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Table representation of search results timeline featuring number of search results per year.

Year Number of Results
2007 2
2008 5
2009 6
2010 5
2011 9
2012 10
2013 5
2014 4
2015 11
2016 3
2017 1
2018 7
2019 4
2020 2
2021 5
2022 5
2023 2
2024 2

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77 results

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Page 1
A phase I study of danusertib (PHA-739358) in adult patients with accelerated or blastic phase chronic myeloid leukemia and Philadelphia chromosome-positive acute lymphoblastic leukemia resistant or intolerant to imatinib and/or other second generation c-ABL therapy.
Borthakur G, Dombret H, Schafhausen P, Brummendorf TH, Boissel N, Jabbour E, Mariani M, Capolongo L, Carpinelli P, Davite C, Kantarjian H, Cortes JE. Borthakur G, et al. Haematologica. 2015 Jul;100(7):898-904. doi: 10.3324/haematol.2014.115279. Epub 2015 Apr 17. Haematologica. 2015. PMID: 25887498 Free PMC article. Clinical Trial.
Danusertib is a pan-aurora kinase inhibitor with potent activity against Abl kinase including the gatekeeper T315I mutant. ...Two dosing schedules were studied: schedule A, in which danusertib was given by 3-hour intravenous infusion daily for 7 consecutive days (da …
Danusertib is a pan-aurora kinase inhibitor with potent activity against Abl kinase including the gatekeeper T315I mutant. ...Two dos …
Danusertib (formerly PHA-739358)--a novel combined pan-Aurora kinases and third generation Bcr-Abl tyrosine kinase inhibitor.
Gontarewicz A, Brümmendorf TH. Gontarewicz A, et al. Recent Results Cancer Res. 2010;184:199-214. doi: 10.1007/978-3-642-01222-8_14. Recent Results Cancer Res. 2010. PMID: 20072840 Review.
Among those, one of the most advanced clinical compound currently is Danusertib (formerly PHA-739358), which exhibits inhibitory activity against all known Aurora kinases as well as other cancer-relevant kinases such as the Bcr-Abl tyrosine kinase, including …
Among those, one of the most advanced clinical compound currently is Danusertib (formerly PHA-739358), which exhibits i …
Treatment of human pre-B acute lymphoblastic leukemia with the Aurora kinase inhibitor PHA-739358 (Danusertib).
Fei F, Lim M, Schmidhuber S, Moll J, Groffen J, Heisterkamp N. Fei F, et al. Mol Cancer. 2012 Jun 21;11:42. doi: 10.1186/1476-4598-11-42. Mol Cancer. 2012. PMID: 22721004 Free PMC article.
PHA-739358 further effectively blocked Bcr/Abl tyrosine kinase activity and Aurora kinase B in vivo, and mice transplanted with human Bcr/Abl T315I ALL cells treated with a 3x 7-day cycle of PHA-739358 as mono-treatment had significantly longer surviva …
PHA-739358 further effectively blocked Bcr/Abl tyrosine kinase activity and Aurora kinase B in vivo, and mice transplanted wit …
Danusertib, an aurora kinase inhibitor.
Meulenbeld HJ, Mathijssen RH, Verweij J, de Wit R, de Jonge MJ. Meulenbeld HJ, et al. Expert Opin Investig Drugs. 2012 Mar;21(3):383-93. doi: 10.1517/13543784.2012.652303. Epub 2012 Jan 13. Expert Opin Investig Drugs. 2012. PMID: 22242557 Review.
The use of several small molecule aurora kinase inhibitors as potential anticancer therapeutic is being investigated. Danusertib (formerly PHA-739358) is a small ATP competitive molecule that inhibits aurora A, B and C kinases. ...As a single agent, danuse …
The use of several small molecule aurora kinase inhibitors as potential anticancer therapeutic is being investigated. Danusertib (for …
A phase I dose-escalation study of danusertib (PHA-739358) administered as a 24-hour infusion with and without granulocyte colony-stimulating factor in a 14-day cycle in patients with advanced solid tumors.
Cohen RB, Jones SF, Aggarwal C, von Mehren M, Cheng J, Spigel DR, Greco FA, Mariani M, Rocchetti M, Ceruti R, Comis S, Laffranchi B, Moll J, Burris HA. Cohen RB, et al. Clin Cancer Res. 2009 Nov 1;15(21):6694-701. doi: 10.1158/1078-0432.CCR-09-1445. Epub 2009 Oct 13. Clin Cancer Res. 2009. PMID: 19825950 Free PMC article. Clinical Trial.
PURPOSE: This study was conducted to assess the safety, tolerability, pharmacokinetics, and pharmacodynamics of the i.v. pan-aurora kinase inhibitor PHA-739358, danusertib, in patients with advanced solid tumors. EXPERIMENTAL DESIGN: In part 1, patients recei …
