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Gefitinib hydrochloride Chemical Structure

Gefitinib hydrochloride

Data Sheet For research use only. Not for human use.
Cat. No. :BCP05217CAS No. :184475-55-6Purity:98%
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  • Chemical Properties&Biological Activity
CAS No. 184475-55-6 Cat. No. BCP05217
Name Gefitinib hydrochloride
Synonyms ZD 1839;ZD-1839;ZD1839;
SMILES
Chemical Name
Formula C22H24ClFN4O3.HCl M. Wt 483.37
Purity 98% Storage Store at 4-8°C
Description in vitro: Gefitinib effectively inhibits all tyrosine phosphorylation sites on EGFR in both the high and low-EGFR-expressing cell lines including NR6, NR6M and NR6W cell lines. The phosphorylation sites Tyr1173 and Tyr992 are less sensitive requiring higher concentrations of Gefitinib for inhibition. Gefitinib effectively blocks the phosphorylation of PLC-γ, with IC50 of 27nM, in NR6W cells. The NR6wtEGFR and NR6M cell lines has low levels of PLC-γ phosphorylation but the level in the NR6M cell line is more resistant to inhibition by Gefitinib with IC50 of 43 nM and 369 nM, respectively. Gefitinib inhibits Akt phosphorylations, with IC50 of 220 and 263nM, in the low-EGFR- and -EGFRvIII-expressing cell lines, respectively. Gefitinib in the dose range from 0.1 to 0.5μM significantly facilitates, rather than abrogates, colony formation of NR6M cells. However, at a concentration of 2 μM Gefitinib completely blocks NR6M colony formation. Gefitinib rapidly and in a dose-dependent manner inhi
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