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Gefitinib

Chemical Structure : Gefitinib

CAS No.: 184475-35-2

Gefitinib (ZD-1839)

Catalog No.: PC-45891Not For Human Use, Lab Use Only.

Gefitinib (ZD-1839) is a potent, selective, orally active EGFR inhibitor with IC50 of 23 nM.

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Biological Activity

Gefitinib (ZD-1839) is a potent, selective, orally active EGFR inhibitor with IC50 of 23 nM.
Gefitinib (ZD-1839) inhibits EGF-stimulated proliferation of KB cells with IC50 of 80 nM.
Gefitinib (ZD-1839) blocks the growth of GEO colon cancer, ZR-75-1 and MCF-10A Ha-ras breast cancer, and OVCAR-3 ovarian cancer cell lines with IC50 of 0.2-0.4 uM.
Gefitinib (ZD-1839) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth.
Gefitinib (ZD-1839) has been used to treat advanced (or recurrent) non-small cell lung cancer.

Physicochemical Properties

M.Wt 446.9024
Formula C22H24ClFN4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 30 mg/mL

Chemical Name/SMILES

4-Quinazolinamine, N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(4-morpholinyl)propoxy]-

References

1. Barker AJ, et al. Bioorg Med Chem Lett. 2001 Jul 23;11(14):1911-4.

2. Sirotnak FM, et al. Clin Cancer Res. 2000 Dec;6(12):4885-92.

3. Moasser MM, et al. Cancer Res. 2001 Oct 1;61(19):7184-8.

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