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Cellagen Technology
EGFR inhibitor
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]
Cellagen Technology
EGFR inhibitor
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]
