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BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR.

Carboni JM, Wittman M, Yang Z, Lee F, Greer A, Hurlburt W, Hillerman S, Cao C, Cantor GH, Dell-John J, Chen C, Discenza L, Menard K, Li A, Trainor G, Vyas D, Kramer R, Attar RM, Gottardis MM.

Mol Cancer Ther. 2009 Dec;8(12):3341-9. doi: 10.1158/1535-7163.MCT-09-0499.


BMS-754807, a small-molecule inhibitor of insulin-like growth factor-1 receptor/insulin receptor, enhances gemcitabine response in pancreatic cancer.

Awasthi N, Zhang C, Ruan W, Schwarz MA, Schwarz RE.

Mol Cancer Ther. 2012 Dec;11(12):2644-53. doi: 10.1158/1535-7163.MCT-12-0447. Epub 2012 Oct 9.


Differential mechanisms of acquired resistance to insulin-like growth factor-i receptor antibody therapy or to a small-molecule inhibitor, BMS-754807, in a human rhabdomyosarcoma model.

Huang F, Hurlburt W, Greer A, Reeves KA, Hillerman S, Chang H, Fargnoli J, Graf Finckenstein F, Gottardis MM, Carboni JM.

Cancer Res. 2010 Sep 15;70(18):7221-31. doi: 10.1158/0008-5472.CAN-10-0391. Epub 2010 Aug 31.


High IGF-IR activity in triple-negative breast cancer cell lines and tumorgrafts correlates with sensitivity to anti-IGF-IR therapy.

Litzenburger BC, Creighton CJ, Tsimelzon A, Chan BT, Hilsenbeck SG, Wang T, Carboni JM, Gottardis MM, Huang F, Chang JC, Lewis MT, Rimawi MF, Lee AV.

Clin Cancer Res. 2011 Apr 15;17(8):2314-27. doi: 10.1158/1078-0432.CCR-10-1903. Epub 2010 Dec 22.


Dual IGF-1R/InsR inhibitor BMS-754807 synergizes with hormonal agents in treatment of estrogen-dependent breast cancer.

Hou X, Huang F, Macedo LF, Harrington SC, Reeves KA, Greer A, Finckenstein FG, Brodie A, Gottardis MM, Carboni JM, Haluska P.

Cancer Res. 2011 Dec 15;71(24):7597-607. doi: 10.1158/0008-5472.CAN-11-1080. Epub 2011 Oct 31.


Antitumor activity of GSK1904529A, a small-molecule inhibitor of the insulin-like growth factor-I receptor tyrosine kinase.

Sabbatini P, Rowand JL, Groy A, Korenchuk S, Liu Q, Atkins C, Dumble M, Yang J, Anderson K, Wilson BJ, Emmitte KA, Rabindran SK, Kumar R.

Clin Cancer Res. 2009 May 1;15(9):3058-67. doi: 10.1158/1078-0432.CCR-08-2530. Epub 2009 Apr 21.


In vitro and in vivo antitumor effects of the dual insulin-like growth factor-I/insulin receptor inhibitor, BMS-554417.

Haluska P, Carboni JM, Loegering DA, Lee FY, Wittman M, Saulnier MG, Frennesson DB, Kalli KR, Conover CA, Attar RM, Kaufmann SH, Gottardis M, Erlichman C.

Cancer Res. 2006 Jan 1;66(1):362-71.


Combined Inhibition of IGF-1R/IR and Src family kinases enhances antitumor effects in prostate cancer by decreasing activated survival pathways.

Dayyani F, Parikh NU, Varkaris AS, Song JH, Moorthy S, Chatterji T, Maity SN, Wolfe AR, Carboni JM, Gottardis MM, Logothetis CJ, Gallick GE.

PLoS One. 2012;7(12):e51189. doi: 10.1371/journal.pone.0051189. Epub 2012 Dec 26.


IGF-1R Inhibition Activates a YES/SFK Bypass Resistance Pathway: Rational Basis for Co-Targeting IGF-1R and Yes/SFK Kinase in Rhabdomyosarcoma.

Wan X, Yeung C, Heske C, Mendoza A, Helman LJ.

Neoplasia. 2015 Apr;17(4):358-66. doi: 10.1016/j.neo.2015.03.001.


Augmentation of response to nab-paclitaxel by inhibition of insulin-like growth factor (IGF) signaling in preclinical pancreatic cancer models.

Awasthi N, Scire E, Monahan S, Grojean M, Zhang E, Schwarz MA, Schwarz RE.

Oncotarget. 2016 Jul 26;7(30):46988-47001. doi: 10.18632/oncotarget.9029.


BMS-754807 is cytotoxic to non-small cell lung cancer cells and enhances the effects of platinum chemotherapeutics in the human lung cancer cell line A549.

Franks SE, Jones RA, Briah R, Murray P, Moorehead RA.

BMC Res Notes. 2016 Mar 1;9:134. doi: 10.1186/s13104-016-1919-4.


A pilot study for the early assessment of the effects of BMS-754807 plus gefitinib in an H292 tumor model by [(18)F]fluorothymidine-positron emission tomography.

Lee SJ, Kim EJ, Lee HJ, Kim SY, Oh SJ, Ryu JS, Moon DH, Ahn JH, Kim SW.

Invest New Drugs. 2013 Jun;31(3):506-15. doi: 10.1007/s10637-012-9874-y. Epub 2012 Sep 18.


IRS2 copy number gain, KRAS and BRAF mutation status as predictive biomarkers for response to the IGF-1R/IR inhibitor BMS-754807 in colorectal cancer cell lines.

Huang F, Chang H, Greer A, Hillerman S, Reeves KA, Hurlburt W, Cogswell J, Patel D, Qi Z, Fairchild C, Ryseck RP, Wong TW, Finckenstein FG, Jackson J, Carboni JM.

Mol Cancer Ther. 2015 Feb;14(2):620-30. doi: 10.1158/1535-7163.MCT-14-0794-T. Epub 2014 Dec 19.


AMG 479, a fully human anti-insulin-like growth factor receptor type I monoclonal antibody, inhibits the growth and survival of pancreatic carcinoma cells.

Beltran PJ, Mitchell P, Chung YA, Cajulis E, Lu J, Belmontes B, Ho J, Tsai MM, Zhu M, Vonderfecht S, Baserga R, Kendall R, Radinsky R, Calzone FJ.

Mol Cancer Ther. 2009 May;8(5):1095-105. doi: 10.1158/1535-7163.MCT-08-1171. Epub 2009 Apr 14.


Insulin receptor (IR) pathway hyperactivity in IGF-IR null cells and suppression of downstream growth signaling using the dual IGF-IR/IR inhibitor, BMS-754807.

Dinchuk JE, Cao C, Huang F, Reeves KA, Wang J, Myers F, Cantor GH, Zhou X, Attar RM, Gottardis M, Carboni JM.

Endocrinology. 2010 Sep;151(9):4123-32. doi: 10.1210/en.2010-0032. Epub 2010 Jul 7.


A novel, potent, and selective insulin-like growth factor-I receptor kinase inhibitor blocks insulin-like growth factor-I receptor signaling in vitro and inhibits insulin-like growth factor-I receptor dependent tumor growth in vivo.

Ji QS, Mulvihill MJ, Rosenfeld-Franklin M, Cooke A, Feng L, Mak G, O'Connor M, Yao Y, Pirritt C, Buck E, Eyzaguirre A, Arnold LD, Gibson NW, Pachter JA.

Mol Cancer Ther. 2007 Aug;6(8):2158-67. Epub 2007 Aug 1.


Initial testing (stage 1) of the IGF-1 receptor inhibitor BMS-754807 by the pediatric preclinical testing program.

Kolb EA, Gorlick R, Lock R, Carol H, Morton CL, Keir ST, Reynolds CP, Kang MH, Maris JM, Billups C, Smith MA, Houghton PJ.

Pediatr Blood Cancer. 2011 Apr;56(4):595-603. doi: 10.1002/pbc.22741. Epub 2010 Dec 22.


Efficacy of ganitumab (AMG 479), alone and in combination with rapamycin, in Ewing's and osteogenic sarcoma models.

Beltran PJ, Chung YA, Moody G, Mitchell P, Cajulis E, Vonderfecht S, Kendall R, Radinsky R, Calzone FJ.

J Pharmacol Exp Ther. 2011 Jun;337(3):644-54. doi: 10.1124/jpet.110.178400. Epub 2011 Mar 8.


Enhancement of doxorubicin cytotoxicity of human cancer cells by tyrosine kinase inhibition of insulin receptor and type I IGF receptor.

Zeng X, Zhang H, Oh A, Zhang Y, Yee D.

Breast Cancer Res Treat. 2012 May;133(1):117-26. doi: 10.1007/s10549-011-1713-x. Epub 2011 Aug 18.


The mechanisms of differential sensitivity to an insulin-like growth factor-1 receptor inhibitor (BMS-536924) and rationale for combining with EGFR/HER2 inhibitors.

Huang F, Greer A, Hurlburt W, Han X, Hafezi R, Wittenberg GM, Reeves K, Chen J, Robinson D, Li A, Lee FY, Gottardis MM, Clark E, Helman L, Attar RM, Dongre A, Carboni JM.

Cancer Res. 2009 Jan 1;69(1):161-70. doi: 10.1158/0008-5472.CAN-08-0835.

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