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PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib.
Engelman JA, Zejnullahu K, Gale CM, Lifshits E, Gonzales AJ, Shimamura T, Zhao F, Vincent PW, Naumov GN, Bradner JE, Althaus IW, Gandhi L, Shapiro GI, Nelson JM, Heymach JV, Meyerson M, Wong KK, Jänne PA. Engelman JA, et al. Among authors: vincent pw. Cancer Res. 2007 Dec 15;67(24):11924-32. doi: 10.1158/0008-5472.CAN-07-1885. Cancer Res. 2007. PMID: 18089823
Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor.
Gonzales AJ, Hook KE, Althaus IW, Ellis PA, Trachet E, Delaney AM, Harvey PJ, Ellis TA, Amato DM, Nelson JM, Fry DW, Zhu T, Loi CM, Fakhoury SA, Schlosser KM, Sexton KE, Winters RT, Reed JE, Bridges AJ, Lettiere DJ, Baker DA, Yang J, Lee HT, Tecle H, Vincent PW. Gonzales AJ, et al. Among authors: vincent pw. Mol Cancer Ther. 2008 Jul;7(7):1880-9. doi: 10.1158/1535-7163.MCT-07-2232. Epub 2008 Jul 7. Mol Cancer Ther. 2008. PMID: 18606718
Tyrosine kinase inhibitors. 14. Structure-activity relationships for methylamino-substituted derivatives of 4-[(3-bromophenyl)amino]-6-(methylamino)-pyrido[3,4-d]pyrimidine (PD 158780), a potent and specific inhibitor of the tyrosine kinase activity of receptors for the EGF family of growth factors.
Rewcastle GW, Murray DK, Elliott WL, Fry DW, Howard CT, Nelson JM, Roberts BJ, Vincent PW, Showalter HD, Winters RT, Denny WA. Rewcastle GW, et al. Among authors: vincent pw. J Med Chem. 1998 Feb 26;41(5):742-51. doi: 10.1021/jm970641d. J Med Chem. 1998. PMID: 9513602
Tyrosine kinase inhibitors. 15. 4-(Phenylamino)quinazoline and 4-(phenylamino)pyrido[d]pyrimidine acrylamides as irreversible inhibitors of the ATP binding site of the epidermal growth factor receptor.
Smaill JB, Palmer BD, Rewcastle GW, Denny WA, McNamara DJ, Dobrusin EM, Bridges AJ, Zhou H, Showalter HD, Winters RT, Leopold WR, Fry DW, Nelson JM, Slintak V, Elliot WL, Roberts BJ, Vincent PW, Patmore SJ. Smaill JB, et al. Among authors: vincent pw. J Med Chem. 1999 May 20;42(10):1803-15. doi: 10.1021/jm9806603. J Med Chem. 1999. PMID: 10346932
MET Tyrosine Kinase Inhibition Enhances the Antitumor Efficacy of an HGF Antibody.
Farrell PJ, Matuszkiewicz J, Balakrishna D, Pandya S, Hixon MS, Kamran R, Chu S, Lawson JD, Okada K, Hori A, Mizutani A, Iwata H, de Jong R, Hibner B, Vincent P. Farrell PJ, et al. Mol Cancer Ther. 2017 Jul;16(7):1269-1278. doi: 10.1158/1535-7163.MCT-16-0771. Epub 2017 Mar 24. Mol Cancer Ther. 2017. PMID: 28341789
BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis.
Wilhelm SM, Carter C, Tang L, Wilkie D, McNabola A, Rong H, Chen C, Zhang X, Vincent P, McHugh M, Cao Y, Shujath J, Gawlak S, Eveleigh D, Rowley B, Liu L, Adnane L, Lynch M, Auclair D, Taylor I, Gedrich R, Voznesensky A, Riedl B, Post LE, Bollag G, Trail PA. Wilhelm SM, et al. Cancer Res. 2004 Oct 1;64(19):7099-109. doi: 10.1158/0008-5472.CAN-04-1443. Cancer Res. 2004. PMID: 15466206
31 results