Gefitinib

ArtNr	S1025-10mM
Hersteller	Selleckchem
CAS-Nr.	184475-35-2
Menge	10 mM/1 mL
Quantity options	100 mg 1 g 10 g 10 mM/1 mL 250 mg 5 g
Kategorie	Oncology Neuroscience Neural Signaling Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Bladder Cancer Colorectal Cancer
Typ	Inhibitors
Specific against	other
Smiles	COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	ZD1839
Similar products	Gefitinib
Lieferbar
Manufacturer - Targets	EGFR, TYR
Storage Conditions	2 years -80 in solvent
Molecular Weight	446, 9
Administration	Once daily by oral administration (0.1 mL/10 g body weight) for 14 days
Animal Models	Female nude mice (cba nu/nu) aged 8â€“10 weeks are intra-dermal injected with LoVo cells.
Cell lines	NR6, NR6M and NR6W cells
Clinical Trials	Gefitinib has entered in a phase II clinical trial in the treatment of non small cell lung cancer.
Concentrations	0-2 uM
Dosages	100 mg/kg
Formulation	0.5% polysorbate
IC50	37 nM, 37 nM, 37 nM, 37 nM, 37 nM, 37 nM
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-gamma, with IC50 of 27nM, in NR6W cells. The NR6wtEGFR and NR6M cell lines has low levels of PLC-gamma 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 0.5uM significantly facilitates, rather than abrogates, colony formation of NR6M cells. However, at a concentration of 2 uM Gefitinib completely blocks NR6M colony formation. Gefitinib rapidly and in a dose-dependent manner inhibits EGFR and ERK phosphorylation up to 72 hours after EGF stimulation in both the high- and low-EGFR-expressing cell lines. [1] Gefitinib is the monolayer growth of these EGF-driven untransformed MCF10A cells with an IC50 of 20 nM. [2] The combination of Gefitinib (0.2 uM and 0.5 uM) with irradiation lead to a significant growth inhibition in LoVo cells, compared with radiation alone.. [3]
In vivo	Gefitinib (100 mg/kg) improves the anti-tumor effect of radiotherapy in LoVo tumor xenografts. [3] Gefitinib treatment of nude mice bearing established human GEO colon cancer xenografts reveals a reversible dose-dependent inhibition of tumor growth because GEO tumors resumes the growth rate of controls at the end of the treatment. [4]
Incubation Time	72 hours
Method	Exponentially growing cells including NR6, NR6M, NR6M and NR6W cells are seeded in sextuple in 96-well plates at a concentration of 2000 cells/well, allowed to adhere and subsequently washed in PBS and incubated overnight in medium containing 0.5% FCS. Cells are then treated with varying concentrations (0-2 uM) of Gefitinib or the solute control DMSO and EGF. The optimal EGF concentration for inducing proliferation of NR6wtEGFR and NR6W cells has previously been determined and hence NR6wtEGFR and NR6W cells are supplemented with 10 nM and 0.1 nM EGF, respectively. EGF is not added to NR6 and NR6M cells. After 72 hours the amount of cells are measured by performing a MTT proliferation assay.
Solubility (25C)	DMSO 89 mg/mL, Water <1 mg/mL, Ethanol 4 mg/mL
Information	Gefitinib is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.
Chemical Name	N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine
Features	Gefitinib is a potent EGFR tyrosine kinase inhibitor.

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