企业QQ
官方微信
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:
| Chemical Formula: | C22H24ClFN4O3 | |
| CAS #: | 184475-35-2 | |
| Molecular Weight: | 446.9 | |
| Purity: | >99% | |
| Appearance: | White | |
| Chemical Name: | N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | Iressa, 184475-35-2, Irressat, ZD 1839, ZD-1839, ZD1839, Gefitinib |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Wakeling et al., ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res. 2002, 62, 5749-5754. Pubmed ID: 12384534 |
| 2. | Anderson et al., ZD1839 (Iressa), a novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, potently inhibits the growth of EGFR-positive cancer cell lines with or without erbB2 overexpression. Int. J. Cancer. 2001, 94, 774-782. Pubmed ID: 11745477 |
| 3. | Moasser et al., The tyrosine kinase inhibitor ZD1839 ("Iressa") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells. Cancer Res. 2001, 61, 7184-7188. Pubmed ID: 11585753 |
| 4. | Sirotnak et al., Efficacy of cytotoxic agents against human tumor xenografts is markedly enhanced by coadministration of ZD1839 (Iressa), an inhibitor of EGFR tyrosine kinase. Clin. Cancer Res. 2000, 6, 4885-4892. Pubmed ID: 11745477 |