4-[(3-chloro-4-fluorophenyl)amino]-6-[3-(morpholin-4-yl)-propyloxy]-7-methoxy-quianazoline

Synonym
Product Category
Product Code
CAS Number
MDL Number
Pubchem CID
Reaxys RN
Gefitinib, ZD1839
API & Intermediates
KAPI1F02
184475-35-2
MFCD04307832
123631
8949523
image-155171-Trimethyl(trifluoromethyl)silane_reagent.png
Chemical Name
Molecular Formula
Molecular Weight
Assay
Appearance
Melting Point
Packaging
Storage
4-[(3-chloro-4-fluorophenyl)amino]-6-[3-(morpholin-4-yl)-propyloxy]-7-methoxy-quianazoline
C22H24ClFN4O3
446.91
≥98%(HPLC)
White to Off-white Solid
194-198°C
10g,20g,50g,100g,500g,1kg and 5kg
-20°C Freezer
Gefitinib (formally labeled as ZD1839) is a selective epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitor that blocks the growth of GEO colon, ZR-75-1, MCF-10A Ha-ras breast and OVCAR-3 ovarian cancer cell lines with IC50 values of 0.2-0.4 µM. By interfering with the intracellular kinase domain, gefitinib prevents EGFR autophosphorylation and prevents downstream signal transduction. Formulations containing gefitinib were previously used to treat advanced (or recurrent) non-small cell lung cancer (NSCLC) with approval. However, the FDA retracted its general approval when a phase III trial failed to demonstrate an overall survival benefit. Formulations containing gefitinib appear to be most efficacious in treating certain EGFR gene mutations prevalent in Asian populations.
Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitor. [1]
ZD1839 (Iressa), a novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, potently inhibits the growth of EGFR-positive cancer cell lines with or without erbB2 overexpression. [2]
ZD1839 (Iressa) induces antiangiogenic effects through inhibition of epidermal growth factor receptor tyrosine kinase. [3]
Efficacy of gefitinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in symptomatic patients with non-small cell lung cancer: a randomized trial. [4]
Gefitinib in non-small cell lung cancer. [5]
EGFR Inhibition in the Treatment of Non-Small Cell Lung Cancer. [6]
Gefitinib as first-line therapy for advanced or metastatic non-small cell lung cancer patients in southern Taiwan. [7]
Efficacy of gefitinib for elderly patients with advanced non-small cell lung cancer harboring epidermal growth factor receptor gene mutations: a retrospective analysis. [8]
References:
[1] F.Ciardiello, et al, Clin. Cancer Res., 2000, 6(5), pp 2053-2063.
[2] N.G.Anderson, et al, Int. J. Cancer, 2001, 94(6), pp 774-782.
[3] A.Hirata, et al, Cancer Res., 2002, 62, pp 2554-2550.
[4] M.G.Kris, et al, J. Am. Med. Assoc., 2003, 290(16), pp 2149-2158.
[5] K.Tamura, et al, Expert Opin. Pharmacother., 2005, 6(6), pp 985-993.
[6] D.E.Gerber, Drug Dev. Res., 2008, 69(6), pp 359-372.
[7] C.T.Yang, et al, Kaohsiung J. Med. Sci., 2010, 26(1), pp 1-7.
[8] H.Uruga, et al, Intern. Med., 2010, 49(2), pp 103-107.
Signal Word
Hazard Statements
Precautionary Statements
HS Code
RIDADR
Legal Information
Warning
H302,H315,H319,H335
P301+P312+P330,P305+P351+P338
29349990900
NONH for all modes of transport
Sales restrictions may apply.
1. Product Specification
For further information and support on Ph. Eur. Reference Standard, please go to the website of the issuing pharmacopoeia.
2. Safety Data Sheet
SDS issued by EDQM can be found here.
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