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Items: 1 to 20 of 91

1.

Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition.

Hoeflich KP, Merchant M, Orr C, Chan J, Den Otter D, Berry L, Kasman I, Koeppen H, Rice K, Yang NY, Engst S, Johnston S, Friedman LS, Belvin M.

Cancer Res. 2012 Jan 1;72(1):210-9. doi: 10.1158/0008-5472.CAN-11-1515. Epub 2011 Nov 14.

2.

Bcl-2/Bcl-xL inhibition increases the efficacy of MEK inhibition alone and in combination with PI3 kinase inhibition in lung and pancreatic tumor models.

Tan N, Wong M, Nannini MA, Hong R, Lee LB, Price S, Williams K, Savy PP, Yue P, Sampath D, Settleman J, Fairbrother WJ, Belmont LD.

Mol Cancer Ther. 2013 Jun;12(6):853-64. doi: 10.1158/1535-7163.MCT-12-0949. Epub 2013 Mar 8.

3.

The novel dual PI3K/mTOR inhibitor GDC-0941 synergizes with the MEK inhibitor U0126 in non-small cell lung cancer cells.

Zou ZQ, Zhang LN, Wang F, Bellenger J, Shen YZ, Zhang XH.

Mol Med Rep. 2012 Feb;5(2):503-8. doi: 10.3892/mmr.2011.682. Epub 2011 Nov 16.

PMID:
22101421
4.

PI3K pathway activation mediates resistance to MEK inhibitors in KRAS mutant cancers.

Wee S, Jagani Z, Xiang KX, Loo A, Dorsch M, Yao YM, Sellers WR, Lengauer C, Stegmeier F.

Cancer Res. 2009 May 15;69(10):4286-93. doi: 10.1158/0008-5472.CAN-08-4765. Epub 2009 Apr 28.

5.

The PI3K inhibitor GDC-0941 combines with existing clinical regimens for superior activity in multiple myeloma.

Munugalavadla V, Mariathasan S, Slaga D, Du C, Berry L, Del Rosario G, Yan Y, Boe M, Sun L, Friedman LS, Chesi M, Leif Bergsagel P, Ebens A.

Oncogene. 2014 Jan 16;33(3):316-25. doi: 10.1038/onc.2012.594. Epub 2013 Jan 14.

PMID:
23318440
6.

GDC-0941, a novel class I selective PI3K inhibitor, enhances the efficacy of docetaxel in human breast cancer models by increasing cell death in vitro and in vivo.

Wallin JJ, Guan J, Prior WW, Lee LB, Berry L, Belmont LD, Koeppen H, Belvin M, Friedman LS, Sampath D.

Clin Cancer Res. 2012 Jul 15;18(14):3901-11. doi: 10.1158/1078-0432.CCR-11-2088. Epub 2012 May 14.

7.

PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts.

Choo EF, Ng CM, Berry L, Belvin M, Lewin-Koh N, Merchant M, Salphati L.

Cancer Chemother Pharmacol. 2013 Jan;71(1):133-43. doi: 10.1007/s00280-012-1988-6. Epub 2012 Oct 7.

PMID:
23053270
8.

Pharmacokinetic-pharmacodynamic modeling of tumor growth inhibition and biomarker modulation by the novel phosphatidylinositol 3-kinase inhibitor GDC-0941.

Salphati L, Wong H, Belvin M, Bradford D, Edgar KA, Prior WW, Sampath D, Wallin JJ.

Drug Metab Dispos. 2010 Sep;38(9):1436-42. doi: 10.1124/dmd.110.032912. Epub 2010 Jun 10.

9.

Modeling targeted inhibition of MEK and PI3 kinase in human pancreatic cancer.

Junttila MR, Devasthali V, Cheng JH, Castillo J, Metcalfe C, Clermont AC, Otter DD, Chan E, Bou-Reslan H, Cao T, Forrest W, Nannini MA, French D, Carano R, Merchant M, Hoeflich KP, Singh M.

Mol Cancer Ther. 2015 Jan;14(1):40-7. doi: 10.1158/1535-7163.MCT-14-0030. Epub 2014 Nov 5.

10.

Predictive biomarkers of sensitivity to the phosphatidylinositol 3' kinase inhibitor GDC-0941 in breast cancer preclinical models.

O'Brien C, Wallin JJ, Sampath D, GuhaThakurta D, Savage H, Punnoose EA, Guan J, Berry L, Prior WW, Amler LC, Belvin M, Friedman LS, Lackner MR.

