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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: nelson jm. Cancer Res. 2007 Dec 15;67(24):11924-32. doi: 10.1158/0008-5472.CAN-07-1885. Cancer Res. 2007. PMID: 18089823
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.
Klutchko SR, Zhou H, Winters RT, Tran TP, Bridges AJ, Althaus IW, Amato DM, Elliott WL, Ellis PA, Meade MA, Roberts BJ, Fry DW, Gonzales AJ, Harvey PJ, Nelson JM, Sherwood V, Han HK, Pace G, Smaill JB, Denny WA, Showalter HD. Klutchko SR, et al. Among authors: nelson jm. J Med Chem. 2006 Feb 23;49(4):1475-85. doi: 10.1021/jm050936o. J Med Chem. 2006. PMID: 16480284
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: nelson jm. 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. 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: nelson jm. J Med Chem. 1999 May 20;42(10):1803-15. doi: 10.1021/jm9806603. J Med Chem. 1999. PMID: 10346932
Specific, irreversible inactivation of the epidermal growth factor receptor and erbB2, by a new class of tyrosine kinase inhibitor.
Fry DW, Bridges AJ, Denny WA, Doherty A, Greis KD, Hicks JL, Hook KE, Keller PR, Leopold WR, Loo JA, McNamara DJ, Nelson JM, Sherwood V, Smaill JB, Trumpp-Kallmeyer S, Dobrusin EM. Fry DW, et al. Among authors: nelson jm. Proc Natl Acad Sci U S A. 1998 Sep 29;95(20):12022-7. doi: 10.1073/pnas.95.20.12022. Proc Natl Acad Sci U S A. 1998. PMID: 9751783 Free PMC article.
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