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Cellular and in vivo activity of a novel PI3K inhibitor, PX-866, against human glioblastoma.

Koul D, Shen R, Kim YW, Kondo Y, Lu Y, Bankson J, Ronen SM, Kirkpatrick DL, Powis G, Yung WK.

Neuro Oncol. 2010 Jun;12(6):559-69. doi: 10.1093/neuonc/nop058. Epub 2010 Feb 15.


Combined action of the dinuclear platinum compound BBR3610 with the PI3-K inhibitor PX-866 in glioblastoma.

Gwak HS, Shingu T, Chumbalkar V, Hwang YH, DeJournett R, Latha K, Koul D, Alfred Yung WK, Powis G, Farrell NP, Bögler O.

Int J Cancer. 2011 Feb 15;128(4):787-96. doi: 10.1002/ijc.25394.


The phosphatidylinositol 3-kinase inhibitor, PX-866, is a potent inhibitor of cancer cell motility and growth in three-dimensional cultures.

Howes AL, Chiang GG, Lang ES, Ho CB, Powis G, Vuori K, Abraham RT.

Mol Cancer Ther. 2007 Sep;6(9):2505-14. Epub 2007 Aug 31.


Peroxisome proliferator-activated receptor gamma agonist pioglitazone prevents the hyperglycemia caused by phosphatidylinositol 3-kinase pathway inhibition by PX-866 without affecting antitumor activity.

Ihle NT, Lemos R, Schwartz D, Oh J, Halter RJ, Wipf P, Kirkpatrick L, Powis G.

Mol Cancer Ther. 2009 Jan;8(1):94-100. doi: 10.1158/1535-7163.MCT-08-0714.


Comparative effect of two pan-class I PI3K inhibitors used as anticancer drugs on human T cell function.

Blanco B, Herrero-Sánchez C, Rodríguez-Serrano C, Sánchez-Barba M, Del Cañizo MC.

Int Immunopharmacol. 2015 Sep;28(1):675-85. doi: 10.1016/j.intimp.2015.07.032. Epub 2015 Aug 5.


Combinatorial therapy with adenoviral-mediated PTEN and a PI3K inhibitor suppresses malignant glioma cell growth in vitro and in vivo by regulating the PI3K/AKT signaling pathway.

Nan Y, Guo L, Song Y, Wang L, Yu K, Huang Q, Zhong Y.

J Cancer Res Clin Oncol. 2017 Aug;143(8):1477-1487. doi: 10.1007/s00432-017-2415-5. Epub 2017 Apr 11.


Phase II study of PX-866 in recurrent glioblastoma.

Pitz MW, Eisenhauer EA, MacNeil MV, Thiessen B, Easaw JC, Macdonald DR, Eisenstat DD, Kakumanu AS, Salim M, Chalchal H, Squire J, Tsao MS, Kamel-Reid S, Banerji S, Tu D, Powers J, Hausman DF, Mason WP.

Neuro Oncol. 2015 Sep;17(9):1270-4. doi: 10.1093/neuonc/nou365. Epub 2015 Jan 20.


Molecular pharmacology and antitumor activity of PX-866, a novel inhibitor of phosphoinositide-3-kinase signaling.

Ihle NT, Williams R, Chow S, Chew W, Berggren MI, Paine-Murrieta G, Minion DJ, Halter RJ, Wipf P, Abraham R, Kirkpatrick L, Powis G.

Mol Cancer Ther. 2004 Jul;3(7):763-72.


Targeting the AKT pathway in glioblastoma.

McDowell KA, Riggins GJ, Gallia GL.

Curr Pharm Des. 2011;17(23):2411-20. Review.


Sorafenib/regorafenib and phosphatidyl inositol 3 kinase/thymoma viral proto-oncogene inhibition interact to kill tumor cells.

Sajithlal GB, Hamed HA, Cruickshanks N, Booth L, Tavallai S, Syed J, Grant S, Poklepovic A, Dent P.

Mol Pharmacol. 2013 Oct;84(4):562-71. doi: 10.1124/mol.113.088005. Epub 2013 Jul 22.


Noninvasive detection of target modulation following phosphatidylinositol 3-kinase inhibition using hyperpolarized 13C magnetic resonance spectroscopy.

Ward CS, Venkatesh HS, Chaumeil MM, Brandes AH, Vancriekinge M, Dafni H, Sukumar S, Nelson SJ, Vigneron DB, Kurhanewicz J, James CD, Haas-Kogan DA, Ronen SM.

Cancer Res. 2010 Feb 15;70(4):1296-305. doi: 10.1158/0008-5472.CAN-09-2251. Epub 2010 Feb 9.


In vivo activity of combined PI3K/mTOR and MEK inhibition in a Kras(G12D);Pten deletion mouse model of ovarian cancer.

Kinross KM, Brown DV, Kleinschmidt M, Jackson S, Christensen J, Cullinane C, Hicks RJ, Johnstone RW, McArthur GA.

Mol Cancer Ther. 2011 Aug;10(8):1440-9. doi: 10.1158/1535-7163.MCT-11-0240. Epub 2011 Jun 1.


Inhibition of cathepsin S induces autophagy and apoptosis in human glioblastoma cell lines through ROS-mediated PI3K/AKT/mTOR/p70S6K and JNK signaling pathways.

Zhang L, Wang H, Xu J, Zhu J, Ding K.

Toxicol Lett. 2014 Aug 4;228(3):248-59. doi: 10.1016/j.toxlet.2014.05.015. Epub 2014 May 27.


Enhanced expression of proapoptotic and autophagic proteins involved in the cell death of glioblastoma induced by synthetic glycans.

Faried A, Arifin MZ, Ishiuchi S, Kuwano H, Yazawa S.

J Neurosurg. 2014 Jun;120(6):1298-308. doi: 10.3171/2014.1.JNS131534. Epub 2014 Mar 28.


Identification of novel synergistic targets for rational drug combinations with PI3 kinase inhibitors using siRNA synthetic lethality screening against GBM.

Kim YW, Liu TJ, Koul D, Tiao N, Feroze AH, Wang J, Powis G, Yung WK.

Neuro Oncol. 2011 Apr;13(4):367-75. doi: 10.1093/neuonc/nor012.


A randomized, phase 2 trial of docetaxel with or without PX-866, an irreversible oral phosphatidylinositol 3-kinase inhibitor, in patients with relapsed or metastatic head and neck squamous cell cancer.

Jimeno A, Bauman JE, Weissman C, Adkins D, Schnadig I, Beauregard P, Bowles DW, Spira A, Levy B, Seetharamu N, Hausman D, Walker L, Rudin CM, Shirai K.

Oral Oncol. 2015 Apr;51(4):383-8. doi: 10.1016/j.oraloncology.2014.12.013. Epub 2015 Jan 13.


Lactate and choline metabolites detected in vitro by nuclear magnetic resonance spectroscopy are potential metabolic biomarkers for PI3K inhibition in pediatric glioblastoma.

Al-Saffar NM, Marshall LV, Jackson LE, Balarajah G, Eykyn TR, Agliano A, Clarke PA, Jones C, Workman P, Pearson AD, Leach MO.

PLoS One. 2014 Aug 1;9(8):e103835. doi: 10.1371/journal.pone.0103835. eCollection 2014.


Aurora-A inhibition offers a novel therapy effective against intracranial glioblastoma.

Van Brocklyn JR, Wojton J, Meisen WH, Kellough DA, Ecsedy JA, Kaur B, Lehman NL.

Cancer Res. 2014 Oct 1;74(19):5364-70. doi: 10.1158/0008-5472.CAN-14-0386. Epub 2014 Aug 8.

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