名称：原装进口| Gefitinib, Free Base
Storage: Store at or below -20 ºC.
Solubility: Soluble in DMSO, up to about 100 mg/mL; very poorly soluble in water or ethanol. Disposal: A. Gefitinib, Free Base, >99%.
View the MSDS for this product
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. The IC50 values for gefitinib for inhibiting HT-29 and LoVo cell growth were 23.6 - >100 µM and 7.3 - 48.5 µM, respectively, when the exposure times are from 18 hours to 3 days.
The functions of the EGFR tyrosine kinase in activating the Ras signal transduction cascade and malignant cell growth are thus inhibited. Gefitinib was found to be a potent inhibitor of EGFR kinase (Ki = 0.40 nM), but much weaker against ErbB-2 kinase (Ki = 870 nM) and ErbB-4 kinase (Ki = 1.1 µM). EGFR tyrosine kinase inhibitor that binds to the ATP-binding site of the enzyme.