Gefitinib (ZD1839, Iressa) is an orally-available, aminoquinazoline-based inhibitor of EGFR with an IC50 of 33 nM. Gefitinib exhibits >100-fold selectivity over erbB2 and the VEGF family of kinases, as well as the serine-threonine kinases raf, MEK1, and ERK2 (MAPK). It selectively inhibits EGF-stimulated EGFR phosphorylation and EGF-stimulated tumor cell growth (IC50, 54 nM). [1] Tumor growth inhibition of EGFR-postiive cancer cell lines is observed both in the presence or absence of erbB2 overexpression. [2]

Gefitinib has also been shown to be effective in HER2-overexpressing cell lines, associated with the dephosphorylation of EGFR, HER2, and HER3, accompanied by the loss of association of HER3 with PI3K, and subsequent downregulation of Akt activity. [3]

Gefitinib is synergistic with other cancer therapies such as taxanes, paclitaxel and docetaxel, inducing partial to complete regressions cell lines such as A431 and PC-3. [4]

Technical information:

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4^oC desiccated, or store DMSO solution at -20^oC.

Reference:

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.