2006
DOI: 10.1158/1078-0432.ccr-06-0642
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Preclinical Antitumor Activity of BMS-599626, a pan-HER Kinase Inhibitor That Inhibits HER1/HER2 Homodimer and Heterodimer Signaling

Abstract: Purpose: The studies described here are intended to characterize the ability of BMS-599626, a small-molecule inhibitor of the human epidermal growth factor receptor (HER) kinase family, to modulate signaling and growth of tumor cells that depend on HER1and/or HER2. Experimental Design: The potency and selectivity of BMS-599626 were assessed in biochemical assays using recombinant protein kinases, as well as in cell proliferation assays using tumor cell lines with varying degrees of dependence on HER1 or HER2 s… Show more

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Cited by 73 publications
(48 citation statements)
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“…Until now, there have been studies on the activity of pan-HER TKIs, such as BMS-599626 and HM781-36B (22,23), in gastric cancer, and a phase II study of PF00299804 as monotherapy in patients with HER2-positive advanced gastric cancer is currently ongoing (24). In the present study, we evaluated the activity of PF00299804 in a large panel of gastric cancer cell lines and sought to determine the mechanisms of selectivity of PF00299804 for gastric cancer cell lines through investigating alteration of HER family heterodimer formation during treatment.…”
Section: Introductionmentioning
confidence: 99%
“…Until now, there have been studies on the activity of pan-HER TKIs, such as BMS-599626 and HM781-36B (22,23), in gastric cancer, and a phase II study of PF00299804 as monotherapy in patients with HER2-positive advanced gastric cancer is currently ongoing (24). In the present study, we evaluated the activity of PF00299804 in a large panel of gastric cancer cell lines and sought to determine the mechanisms of selectivity of PF00299804 for gastric cancer cell lines through investigating alteration of HER family heterodimer formation during treatment.…”
Section: Introductionmentioning
confidence: 99%
“…Lapatinib and erlotinib were obtained from LC Laboratories. Recombinant enzymes and biochemical assays of protein kinase activity were as described previously (31). KinomeScan profiling of BMS-690514 was done by Ambit Biosciences (32).…”
Section: Methodsmentioning
confidence: 99%
“…LX1 cells, which do not express EGFR or HER2, were transfected with EGFR L858R mutant plasmid by Fugene 6 (Roche Applied Science). At 48 hours after transfection, cells were treated for 1 hour with BMS-690514, and cell lysates were prepared as described previously (31). Immunoprecipitation was conducted by an anti-EGFR antibody and the immunoprecipitates were analyzed in Western blots by using antiphosphotyrosine and anti-EGFR antibodies.…”
Section: Transfection and Protein Expression Analysesmentioning
confidence: 99%
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“…These include BMS-599626 [Wong et al 2006], HM781-36B [Nam et al 2011] and PF00299804 [Nam et al 2012]. A phase II study of PF00299804 monotherapy in patients with HER2-positive AGC is currently ongoing [ClinicalTrials.gov identifier: NCT01152853].…”
Section: Pan-her Inhibitionmentioning
confidence: 99%