生物活性：Afatinib-d4 is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
体外研究(In Vitro)：Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
瑞禧生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Afatinib-d4 相关抗体:
c-Fos Antibody
Caveolin-1 Antibody
Phospho-EGFR (Tyr1068) Antibody
Phospho-EGFR (Tyr1173) Antibody
c-Fos Antibody (YA506)
EGF Antibody
EGFR Antibody
EGR1 Antibody
Phospholipase C gamma 1 Antibody
Phospho-EGFR (Tyr1068) Antibody (YA204)
HER2 Antibody
EGFR Antibody (YA775)
HER2 Antibody (YA771)
ErbB 4 Antibody
Phospho-EGFR (Tyr1092) Antibody
TGF alpha Antibody
HBEGF Antibody (YA1801)
ErbB 3 Antibody
GRB7 Antibody (YA1165)
分子量：489.96
Formula：C24H21D4ClFN5O3
非标记 CAS：850140-72-6
中文名称：阿法替尼 d4
运输条件：Room temperature in continental US; may vary elsewhere.
储存方式：Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
Data Sheet (527 KB)
产品使用指南 (1538 KB)
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
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[2]. Li D, et al. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene. 2008 Aug 7;27(34):4702-11.
 [Content Brief]
[3]. Wong CH, et al. Preclinical evaluation of afatinib (BIBW2992) in esophageal squamous cell carcinoma (ESCC). Am J Cancer Res. 2015 Nov 15;5(12):3588-99.
 [Content Brief]
[4]. Wang XK, et al. Afatinib circumvents multidrug resistance via dually inhibiting ATP binding cassette subfamily G member 2 in vitro and in vivo. Oncotarget. 2014 Dec 15;5(23):11971-85.
 [Content Brief]
[5]. Yoshioka T, et al. Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancer. Cancer Sci. 2018 Apr;109(4):1166-1176.
 [Content Brief]