Afatinib dimaleate
Cat. No.：YN340036
| 产品名称: | Afatinib dimaleate |
| CAS No.: | 850140-73-7 |
| Chemical Name: | N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2E-butenamide, 2Z-butenedioate (1:2) |
| Synonyms: | 双马来酸盐阿法替尼; BIBW 2992MA2 |
| 分子量: | 718.08 |
| 分子式: | C₃₂H₃₃ClFN₅O₁₁ |
| SMILES: | O=C(NC1=C(C=C2C(C(NC3=CC(Cl)=C(C=C3)F)=NC=N2)=C1)O[C@H]4CCOC4)/C=C/CN(C)C.O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O |
| 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: | Afatinib dimaleate (BIBW 2992MA2) 是不可逆的EGFR家族抑制剂，抑制EGFRwt，EGFRL858R，EGFRL858R/T790M和 HER2的IC50分别为0.5 nM，0.4 nM，10 nM 和 14 nM。 |
| IC50和靶点: | [{name:"EGFRL858R:0.4 nM (IC50)"},{name: "EGFR:0.5 nM (IC50)"},{name: "EGFRL858R/T790M:10 nM (IC50)"},{name: "HER2:14 nM (IC50)'}, 'HER3'] |
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| Solvent & Solubility: |
Eskens, F.A.L.M., Mom, C.H., Planting, A.S.T., et al.A phase I dose escalation study of BIBW 2992, an irreversible dual inhibitor of epidermal growth factor receptor 1 (EGFR) and 2 (HER2) tyrosine kinase in a 2-week on, 2-week off schedule in patients with advanced solid tumoursBr. J. Cancer98(1),80-85(2008)
Zhang, Y., Wang, C.-Y., Duan, Y.-J., et al.Afatinib decreases P-glycoprotein expression to promote adriamycin toxicity of A549T cellsJ. Cell. Biochem.119(1),414-423(2018)
Yoshioka, T., Shien, K., Namba, K., et al.Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancerCancer Sci.109(4),1166-1176(2018)
