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Discovery and optimization of a series of 3-(3-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amines: orally bioavailable, selective, and potent ATP-independent Akt inhibitors.
Ashwell MA, Lapierre JM, Brassard C, Bresciano K, Bull C, Cornell-Kennon S, Eathiraj S, France DS, Hall T, Hill J, Kelleher E, Khanapurkar S, Kizer D, Koerner S, Link J, Liu Y, Makhija S, Moussa M, Namdev N, Nguyen K, Nicewonger R, Palma R, Szwaya J, Tandon M, Uppalapati U, Vensel D, Volak LP, Volckova E, Westlund N, Wu H, Yang RY, Chan TC. Ashwell MA, et al. Among authors: hall t. J Med Chem. 2012 Jun 14;55(11):5291-310. doi: 10.1021/jm300276x. Epub 2012 May 31. J Med Chem. 2012. PMID: 22533986
Development and validation of a liquid chromatography-tandem mass spectrometry method for the determination of ARQ 501 (beta-lapachone) in plasma and tumors from nu/nu mouse xenografts.
Savage RE, Hall T, Bresciano K, Bailey J, Starace M, Chan TC. Savage RE, et al. Among authors: hall t. J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Sep 1;872(1-2):148-53. doi: 10.1016/j.jchromb.2008.07.031. Epub 2008 Jul 31. J Chromatogr B Analyt Technol Biomed Life Sci. 2008. PMID: 18706870
Antitumor Activity of a Novel Fibroblast Growth Factor Receptor Inhibitor for Intrahepatic Cholangiocarcinoma.
Raggi C, Fiaccadori K, Pastore M, Correnti M, Piombanti B, Forti E, Navari N, Abbadessa G, Hall T, Destro A, Di Tommaso L, Roncalli M, Meng F, Glaser S, Rovida E, Peraldo-Neia C, Olaizola P, Banales JM, Gerussi A, Elvevi A, Droz Dit Busset M, Bhoori S, Mazzaferro V, Alpini G, Marra F, Invernizzi P. Raggi C, et al. Among authors: hall t. Am J Pathol. 2019 Oct;189(10):2090-2101. doi: 10.1016/j.ajpath.2019.06.007. Epub 2019 Jul 24. Am J Pathol. 2019. PMID: 31351075 Free article.
ARQ 087 inhibits FGFR signaling and rescues aberrant cell proliferation and differentiation in experimental models of craniosynostoses and chondrodysplasias caused by activating mutations in FGFR1, FGFR2 and FGFR3.
Balek L, Gudernova I, Vesela I, Hampl M, Oralova V, Kunova Bosakova M, Varecha M, Nemec P, Hall T, Abbadessa G, Hatch N, Buchtova M, Krejci P. Balek L, et al. Among authors: hall t. Bone. 2017 Dec;105:57-66. doi: 10.1016/j.bone.2017.08.016. Epub 2017 Aug 18. Bone. 2017. PMID: 28826843
A Phase 1 study of ARQ 087, an oral pan-FGFR inhibitor in patients with advanced solid tumours.
Papadopoulos KP, El-Rayes BF, Tolcher AW, Patnaik A, Rasco DW, Harvey RD, LoRusso PM, Sachdev JC, Abbadessa G, Savage RE, Hall T, Schwartz B, Wang Y, Kazakin J, Shaib WL. Papadopoulos KP, et al. Among authors: hall t. Br J Cancer. 2017 Nov 21;117(11):1592-1599. doi: 10.1038/bjc.2017.330. Epub 2017 Oct 3. Br J Cancer. 2017. PMID: 28972963 Free PMC article. Clinical Trial.
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