Dacomitinib
Cat. No.：YN340128
CAS No. ：1110813-31-4
| 产品名称: | Dacomitinib |
| CAS No.: | 1110813-31-4 |
| Chemical Name: | N-[4-[(3-chloro-4-fluorophenyl)amino]-7-methoxy-6-quinazolinyl]-4-(1-piperidinyl)-(2E)-butenamide |
| Synonyms: | 达克替尼; PF-00299804; PF-299804 |
| 分子量: | 469.94 |
| 分子式: | C₂₄H₂₅ClFN₅O₂ |
| SMILES: | O=C(/C=C/CN1CCCCC1)NC2=CC3=C(C=C2OC)N=CN=C3NC4=CC=C(C(Cl)=C4)F |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Dacomitinib (PF-00299804) 是一种特异，不可逆的ERBB家族抑制剂，作用于EGFR，ERBB2和ERBB4的IC50分别为 6 nM，45.7 nM 和 73.7 nM。 |
| IC50和靶点: | [{name:"EGFR:6 nM (IC50)"},{name: "ErbB2:45.7 nM (IC50)"},{name: "ErbB4:73.7 nM (IC50)"}] |
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| Solvent & Solubility: |
Gerber, D.E.EGFR inhibition in the treatment of non-small cell lung cancerDrug Dev. Res.69(6),359-372(2008)
Ciardiello, F., and Tortora, G.A novel approach in the treatment of cancer: Targeting the epidermal growth factor receptorClin. Cancer Res.7(10),2958-2970(2001)
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 gefitinibCancer Res.67(24),11924-11932(2007)
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 inhibitorMol. Cancer Ther.7(7),1880-1889(2008)
