Gefitinib (Standard)

Gefitinib (Standard) is the analytical standard of Gefitinib. This product is intended for research and analytical applications. 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 and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer [1][2][5].

Product Specifications

CAS Number

[184475-35-2]

Product Name Alternative

ZD1839 (Standard)

UNSPSC

12352005

Hazard Statement

H302, H315, H318, H351, H360, H373, H410

Target

Apoptosis; Autophagy; EGFR; Reference Standards

Type

Reference Standards

Related Pathways

Apoptosis; Autophagy; JAK/STAT Signaling; Others; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gefitinib-standard.html

Purity

99.94

Smiles

ClC1=C(C=CC(NC2=NC=NC3=C2C=C(C(OC)=C3)OCCCN4CCOCC4)=C1)F

Molecular Formula

C22H24ClFN4O3

Molecular Weight

446.90

Precautions

H302, H315, H318, H351, H360, H373, H410

References & Citations

[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. |[3]Muhammad Tariq, et al. Gefitinib inhibits M2-like polarization of tumor-associated macrophages in Lewis lung cancer by targeting the STAT6 signaling pathway. Acta Pharmacol Sin. 2017 Nov;38 (11) :1501-1511. |[4]Mark S Cragg, et al. Gefitinib-induced killing of NSCLC cell lines expressing mutant EGFR requires BIM and can be enhanced by BH3 mimetics. PLoS Med. 2007 Oct;4 (10) :1681-89; discussion 1690. |[5]Marie P Piechocki, et al. Gefitinib prevents cancer progression in mice expressing the activated rat HER2/neu. Int J Cancer. 2008 Apr 15;122 (8) :1722-9. |[6]Tomoya Takenaka, et al. Effects of gefitinib treatment on cellular uptake of extracellular vesicles in EGFR-mutant non-small cell lung cancer cells. Int J Pharm. 2019 Dec 15;572:118762. |[7]Amin Li, et al. Gefitinib sensitization of cisplatin-resistant wild-type EGFR non-small cell lung cancer cells. J Cancer Res Clin Oncol. 2020 Jul;146 (7) :1737-1749.