Product Information

S1025 Gefitinib
Technical Data:
M.Wt: Formula: Solubility: Purity: Storage: CAS No.: 446.90 C22H24ClFN4O3 DMSO 99% at -20 2 years 184475-35-2
N O O O HN N N Cl F

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Synonyms: ZD-1839,

Iressa

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Biological Activity
Gefitinib (ZD-1839, Iressa) is a novel potent EGFR tyrosine kinase and Akt phosphorylations inhibitor with IC50 of 37, 26 and 57 nM for Tyr1173, Tyr1173 and Tyr992 in, respectively, the low and high EGFR expressing cell lines. Immunoblot analysis of whole cell lysates revealed that in general gefitinib effectively inhibited all tyrosine phosphorylation sites on EGFR in both the high and low-EGFR-expressing cell lines. However, the phosphorylation sites Tyr1173 and Tyr992 were less sensitive requiring higher concentrations of gefitinib for inhibition. As was the case for ERK, gefitinib fails to effectively inhibit AKT phosphorylation in the high-EGFR-expressing cell line indicating that EGFR is not the major activator of AKT in this cell line. The low IC50 (7 nM), however show that the weak induction of AKT phosphorylation by EGFR in this cell line is efficiently blocked by gefitinib. Gefitinib inhibits AKT phosphorylations, with IC50 values of 220 and 263 nM, in the low-EGFR- and EGFRvIII-expressing cell lines, respectively. [1]

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References
[1] Pedersen MW et al. Br J Cancer. 2005 Oct 17; 93(8):915-23.

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Notes
PLEASE KEEP THE PRODUCT UNDER -20 FOR LONG-TERM STORAGE. NOT FOR HUMAN OR VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.
Specific storage and handling information for each product is indicated on the product datasheet. Most Selleck products, stored under the recommended conditions, are stable for two years. Products are sometimes shipped at a temperature that differs from the recommended storage temperature,most are recommended stored at -20 Many products are stable in the short-term at temperatures that differ from that . required for long-term storage. We ensure that the product is shipped under conditions that will maintain the quality of the product, but save your shipping charges by using the most economical storage conditons for an overnight shipment. Upon receipt of the product, follow the storage recommendations on the product data sheet.

be received from our customer service team. Returns accepted will be subject to a 30% restocking charge.

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