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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: schwartz b. Haematologica. 2020 Oct 1;105(10):2420-2431. doi: 10.3324/haematol.2019.224956. Haematologica. 2020. PMID: 33054082 Free PMC article.
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: schwartz b. 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
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: schwartz b. 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.
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: schwartz b. 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.
2,420 results