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Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor.
Lapierre JM, Eathiraj S, Vensel D, Liu Y, Bull CO, Cornell-Kennon S, Iimura S, Kelleher EW, Kizer DE, Koerner S, Makhija S, Matsuda A, Moussa M, Namdev N, Savage RE, Szwaya J, Volckova E, Westlund N, Wu H, Schwartz B. Lapierre JM, et al. Among authors: eathiraj s. J Med Chem. 2016 Jul 14;59(13):6455-69. doi: 10.1021/acs.jmedchem.6b00619. Epub 2016 Jun 29. J Med Chem. 2016. PMID: 27305487
The BTK Inhibitor ARQ 531 Targets Ibrutinib-Resistant CLL and Richter Transformation.
Reiff SD, Mantel R, Smith LL, Greene JT, Muhowski EM, Fabian CA, Goettl VM, Tran M, Harrington BK, Rogers KA, Awan FT, Maddocks K, Andritsos L, Lehman AM, Sampath D, Lapalombella R, Eathiraj S, Abbadessa G, Schwartz B, Johnson AJ, Byrd JC, Woyach JA. Reiff SD, et al. Among authors: eathiraj s. Cancer Discov. 2018 Oct;8(10):1300-1315. doi: 10.1158/2159-8290.CD-17-1409. Epub 2018 Aug 9. Cancer Discov. 2018. PMID: 30093506 Free PMC article.
The new small tyrosine kinase inhibitor ARQ531 targets acute myeloid leukemia cells by disrupting multiple tumor-addicted programs.
Soncini D, Orecchioni S, Ruberti S, Minetto P, Martinuzzi C, Agnelli L, Todoerti K, Cagnetta A, Miglino M, Clavio M, Contini P, Varaldo R, Bergamaschi M, Guolo F, Passalacqua M, Nencioni A, Monacelli F, Gobbi M, Neri A, Abbadessa G, Eathiraj S, Schwartz B, Bertolini F, Lemoli RM, Cea M. Soncini D, et al. Among authors: eathiraj s. Haematologica. 2020 Oct 1;105(10):2420-2431. doi: 10.3324/haematol.2019.224956. Haematologica. 2020. PMID: 33054082 Free PMC article.
[No title available]
[No authors listed] [No authors listed] PMID: 31624110
Preclinical efficacy for a novel tyrosine kinase inhibitor, ArQule 531 against acute myeloid leukemia.
Elgamal OA, Mehmood A, Jeon JY, Carmichael B, Lehman A, Orwick SJ, Truxall J, Goettl VM, Wasmuth R, Tran M, Mitchell S, Lapalombella R, Eathiraj S, Schwartz B, Stegmaier K, Baker SD, Hertlein E, Byrd JC. Elgamal OA, et al. Among authors: eathiraj s. J Hematol Oncol. 2020 Jan 28;13(1):8. doi: 10.1186/s13045-019-0821-7. J Hematol Oncol. 2020. PMID: 31992353 Free PMC article.
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: eathiraj s. J Med Chem. 2012 Jun 14;55(11):5291-310. doi: 10.1021/jm300276x. Epub 2012 May 31. J Med Chem. 2012. PMID: 22533986
20 results