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Dacomitinib (PF299804)
- Product Name:Dacomitinib (PF299804)
- CAS:1110813-31-4
- MF:C24H25ClFN5O2
- MW:469.9390032
- EINECS:-0
- Mol File:1110813-31-4.mol
-
Dacomitinib (PF299804) Chemical Properties
- Boiling point:665.7±55.0 °C(Predicted)
- Density 1.344
- form White solid.
- pka12.05±0.43(Predicted)
- CAS DataBase Reference1110813-31-4
- HS Code 29335990
Dacomitinib (PF299804) Usage And Synthesis
- DescriptionDacomitinib 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 activityDacomitibib (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 StudyDacomitinib 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). - UsesPF299804 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.
- DefinitionChEBI: 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)SupplierMore
- Company Name:ExcelChemical (Shanghai) Chemical Technology Co., Ltd. Gold
- Tel:+86 13671938079
- Email:sales@wanyuchem.com
- Products Intro:Product Name:PF-00299804
CAS:1110813-31-4
Purity:>99% Package:10g,100g
- Company Name:Wuhu Sumu Pharmaceutical Technology Co., Ltd. Gold
- Tel:18895393626
- Email:3145613242@qq.com
- Products Intro:Product Name:Dacomitinib,PF299804
CAS:1110813-31-4
Purity:99.50% Package:2kg
- Company Name:WuHu Linze pharmaceutical Co.,Ltd. Gold
- Tel:18356571950
- Email:2030235803@qq.com
- Products Intro:Product Name:Dacomitinib (PF299804)
CAS:1110813-31-4
Purity:99% HPLC Package:5KG;1KG;500G;100G;50G;10G;5G
- Company Name:Wuhan Xinbaichuan Pharmaceutical Technology Co., Ltd. Gold
- Tel:027-50478167
- Email:252994272@qq.com
- Products Intro:Product Name:Dacomitinib (PF299804)
CAS:1110813-31-4
Purity:99% HPLC
- Company Name:Jurong Coupling Biotechnology Co., Ltd. Gold
- Tel:13656108824
- Email:278191416@qq.com
- Products Intro:Product Name:Dacomitinib (PF299804)
CAS:1110813-31-4
Package:50 g/
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