Gefitinib, Free Base (Iressa)

Supplier:

United States Biological

Cat no: G2023-95A

Gefitinib, Free Base (Iressa)

EGFR tyrosine kinase inhibitor that binds to the ATP-binding site of the enzyme. The functions of the EGFR tyrosine kinase in activating the Ras signal transduction cascade and malignant cell growth are thus inhibited. It has been shown that a mutation in the EGFR tyrosine kinase domain is responsible for activating anti-apoptotic pathways in gefitinib-sensitive non-small cell lung cancers. These mutations tend to increase sensitivity to tyrosine kinase inhibitors including gefitinib and erlotinib. The adenocarcinoma subset of non-small cell lung cancer histologies often have these mutations, which are commonly found in Asians, women, and non-smokers.\n\nSolubility:\nSoluble in DMSO, up to about 100mg/ml; very poorly soluble in water or ethanol.\n\nMelting Point:\n188-193 degrees C\n\nElemental Analysis:\nCalculated:\nC - 59.13%\nH - 5.41%\nCl - 7.93%\nF - 4.25%\nN - 12.54%\n\nStorage and Stability:\nMay be stored at RT for short-term only. Long-term storage is recommended at -20 degrees C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.

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SPECIFICATIONS

Catalog Number

G2023-95A

Size

1g

Form

Supplied as a white to off-white powder.

Purity

~99% (HPLC, TLC)

References

1. Pao, W., et al. \"EGF receptor gene mutations are common in lung cancers from \"never smokers\" and are associated with sensitivity of tumors to gefitinib and erlotinib.\" Proc. Natl. Acad. Sci. USA 101:13306-13311 (2004). 2. Sordella, R., et al. \"Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways.\" Science 305:1163-1167 (2004). 3. Azzariti, A., et al. \"Prolonged exposure of colon cancer cells to the epidermal growth factor receptor inhibitor gefitinib (Iressa(TM)) and to the antiangiogenic agent ZD6474: Cytotoxic and biomolecular effects.\" World J. Gastroenterol. 12:5140-5147 (2006). 4. Wakeling, A.E., et al. \"ZD1839 (Iressa), An Orally Active Inhibitor of Epidermal Growth Factor Signaling with Potential for Cancer Therapy.\" Cancer Res. 62:5749-5754 (2002).

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SUPPLIER INFO

United States Biological

Address:

4 Technology Way, Salem, MA 01970, US

Phone:

+1 800 520 3011

Website:

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