Clin Cancer Res. 2010 Jul 15;16(14):3670-83. doi: 10.1158/1078-0432.CCR-09-2828. Epub 2010 May 7. Erratum in: Clin Cancer Res. 2011 Apr 1;17(7):2066-7.

11.

mTOR kinase inhibitor potentiates apoptosis of PI3K and MEK inhibitors in diagnostically defined subpopulations.

Vijapurkar U, Robillard L, Zhou S, Degtyarev M, Lin K, Truong T, Tremayne J, Ross LB, Pei Z, Friedman LS, Blackwood EM, Belvin M.

Cancer Lett. 2012 Dec 30;326(2):168-75. doi: 10.1016/j.canlet.2012.08.011. Epub 2012 Aug 16.

PMID:
22902509
12.

[Growth inhibition of combined pathway inhibitors on KRAS mutated non-small cell lung cancer cell line].

Li ZW, Yang ZL, Feng HL, Bian XC, Liu YY, Liu YQ.

Zhonghua Bing Li Xue Za Zhi. 2013 May;42(5):330-5. doi: 10.3760/cma.j.issn.0529-5807.2013.05.009. Chinese.

PMID:
24004591
13.

In vivo antitumor activity of MEK and phosphatidylinositol 3-kinase inhibitors in basal-like breast cancer models.

Hoeflich KP, O'Brien C, Boyd Z, Cavet G, Guerrero S, Jung K, Januario T, Savage H, Punnoose E, Truong T, Zhou W, Berry L, Murray L, Amler L, Belvin M, Friedman LS, Lackner MR.

Clin Cancer Res. 2009 Jul 15;15(14):4649-64. doi: 10.1158/1078-0432.CCR-09-0317. Epub 2009 Jun 30.

14.

The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .

Folkes AJ, Ahmadi K, Alderton WK, Alix S, Baker SJ, Box G, Chuckowree IS, Clarke PA, Depledge P, Eccles SA, Friedman LS, Hayes A, Hancox TC, Kugendradas A, Lensun L, Moore P, Olivero AG, Pang J, Patel S, Pergl-Wilson GH, Raynaud FI, Robson A, Saghir N, Salphati L, Sohal S, Ultsch MH, Valenti M, Wallweber HJ, Wan NC, Wiesmann C, Workman P, Zhyvoloup A, Zvelebil MJ, Shuttleworth SJ.

J Med Chem. 2008 Sep 25;51(18):5522-32. doi: 10.1021/jm800295d.

PMID:
18754654
15.

Preclinical pharmacokinetics of the novel PI3K inhibitor GDC-0941 and prediction of its pharmacokinetics and efficacy in human.

Salphati L, Pang J, Plise EG, Chou B, Halladay JS, Olivero AG, Rudewicz PJ, Tian Q, Wong S, Zhang X.

Xenobiotica. 2011 Dec;41(12):1088-99. doi: 10.3109/00498254.2011.603384. Epub 2011 Aug 13.

PMID:
21838594
17.

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.

18.

Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models.

Lin J, Sampath D, Nannini MA, Lee BB, Degtyarev M, Oeh J, Savage H, Guan Z, Hong R, Kassees R, Lee LB, Risom T, Gross S, Liederer BM, Koeppen H, Skelton NJ, Wallin JJ, Belvin M, Punnoose E, Friedman LS, Lin K.

Clin Cancer Res. 2013 Apr 1;19(7):1760-72. doi: 10.1158/1078-0432.CCR-12-3072. Epub 2013 Jan 3.

19.

Phosphoproteomic characterization of DNA damage response in melanoma cells following MEK/PI3K dual inhibition.

Kirkpatrick DS, Bustos DJ, Dogan T, Chan J, Phu L, Young A, Friedman LS, Belvin M, Song Q, Bakalarski CE, Hoeflich KP.

Proc Natl Acad Sci U S A. 2013 Nov 26;110(48):19426-31. doi: 10.1073/pnas.1309473110. Epub 2013 Nov 11. Erratum in: Proc Natl Acad Sci U S A. 2014 Jan 7;111(1):562.

20.

Blockade of the extracellular signal-regulated kinase pathway enhances the therapeutic efficacy of microtubule-destabilizing agents in human tumor xenograft models.

Watanabe K, Tanimura S, Uchiyama A, Sakamoto T, Kawabata T, Ozaki K, Kohno M.

Clin Cancer Res. 2010 Feb 15;16(4):1170-8. doi: 10.1158/1078-0432.CCR-09-2482. Epub 2010 Feb 9.

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