Gefitinib impurity 2

Gefitinibimpurity2是Gefitinib的杂质。Gefitinib是一种有效的，具有口服活性的选择性EGFR酪氨酸激酶抑制剂，IC50为33nM。Gefitinib选择性抑制EGF刺激的肿瘤细胞生长(IC50为54nM)，并阻断EGF刺激的肿瘤细胞中EGFR自磷酸化。Gefitinib还可诱导细胞自噬(autophagy)。Gefitinib具有抗肿瘤活性。

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Background

Gefitinib impurity 2 is the impurity of 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].

[1]. 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. [2]. 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.