| 货号 | 9001879-50mg |
| 描述 | The epidermal growth factor receptors (EGFR), whose members include ErbB1 (HER1), ErbB2 (HER2), ErbB3 (HER3), and ErbB4 (HER4), are receptor tyrosine kinases that are often over-expressed in cancer.1,2 PF-299804 is a second generation pan-ErbB receptor tyrosine kinase inhibitor (IC50s = 6, 45.7, and 73.7 nM for ErbB1, ErbB2, and ErbB4, respectively) that irreversibly binds to the ATP site in the catalytic domains of ErbB receptors.3,4 At 15 mg/kg, it demonstrates antitumor activity ranging from delay in tumor growth to complete regression in various tumor xenograft models expressing either wild-type ErbB or mutant ErbB family members that show resistance to first generation ErbB kinase inhibitors.3,4 |
| 别名 | Dacomitinib;PF299; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Gerber, D.E. EGFR inhibition in the treatment of non-small cell lung cancer. Drug Dev. Res. 69(6), 359-372 (2008). 2.Ciardiello, F., and Tortora, G. A novel approach in the treatment of cancer: Targeting the epidermal growth factor receptor. Clin. Cancer Res. 7(10), 2958-2970 (2001). 3.Engelman, J.A.,Zejnullahu, K.,Gale, C.M., et al. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to gefitinib. Cancer Research 67(24), 11924-11932 (2007). 4.Gonzales, A.J.,Hook, K.E.,Althaus, I.W., et al. Antitumor activity and pharmacokinetic properties of PF-00299804, a second-generation irreversible pan-erbB receptor tyrosine kinase inhibitor. Molecular Cancer Therapeutics 7(7), 1880-1889 (2008). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 469.9 |
| 分子式 | C24H25ClFN5O2 |
| CAS号 | 1110813-31-4 |
| 稳定性 | ≥ 2 years |
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