Description Biological activity Uses Clinical Study
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Dacomitinib (PF299804)

Description Biological activity Uses Clinical Study
Dacomitinib (PF299804) Structure
Dacomitinib (PF299804)
  • CAS No.1110813-31-4
  • Chemical Name:Dacomitinib (PF299804)
  • CBNumber:CB22566418
  • Molecular Formula:C24H25ClFN5O2
  • Formula Weight:469.94
  • MOL File:1110813-31-4.mol
Dacomitinib (PF299804) Property
Safety
  • HS Code  :29335990
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal word
  • Hazard statements
  • Precautionary statements
Dacomitinib (PF299804) Price More Price(6)
  • Brand: TCI Chemical
  • Product number: D5450
  • Product name : Dacomitinib
  • Purity: >98.0%(HPLC)
  • Packaging: 50mg
  • Price: $160
  • Updated: 2021/03/22
  • Buy: Buy
  • Brand: TCI Chemical
  • Product number: D5450
  • Product name : Dacomitinib
  • Purity: >98.0%(HPLC)
  • Packaging: 250mg
  • Price: $479
  • Updated: 2021/03/22
  • Buy: Buy
  • Brand: Cayman Chemical
  • Product number: 9001879
  • Product name : PF-299804
  • Purity: ≥98%
  • Packaging: 1mg
  • Price: $35
  • Updated: 2021/03/22
  • Buy: Buy
  • Brand: Cayman Chemical
  • Product number: 9001879
  • Product name : PF-299804
  • Purity: ≥98%
  • Packaging: 5mg
  • Price: $158
  • Updated: 2021/03/22
  • Buy: Buy
  • Brand: Cayman Chemical
  • Product number: 9001879
  • Product name : PF-299804
  • Purity: ≥98%
  • Packaging: 10mg
  • Price: $280
  • Updated: 2021/03/22
  • Buy: Buy

Dacomitinib (PF299804) Chemical Properties,Usage,Production

  • Description Dacomitinib is a selective and irreversible inhibitor of EGFR. It is a drug candidate for the treatment of non-small cell lung carcinoma. It is current under the Phase III clinical trials. It also shows potential for the treatment of HER-2 amplified breast cancer cells lines that are resistant to trastuzumab and lapatinib. 
  • Biological activity Dacomitibib (Dacomitinib, PF299804) is an effective and irreversible pan-ErbB inhibitor that is most effective in EGFR, with an IC50 of 6 nM. It is also highly effective in NSCLCs that carries EGFR or ERBB2 mutants (against Gefitinib) and EGFR T790M mutant. Phase 2.
    Dacomitinib is taken orally once-daily. It is an irreversible inhibitor of HER-1 (EGFR), HER-2 and HER-4 tyrosine kinases. Dacomitinib targets multiple receptors of the HER pathway, whereas currently marketed HER-1 (EGFR) inhibitors for non-small cell lung cancer (NSCLC) target only one receptor in this pathway,developed by Pfizer.
  • Uses

    Dacomitinib (PF299804), which name is (E)-N-[4-(3-chloro-4-fluoroanilino)-7- methoxyquinazolin-6-yl]-4-piperidin-1-ylbut-2-enamide, is a potent, orally available, highly selective, irreversible small-molecule tyrosine kinase inhibitor (TKI) of tyrosine kinase human epidermal growth factor receptors (HER) 1 (EGFR), HER2, and HER4. It is most effective against EGFR with IC50 of 6 nM. It is highly effective against NSCLCs carrying EGFR or ERBB2 mutant (anti-Gefitinib) and EGFR T790M mutant.

  • Clinical Study Dacomitinib has advanced to several Phase III clinical trials. The results of the first trials were disappointing, with a failure to meet the study goals, Additional Phase III trials are ongoing.
    Clinical evaluation of dacomitinib is ongoing in a number of clinical trials in patients with advanced NSCLC across lines of therapies and a range of histologies and molecular subtypes, such as EGFR and KRAS status.
    Additionally, there is an ongoing clinical trial evaluating dacomitinib in recurrent and/or metastatic (RM) squamous cell carcinoma of the head and neck (SCCHN).
  • Uses PF299804 is a potent, irreversible pan-ErbB inhibitor against ErbB1, ErbB2 and ErbB4 with IC50 of 6 nM, 45.7 nM and 73.7 nM, respectively.
  • Definition ChEBI: A member of the class of quinazolines that is 7-methoxyquinazoline-4,6-diamine in which the amino group at position 4 is substituted by a 3-chloro-4-fluorophenyl group and the amino group at position 6 is substituted by an (E)-4-(piperidin 1-yl)but-2-enoyl group.
Dacomitinib (PF299804) Preparation Products And Raw materials
Raw materials
Preparation Products
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  • (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-2-butenamide Dacomitinib (PF299804, PF299)
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  • Dacomitinib, >=98%
  • 2-Butenamide,N-[4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-, (2E)-
  • PF299
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  • PF299804;(E)-N-(4-((3-CHLORO-4-FLUOROPHENYL)AMINO)-7-METHOXYQUINAZOLIN-6-YL)-4-(PIPERIDIN-1-YL)BUT-2-ENAMIDE
  • (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-2-butenamide
  • Dacomitinib, 98%, a potent irreversible ErbB inbibitor
  • (E)-N-(4-((3-chloro-4-fluorophenyl)aMino)-7-Methoxyquinazolin-6-yl)-4-(piperidin-1-yl)but-2-enaMide
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  • Dacomitinib (PF299804) USP/EP/BP
  • Dacomitinib dihydrochloride salt
  • 1110813-31-4
  • C24H25ClFN5O2
  • Inhibitors
  • Anti-cancer&immunity
  • API
  • API
  • 1
  • APIs