|
Back to products
Browse products
Approved anticancer agents
Anticancer agents in trials
Anticancer agents
in preclinical trials
Anticancer molecular libraries
Other drug agents
Drug intermediates
Bio-reagents and biochemicals
|
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
|
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.
|
Contact MedKoo:
Email:
sales@medkoo.com
(Keyword; CAS#; MedKoo code#)
|