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Afatinib-d6
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Afatinib-d6图片
CAS NO:1313874-96-2
包装与价格:
包装价格(元)
500 μg电议
1mg电议

产品介绍
Afatinib-d6 (BIBW 2992 D6) 是氘标记的 Afatinib。阿法替尼 (BIBW 2992) 是一种不可逆的 EGFR 家族抑制剂。
Cas No.1313874-96-2
别名BIBW 2992 D6
Canonical SMILESFC(C=C1)=C(Cl)C=C1NC2=NC=NC3=C2C=C(NC(/C=C/CN(C([2H])([2H])[2H])C([2H])([2H])[2H])=O)C(O[C@@H]4COCC4)=C3
分子式C24H19ClD6FN5O3
分子量492
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Afatinib-d6is intended for use as an internal standard for the quantification of afatinib by GC- or LC-MS. Afatinib is an irreversible inhibitor of epidermal growth factor receptor (EGFR) and ErbB2 (IC50s = 0.5 and 14 nM, respectively).1It increases the cytotoxicity of adriamycin in a concentration-dependent manner in multidrug-resistant A549T lung cancer cells overexpressing P-glycoprotein.2Afatinib (20 mg/kg) reduces tumor growth inErbB2-amplified NCI-N87 and NUGC4 gastric cancer mouse xenograft models.3Formulations containing afatinib have been used in the treatment of non-small cell lung cancer.

1.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) 2.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) 3.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)