Product Name

Gefitinib

General description

Gefitinib is a selective tyrosine kinase receptor inhibitor used in the therapy of non-small cell lung cancer.

Synonym

N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine; AKOS 91371;Iressa; ZD1839; Irressat; ZD-1839

Purity

≥99%(HPLC)

CAS   Number

184475-35-2

Formula

C²²H²⁴ClFN⁴O³

Molecular   Weight

446.907

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

White to Off-white solid

Solubility(25℃)

DMSO

≥50mg/mL

Ethanol

~4mg/mL

Water

Insoluble

l  Biological Information

Biochem/Physiol   Actions

Gefitinib inhibits the intracellular phosphorylation of numerous tyrosine kinases associated with transmembrane cell surface receptors, including the tyrosine kinases associated with the epidermal growth factor receptor (EGFR-TK). EGFR is expressed on the cell surface of many normal cells and cancer cells.

Gefitinib is an anilinoquinazoline with antineoplastic activity. Gefitinib inhibits the catalytic activity of   numerous tyrosine kinases including the epidermal growth factor receptor (EGFR), which may result in inhibition of tyrosine kinase-dependent tumor growth. Specifically, this agent competes with the binding of ATP to the tyrosine kinase domain of EGFR, thereby inhibiting receptor autophosphorylation and resulting in inhibition of signal transduction. Gefitinib may also induce cell cycle arrest and inhibit angiogenesis.

Application

1. Antineoplastic Agents

2. Protein Kinase Inhibitors

l  Packaging & Storage

Packaging

250mg; 1g

Storage temp.

0-5℃

l  Precautions and Disclaimer

This   product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov