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Page 1
MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.
Pan BS, Chan GK, Chenard M, Chi A, Davis LJ, Deshmukh SV, Gibbs JB, Gil S, Hang G, Hatch H, Jewell JP, Kariv I, Katz JD, Kunii K, Lu W, Lutterbach BA, Paweletz CP, Qu X, Reilly JF, Szewczak AA, Zeng Q, Kohl NE, Dinsmore CJ. Pan BS, et al. Cancer Res. 2010 Feb 15;70(4):1524-33. doi: 10.1158/0008-5472.CAN-09-2541. Epub 2010 Feb 9. Cancer Res. 2010. PMID: 20145145
Seven of 10 MK-2461-sensitive tumor cell lines identified from a large panel harbored genomic amplification of MET or FGFR2. ...Taken together, our findings support further preclinical development of MK-2461 for cancer therapy....
Seven of 10 MK-2461-sensitive tumor cell lines identified from a large panel harbored genomic amplification of MET or FGFR2. . …
Design and synthesis of novel substituted naphthyridines as potential c-Met kinase inhibitors based on MK-2461.
Wu JF, Liu MM, Huang SX, Wang Y. Wu JF, et al. Bioorg Med Chem Lett. 2015 Aug 15;25(16):3251-5. doi: 10.1016/j.bmcl.2015.05.082. Epub 2015 May 31. Bioorg Med Chem Lett. 2015. PMID: 26077488
Two series of novel 1,5-naphthyridine and 1,6-naphthyridine derivatives were designed and synthesized based on the c-Met kinase inhibitor MK-2461 under the guidance of scaffold hopping strategy. All were tested on c-Met kinase and in vitro anti-tumor activities agai …
Two series of novel 1,5-naphthyridine and 1,6-naphthyridine derivatives were designed and synthesized based on the c-Met kinase inhibitor …
Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.
Katz JD, Jewell JP, Guerin DJ, Lim J, Dinsmore CJ, Deshmukh SV, Pan BS, Marshall CG, Lu W, Altman MD, Dahlberg WK, Davis L, Falcone D, Gabarda AE, Hang G, Hatch H, Holmes R, Kunii K, Lumb KJ, Lutterbach B, Mathvink R, Nazef N, Patel SB, Qu X, Reilly JF, Rickert KW, Rosenstein C, Soisson SM, Spencer KB, Szewczak AA, Walker D, Wang W, Young J, Zeng Q. Katz JD, et al. J Med Chem. 2011 Jun 23;54(12):4092-108. doi: 10.1021/jm200112k. Epub 2011 May 24. J Med Chem. 2011. PMID: 21608528
Screening efforts identified a unique class of 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one kinase inhibitors, exemplified by 1. Subsequent SAR studies led to the development of 81 (MK-2461), a potent inhibitor of c-Met that was efficacious in preclinical animal mode …
Screening efforts identified a unique class of 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one kinase inhibitors, exemplified by 1. Subsequent S …
Targeting the C-MET/HGF Signaling Pathway in Pancreatic Ductal Adenocarcinoma.
Ghanaatgar-Kasbi S, Khorrami S, Avan A, Aledavoud SA, Ferns GA. Ghanaatgar-Kasbi S, et al. Curr Pharm Des. 2018;24(39):4619-4625. doi: 10.2174/1381612825666190110145855. Curr Pharm Des. 2018. PMID: 30636579 Review.
In this review, we summarize the role of HGF/Met pathway in the pathogenesis of pancreatic cancer, with particular emphasize on HGF/Met inhibitors in the clinical setting, including Cabozantinib (XL184, BMS-907351), Crizotinib (PF-02341066), MK-2461, Merestinib (LY2 …
In this review, we summarize the role of HGF/Met pathway in the pathogenesis of pancreatic cancer, with particular emphasize on HGF/Met inhi …
Gateways to clinical trials.
