生物活性：Gefitinib-d3 (ZD1839-d3) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].
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].
德尔塔生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Gefitinib-d3 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：449.92
Formula：C22H21D3ClFN4O3
CAS 号：1173976-40-3
非标记 CAS：184475-35-2
中文名称：吉非替尼 d3
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 (533 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]. Wakeling AE, et al. ZD1839: an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res. 2002 Oct 15;62(20):5749-54.
 [Content Brief]
[3]. Pedersen MW, et al. Differential response to gefitinib of cells expressing normal EGFR and the mutant EGFRvIII. Br J Cancer. 2005 Oct 17;93(8):915-23.
 [Content Brief]
[4]. Moasser MM, et al. The tyrosine kinase inhibitor ZD1839 inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells. Cancer Res. 2001 Oct 1;61(19):7184-8.
 [Content Brief]
[5]. Morgillo F, et al. Synergistic effects of 1,1-Dimethylbiguanide treatment in combination with gefitinib, a selective EGFR tyrosine kinase inhibitor, in LKB1 wild-type NSCLC cell lines. Clin Cancer Res. 2013 Jul 1;19(13):3508-19.
 [Content Brief]
[6]. Miyake K, et al. Epidermal growth factor receptor-tyrosine kinase inhibitor (gefitinib) augments pneumonitis, but attenuates lung fibrosis in response to radiation injury in rats. J Med Invest. 2012;59(1-2):174-85.
 [Content Brief]
[7]. Noh CK, et al. Simultaneous quantification of volitinib and gefitinib in rat plasma by HPLC-MS/MS for application to a pharmacokinetic study in rats. J Sep Sci. 2017 Jul 27.
 [Content Brief]
[8]. Dhar D, et al. Liver Cancer Initiation Requires p53 Inhibition by CD44-Enhanced Growth Factor Signaling. Cancer Cell. 2018 Jun 11;33(6):1061-1077.e6.
 [Content Brief]