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1110813-31-4,MFCD19443734
Catalog No.:AA008TCL

1110813-31-4 | Dacomitinib

Pack Size
Purity
Availability
Price(USD)
Quantity
  
1mg
98%
in stock  
$6.00   $4.00
- +
25mg
98%
in stock  
$43.00   $30.00
- +
250mg
98%
in stock  
$73.00   $51.00
- +
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA008TCL
Chemical Name:
Dacomitinib
CAS Number:
1110813-31-4
Molecular Formula:
C24H25ClFN5O2
Molecular Weight:
469.9390
MDL Number:
MFCD19443734
SMILES:
COc1cc2ncnc(c2cc1NC(=O)/C=C/CN1CCCCC1)Nc1ccc(c(c1)Cl)F
Properties
Computed Properties
 
Complexity:
665  
Covalently-Bonded Unit Count:
1  
Defined Bond Stereocenter Count:
1  
Heavy Atom Count:
33  
Hydrogen Bond Acceptor Count:
7  
Hydrogen Bond Donor Count:
2  
Rotatable Bond Count:
7  
XLogP3:
4.4  

Downstream Synthesis Route
CASUnavailable 
  1110813-31-4 

[1]CurrentPatentAssignee:PFIZERINC-US2005/250761,2005,A1Locationinpatent:Page/Pagecolumn16-18

CASUnavailable 
  1110813-31-4 

[1]CurrentPatentAssignee:PFIZERINC-US2005/250761,2005,A1Locationinpatent:Page/Pagecolumn18-20

1110813-31-4    32315-10-9   
CASUnavailable 
 
CASUnavailable 

[1]CurrentPatentAssignee:SOUTHEASTUNIVERSITY-CN110025789,2019,ALocationinpatent:Paragraph0120-0123

[1]CurrentPatentAssignee:LUOXINPHARMACEUTICALSGROUPSTOCKCOLTD-CN111978212,2020,A

Literature

Title: Dacomitinib versus gefitinib as first-line treatment for patients with EGFR-mutation-positive non-small-cell lung cancer (ARCHER 1050): a randomised, open-label, phase 3 trial.

Journal: The Lancet. Oncology 20171101

Title: Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.

Journal: Journal of medicinal chemistry 20160908

Title: Dacomitinib in lung cancer: a 'lost generation' EGFR tyrosine-kinase inhibitor from a bygone era?

Journal: Drug design, development and therapy 20150101

Title: The irreversible pan-HER inhibitor PF00299804 alone or combined with gemcitabine has an antitumor effect in biliary tract cancer cell lines.

Journal: Investigational new drugs 20121201

Title: Activation of IL-6R/JAK1/STAT3 signaling induces de novo resistance to irreversible EGFR inhibitors in non-small cell lung cancer with T790M resistance mutation.

Journal: Molecular cancer therapeutics 20121001

Title: Randomized phase II study of dacomitinib (PF-00299804), an irreversible pan-human epidermal growth factor receptor inhibitor, versus erlotinib in patients with advanced non-small-cell lung cancer.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20120920

Title: Second-generation irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs): a better mousetrap? A review of the clinical evidence.

Journal: Critical reviews in oncology/hematology 20120901

Title: Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to trastuzumab and lapatinib.

Journal: Molecular cancer therapeutics 20120901

Title: Irreversible protein kinase inhibitors: balancing the benefits and risks.

Journal: Journal of medicinal chemistry 20120726

Title: The effect of dacomitinib (PF-00299804) on CYP2D6 activity in healthy volunteers who are extensive or intermediate metabolizers.

Journal: Cancer chemotherapy and pharmacology 20120401

Title: Personalizing therapy in an epidermal growth factor receptor-tyrosine kinase inhibitor-resistant non-small-cell lung cancer using PF-00299804 and trastuzumab.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20101001

Title: The role of irreversible EGFR inhibitors in the treatment of non-small cell lung cancer: overcoming resistance to reversible EGFR inhibitors.

Journal: Cancer investigation 20100501

Title: Amplification of EGFR T790M causes resistance to an irreversible EGFR inhibitor.

Journal: Oncogene 20100422

Title: Acquired resistance to epidermal growth factor receptor tyrosine kinase inhibitors in non-small-cell lung cancers dependent on the epidermal growth factor receptor pathway.

Journal: Clinical lung cancer 20090701

Title: Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor.

Journal: Molecular cancer therapeutics 20080701

Title: PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib.

Journal: Cancer research 20071215

Title: Engelman JA, et al. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to ZD1839. Cancer Res. 2007 Dec 15;67(24):11924-32.

Title: Kalous O, et al. Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to Anti-Human HER2 and GW572016. Mol Cancer Ther. 2012 Sep;11(9):1978-87.

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SDS
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