1110813-31-4 | Dacomitinib

Packsize	Purity	Availability	Price	Discounted Price
1mg	98%	in stock	$6.00	$4.00
25mg	98%	in stock	$42.00	$30.00
250mg	98%	in stock	$68.00	$48.00

Description

• Catalog Number: AE11185
• 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

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

Literature

• 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.

  The Lancet. Oncology 20171101

• 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 of medicinal chemistry 20160908

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

  Drug design, development and therapy 20150101

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

  Investigational new drugs 20121201

• 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.

  Molecular cancer therapeutics 20121001

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

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

  Critical reviews in oncology/hematology 20120901

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

  Molecular cancer therapeutics 20120901

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

  Journal of medicinal chemistry 20120726

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

  Cancer chemotherapy and pharmacology 20120401

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

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

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

  Cancer investigation 20100501

• Amplification of EGFR T790M causes resistance to an irreversible EGFR inhibitor.

  Oncogene 20100422

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

  Clinical lung cancer 20090701

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

  Molecular cancer therapeutics 20080701

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

  Cancer research 20071215