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Dacomitinib is a selective and irreversible inhibitor of EGFR. Compared to first generation EGFR inhibitors, dacomitinib shows increased efficacy in models of non-small cell lung cancer (NSCLC) cells. It also suppresses proliferation of pancreatic ductal adenocarcinoma cells.
| Cas No. | 1110813-31-4 |
|---|---|
| Purity | ≥99% |
| Formula | C24H25ClFN5O2 |
| Formula Wt. | 469.95 |
| IUPAC Name | (2E)-N-{4-[(3-Chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl}-4-(1-piperidinyl)-2-butenamide |
| Synonym | PF00299804 Anhydrous |
| Melting Point | 184-187°C |
| Solubility | DMSO 75 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
| Store Temp | -20°C |
|---|---|
| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Gonzales A., Hook K., Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor. Mol Cancer Ther. 7(7):1880-9 (2008). PMID: 18606718.
Nagano T., Tachihara M., et al. Dacomitinib, a second-generation irreversible epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) to treat non-small cell lung cancer. Drugs Today (Barc). 55(4):231-236 (2019). PMID: 31050691.
Momeny M., Esmaeili F., et al. The ERBB receptor inhibitor dacomitinib suppresses proliferation and invasion of pancreatic ductal adenocarcinoma cells. Cell Oncol. 2019. PMID: 31025257.