snyder DS, Khoury J, Bhalla KN, Pinilla-Ibarz J, Larson R, Mitchell D, Wise SC, Rutkoski TJ, Smith BD, Flynn DL, Kantarjian HM, Rosen O, Van Etten RA. Cortes J, et al. Among authors: flynn dl. Haematologica. 2017 Mar;102(3):519-528. doi: 10.3324/haematol.2016.152710. Epub 2016 Dec 7. Haematologica. 2017. PMID: 27927766 Free PMC article. Clinical Trial.
Ripretinib (DCC-2618) Is a Switch Control Kinase Inhibitor of a Broad Spectrum of Oncogenic and Drug-Resistant KIT and PDGFRA Variants.
Smith BD, Kaufman MD, Lu WP, Gupta A, Leary CB, Wise SC, Rutkoski TJ, Ahn YM, Al-Ani G, Bulfer SL, Caldwell TM, Chun L, Ensinger CL, Hood MM, McKinley A, Patt WC, Ruiz-Soto R, Su Y, Telikepalli H, Town A, Turner BA, Vogeti L, Vogeti S, Yates K, Janku F, Abdul Razak AR, Rosen O, Heinrich MC, Flynn DL. Smith BD, et al. Among authors: flynn dl. Cancer Cell. 2019 May 13;35(5):738-751.e9. doi: 10.1016/j.ccell.2019.04.006. Cancer Cell. 2019. PMID: 31085175 Free article.
Discovery of acyl ureas as highly selective small molecule CSF1R kinase inhibitors.
Caldwell TM, Kaufman MD, Wise SC, Mi Ahn Y, Hood MM, Lu WP, Patt WC, Samarakoon T, Vogeti L, Vogeti S, Yates KM, Bulfer SL, Le Bourdonnec B, Smith BD, Flynn DL. Caldwell TM, et al. Among authors: flynn dl. Bioorg Med Chem Lett. 2022 Oct 15;74:128929. doi: 10.1016/j.bmcl.2022.128929. Epub 2022 Aug 9. Bioorg Med Chem Lett. 2022. PMID: 35961461 Free article.
59 results