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MedKoo product information:

 

  Dacomitinib 

  

Dacomitinib is an orally bioavailable, highly selective, second-generation small-molecule inhibitor of the pan-epidermal growth factor receptor (EGFR) family of tyrosine kinases (ErbB family) with potential antineoplastic activity. Dacomitinib specifically and irreversibly binds to and inhibits human EGFR subtypes, resulting in inhibition of proliferation and induction of apoptosis in EGFR-expressing tumor cells. EGFRs play major roles in tumor cell proliferation and tumor vascularization, and are often overexpressed or mutated in various tumor cell types. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

  

Current developer:    Pfizer

  

MedKoo Code#:  205576

Name:  Dacomitinib 

CAS#:  1110813-31-4

 

Synonym:   dacomitinib; PF-00299804. PF-299

 

IUPAC/Chemical name: 

(E)-N-(4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)-4-(piperidin-1-yl)but-2-enamide

 

Chemical structure

Theoretical analysis

 

 

 

MedKoo Code#:  205576
Name:  dacomitinib 
CAS#:  1110813-31-4

Chemical Formula: C24H25ClFN5O2

Exact Mass: 469.16808

Molecular Weight: 469.93900

Elemental Analysis: C, 61.34; H, 5.36; Cl, 7.54; F, 4.04; N, 14.90; O, 6.81

 

 

Availability and price:

This agent is not in stock,  may be  available through  custom synthesis.

 

To inquire quotation and lead time or to ask questions, please send email to sales@medkoo.com to describe your needs. A representative will respond your email shortly. We offer big discount for orders of bulk quantities.

 

 

Information about this agent

 

  

  

References

 1: Giaccone G, Wang Y. Strategies for overcoming resistance to EGFR family tyrosine kinase inhibitors. Cancer Treat Rev. 2011 Oct;37(6):456-64. doi: 10.1016/j.ctrv.2011.01.003. Epub 2011 Mar 1. Review. PubMed PMID: 21367530; PubMed Central PMCID: PMC3139833.

2: Harada T, Lopez-Chavez A, Xi L, Raffeld M, Wang Y, Giaccone G. Characterization of epidermal growth factor receptor mutations in non-small-cell lung cancer patients of African-American ancestry. Oncogene. 2011 Apr 14;30(15):1744-52. Epub 2010 Dec 6. PubMed PMID: 21132006.

3: Kelly RJ, Carter C, Giaccone G. Personalizing therapy in an epidermal growth factor receptor-tyrosine kinase inhibitor-resistant non-small-cell lung cancer using PF-00299804 and trastuzumab. J Clin Oncol. 2010 Oct 1;28(28):e507-10. Epub 2010 Aug 2. PubMed PMID: 20679607.

4: Belani CP. The role of irreversible EGFR inhibitors in the treatment of non-small cell lung cancer: overcoming resistance to reversible EGFR inhibitors. Cancer Invest. 2010 May;28(4):413-23. Review. PubMed PMID: 20307200.

5: Turke AB, Zejnullahu K, Wu YL, Song Y, Dias-Santagata D, Lifshits E, Toschi L, Rogers A, Mok T, Sequist L, Lindeman NI, Murphy C, Akhavanfard S, Yeap BY, Xiao Y, Capelletti M, Iafrate AJ, Lee C, Christensen JG, Engelman JA, Jänne PA. Preexistence and clonal selection of MET amplification in EGFR mutant NSCLC. Cancer Cell. 2010 Jan 19;17(1):77-88. PubMed PMID: 20129249; PubMed Central PMCID: PMC2980857.

6: Ercan D, Zejnullahu K, Yonesaka K, Xiao Y, Capelletti M, Rogers A, Lifshits E, Brown A, Lee C, Christensen JG, Kwiatkowski DJ, Engelman JA, Jänne PA. Amplification of EGFR T790M causes resistance to an irreversible EGFR inhibitor. Oncogene. 2010 Apr 22;29(16):2346-56. Epub 2010 Feb 1. PubMed PMID: 20118985; PubMed Central PMCID: PMC2859699.

7: Nguyen KS, Kobayashi S, Costa DB. Acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancers dependent on the epidermal growth factor receptor pathway. Clin Lung Cancer. 2009 Jul;10(4):281-9. Review. PubMed PMID: 19632948; PubMed Central PMCID: PMC2758558.

8: Tomillero A, Moral MA. Gateways to clinical trials. July-August 2008. Methods Find Exp Clin Pharmacol. 2008 Jul-Aug;30(6):459-95. PubMed PMID: 18850047.

9: Tomillero A, Moral MA. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2008 Jun;30(5):383-408. PubMed PMID: 18806898.

10: 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. Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor. Mol Cancer Ther. 2008 Jul;7(7):1880-9. Epub 2008 Jul 7. PubMed PMID: 18606718.

11: 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. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib. Cancer Res. 2007 Dec 15;67(24):11924-32. PubMed PMID: 18089823.


 

 

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