PURPOSE: This study was conducted to assess the safety, tolerability, pharmacokinetics, and pharmacodynamics of the i.v. pan-aurora kinase i …
Targeting aurora kinases with danusertib (PHA-739358) inhibits growth of liver metastases from gastroenteropancreatic neuroendocrine tumors in an orthotopic xenograft model.
Fraedrich K, Schrader J, Ittrich H, Keller G, Gontarewicz A, Matzat V, Kromminga A, Pace A, Moll J, Bläker M, Lohse AW, Hörsch D, Brümmendorf TH, Benten D. Fraedrich K, et al. Clin Cancer Res. 2012 Sep 1;18(17):4621-32. doi: 10.1158/1078-0432.CCR-11-2968. Epub 2012 Jul 2. Clin Cancer Res. 2012. PMID: 22753592
EXPERIMENTAL DESIGN: Human GEP-NETs were tested for aurora kinase expression. The efficacy of the new aurora kinase inhibitor danusertib was evaluated in two human GEP-NET cell lines (BON1 and QGP) in vitro and in vivo. ...Decreased phosphorylation of histone H3 indicated …
EXPERIMENTAL DESIGN: Human GEP-NETs were tested for aurora kinase expression. The efficacy of the new aurora kinase inhibitor danusertib …
The pan-Aurora kinase inhibitor, PHA-739358, induces apoptosis and inhibits migration in melanoma cell lines.
Xie L, Meyskens FL Jr. Xie L, et al. Melanoma Res. 2013 Apr;23(2):102-13. doi: 10.1097/CMR.0b013e32835df5e4. Melanoma Res. 2013. PMID: 23344158 Free PMC article.
In this study, the antiproliferative and anti-invasive effects of PHA-739358 were investigated in melanoma cell lines. The results demonstrated that PHA-739358 produces a time-dependent and dose-dependent inhibition of cell proliferation, induction of …
In this study, the antiproliferative and anti-invasive effects of PHA-739358 were investigated in melanoma cell lines. The res …
PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer.
Carpinelli P, Ceruti R, Giorgini ML, Cappella P, Gianellini L, Croci V, Degrassi A, Texido G, Rocchetti M, Vianello P, Rusconi L, Storici P, Zugnoni P, Arrigoni C, Soncini C, Alli C, Patton V, Marsiglio A, Ballinari D, Pesenti E, Fancelli D, Moll J. Carpinelli P, et al. Mol Cancer Ther. 2007 Dec;6(12 Pt 1):3158-68. doi: 10.1158/1535-7163.MCT-07-0444. Mol Cancer Ther. 2007. PMID: 18089710
PHA-739358 is a small-molecule 3-aminopyrazole derivative with strong activity against Aurora kinases and cross-reactivities with some receptor tyrosine kinases relevant for cancer. PHA-739358 inhibits all Aurora kinase family members and shows a domin …
PHA-739358 is a small-molecule 3-aminopyrazole derivative with strong activity against Aurora kinases and cross-reactivities w …
Aurora kinase inhibitor PHA-739358 suppresses growth of hepatocellular carcinoma in vitro and in a xenograft mouse model.
Benten D, Keller G, Quaas A, Schrader J, Gontarewicz A, Balabanov S, Braig M, Wege H, Moll J, Lohse AW, Brummendorf TH. Benten D, et al. Neoplasia. 2009 Sep;11(9):934-44. doi: 10.1593/neo.09664. Neoplasia. 2009. PMID: 19724687 Free PMC article.
At concentrations exceeding 50 nM, PHA-739358 completely suppressed tumor cell proliferation in cell culture experiments and strongly decreased histone H3 phosphorylation. ...Remarkably, when tumors restarted to grow under sorafenib monotherapy, subsequent treatment …
At concentrations exceeding 50 nM, PHA-739358 completely suppressed tumor cell proliferation in cell culture experiments and s …
Phase I pharmacokinetic and pharmacodynamic study of the aurora kinase inhibitor danusertib in patients with advanced or metastatic solid tumors.
Steeghs N, Eskens FA, Gelderblom H, Verweij J, Nortier JW, Ouwerkerk J, van Noort C, Mariani M, Spinelli R, Carpinelli P, Laffranchi B, de Jonge MJ. Steeghs N, et al. J Clin Oncol. 2009 Oct 20;27(30):5094-101. doi: 10.1200/JCO.2008.21.6655. Epub 2009 Sep 21. J Clin Oncol. 2009. PMID: 19770380 Clinical Trial.
PURPOSE: Danusertib (PHA-739358) is a small-molecule pan-aurora kinase inhibitor. ...The maximum-tolerated dose was 330 mg/m(2) for the 6-hour IVS and was not identified for the 3-hour IVS. The systemic exposure to danusertib increased linearly with do …
PURPOSE: Danusertib (PHA-739358) is a small-molecule pan-aurora kinase inhibitor. ...The maximum-tolerated dose was 330 …
77 results