184475-55-6

Name	Gefitinib hydrochloride
Synonyms	Gefitinib Hcl Iressa hydrochloride ZD-1839 hydrochloride Gefitinib hydrochloride Gefitinib hydrochloride salt Gefitinib hydrochloride (ZD-1839 hydrochloride) 4-(3-Chloro-4-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazoline hydrochloride N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine hydrochloride
CAS	184475-55-6
EINECS	1533716-785-6
InChI	InChI=1/C22H24ClFN4O3.ClH/c1-29-20-13-19-16(12-21(20)31-8-2-5-28-6-9-30-10-7-28)22(26-14-25-19)27-15-3-4-18(24)17(23)11-15;/h3-4,11-14H,2,5-10H2,1H3,(H,25,26,27);1H

Molecular Formula	C22H24ClFN4O3.HCl
Molar Mass	483.37
Boling Point	607.7°C at 760 mmHg
Flash Point	321.3°C
Vapor Presure	4.9E-15mmHg at 25°C
Storage Condition	2-8℃
Use	This product is for scientific research only and shall not be used for other purposes.
In vitro study	Gefitinib (0.01-0.1 mM) results in increased phosphotyrosine load of the receptor, increased signalling to ERK and stimulation of proliferation and anchorage-independent growth, presumably by inducing EGFRvIII dimerisation in long-term exposure of EGFRvIII-expressing cells. On the other hand, gefitinib (1-2 mM) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth. Gefitinib (ZD1839) inhibits the monolayer growth of these EGF-driven untransformed cells with IC 50 of 20 nM. Gefitinib leads to an inhibition of CALU-3 and GLC82 cell proliferation, with an IC 50 of 2 μM.
In vivo study	Gefitinib (150 mg/kg, p.o.) in conbination with Metformin induces a significant reduction in tumor growth in nude mice bearing H1299 or CALU-3 GEF-R cells that are grown subcutaneously as tumor xenografts. In irradiated rats, Gefitinib treatment augmentes lung inflammation, including inflammatory cell infiltration and pro-inflammatory cytokine expression, while Gefitinib treatment attenuates fibrotic lung remodeling due to the inhibition of lung fibroblast proliferation.