Tomillero A, Moral MA. Tomillero A, et al. Methods Find Exp Clin Pharmacol. 2009 Jan-Feb;31(1):47-57. Methods Find Exp Clin Pharmacol. 2009. PMID: 19357798
(-)-Gossypol; Alemtuzumab, Amlodipine, Anakinra, Azacitidine; Bazedoxifene acetate, Belinostat, Bevacizumab, BI-201335, BI-2536, Biphasic insulin aspart, Bortezomib; Cetuximab, CNTO-328, Custirsen sodium; Dacetuzumab; Elacytarabine, Erlotinib hydrochloride, Everolimus, Exenatide; …
(-)-Gossypol; Alemtuzumab, Amlodipine, Anakinra, Azacitidine; Bazedoxifene acetate, Belinostat, Bevacizumab, BI-201335, BI-2536, Biphasic in …
VEGF-A regulates sFlt-1 production in trophoblasts through both Flt-1 and KDR receptors.
Xiao Z, Li S, Yu Y, Li M, Chen J, Wang F, Zhang J, Deng W, Yang Q, Fan X. Xiao Z, et al. Mol Cell Biochem. 2018 Dec;449(1-2):1-8. doi: 10.1007/s11010-018-3337-5. Epub 2018 Mar 1. Mol Cell Biochem. 2018. PMID: 29497919
Both the mRNA and protein levels of VEGF and sFlt-1 were dramatically up-regulated in the V-J and V-H cells compared to the JEG3 and HTR8 cells, and they were significantly decreased after treatment with an Flt-1 receptor inhibitor (MK-2461), a KDR receptor inhibito …
Both the mRNA and protein levels of VEGF and sFlt-1 were dramatically up-regulated in the V-J and V-H cells compared to the JEG3 and HTR8 ce …
Chemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors.
Klaeger S, Gohlke B, Perrin J, Gupta V, Heinzlmeir S, Helm D, Qiao H, Bergamini G, Handa H, Savitski MM, Bantscheff M, Médard G, Preissner R, Kuster B. Klaeger S, et al. ACS Chem Biol. 2016 May 20;11(5):1245-54. doi: 10.1021/acschembio.5b01063. Epub 2016 Feb 25. ACS Chem Biol. 2016. PMID: 26863403
Surprisingly, low or submicromolar FECH binding was detected for 29 of all compounds tested and isothermal dose response measurements confirmed target engagement in cells. We also show that Vemurafenib, Linsitinib, Neratinib, and MK-2461 reduce heme levels in K562 c …
Surprisingly, low or submicromolar FECH binding was detected for 29 of all compounds tested and isothermal dose response measurements confir …
Structural basis for selective small molecule kinase inhibition of activated c-Met.
Rickert KW, Patel SB, Allison TJ, Byrne NJ, Darke PL, Ford RE, Guerin DJ, Hall DL, Kornienko M, Lu J, Munshi SK, Reid JC, Shipman JM, Stanton EF, Wilson KJ, Young JR, Soisson SM, Lumb KJ. Rickert KW, et al. J Biol Chem. 2011 Apr 1;286(13):11218-25. doi: 10.1074/jbc.M110.204404. Epub 2011 Jan 18. J Biol Chem. 2011. PMID: 21247903 Free PMC article.
Here we describe the structural basis of c-Met activation upon autophosphorylation and the selective small molecule inhibiton of autophosphorylated c-Met. MK-2461 is a potent c-Met inhibitor that is selective for the phosphorylated state of the enzyme. Compound 1 is …
Here we describe the structural basis of c-Met activation upon autophosphorylation and the selective small molecule inhibiton of autophospho …
Genetic alterations of FGF receptors: an emerging field in clinical cancer diagnostics and therapeutics.
Katoh M. Katoh M. Expert Rev Anticancer Ther. 2010 Sep;10(9):1375-9. doi: 10.1586/era.10.128. Expert Rev Anticancer Ther. 2010. PMID: 20836672
Gene amplification of FGFRs results in ligand-independent FGFR signaling to RAS-ERK, PI3K-AKT and JAK-STAT cascades due to the overexpression of wild-type or C-terminally deleted FGFRs. Cediranib, TKI258, Ki23057, MK-2461 and brivanib are broad-range tyrosine kinase …
Gene amplification of FGFRs results in ligand-independent FGFR signaling to RAS-ERK, PI3K-AKT and JAK-STAT cascades due to the overexpressio …