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MedKoo product information:
Gefitinib
Gefitinib is an anilinoquinazoline with antineoplastic activity.
Gefitinib inhibits the catalytic activity of numerous tyrosine
kinases including the epidermal growth factor receptor (EGFR), which
may result in inhibition of tyrosine kinase-dependent tumor growth.
Specifically, this agent competes with the binding of ATP to the
tyrosine kinase domain of EGFR, thereby inhibiting receptor
autophosphorylation and resulting in inhibition of signal
transduction. Gefitinib may also induce cell cycle arrest and
inhibit angiogenesis. Gefitinib (INN) (Iressa) is a drug used in the
treatment of certain types of cancer. Gefitinib is an EGFR inhibitor,
like erlotinib, which interrupts a growth factor in cancer cells. It is
marketed by AstraZeneca and Teva. Check for
active clinical trials or
closed clinical trials using this agent. (NCI
Thesaurus).
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MedKoo Code#: 100140
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Name:
Gefitinib
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CAS#:
184475-35-2
Synonym: US brand name:
Iressa. Code name: ZD 1839.
IUPAC/Chemical name:
N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine
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Chemical structure:
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Theoretical analysis
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MedKoo Code#: 100140
Name: Gefitinib
CAS#: 184475-35-2
Chemical Formula: C22H24ClFN4O3
Exact Mass: 446.15210
Molecular Weight: 446.90
Elemental Analysis: C, 59.13; H, 5.41; Cl,
7.93; F, 4.25; N, 12.54; O, 10.74
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Availability and price:
Gefitinib (98%) is in stock.
100 mg / $190.00
500 mg / $350.00
1 g / $450.00
For quotation, question, and order, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer big discount for
orders of bulk quantities.
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Quality control
data:
Product will be shipped with
supporting analytical data.
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Information about this agent
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According to
http://en.wikipedia.org/wiki/Gefitinib, Gefitinib is the first
selective inhibitor of epidermal growth factor receptor's (EGFR)
tyrosine kinase domain. Thus gefitinib is an EGFR inhibitor. The target
protein (EGFR) is also sometimes referred to as Her1 or ErbB-1 depending
on the literature source. EGFR is overexpressed in the cells of certain
types of human carcinomas - for example in lung and breast cancers. This
leads to inappropriate activation of the anti-apoptotic Ras signalling
cascade, eventually leading to uncontrolled cell proliferation. Research
on gefitinib-sensitive non-small cell lung cancers has shown that a
mutation in the EGFR tyrosine kinase domain is responsible for
activating anti-apoptotic pathways. These mutations tend to confer
increased sensitivity to tyrosine kinase inhibitors such as gefitinib
and erlotinib. Of the types of non-small cell lung cancer histologies,
adenocarcinoma is the type that most often harbors these mutations.
These mutations are more commonly seen in Asians, women, and non-smokers
(who also tend to more often have adenocarcinoma). Gefitinib inhibits
EGFR tyrosine kinase by binding to the adenosine triphosphate
(ATP)-binding site of the enzyme. Thus the function of the EGFR tyrosine
kinase in activating the Ras signal transduction cascade is inhibited,
and malignant cells are inhibited.
Gefitinib is currently
only indicated for the treatment of locally advanced or metastatic
non-small cell lung cancer (NSCLC) in patients who have previously
received chemotherapy. While gefitinib has yet to be proven to be
effective in other cancers, there is potential for its use in the
treatment of other cancers where EGFR overexpression is involved.
In 2004, AstraZeneca informed the United States Food and Drug
Administration (FDA) that a large randomized study failed to demonstrate
a survival advantage for gefitinib in the treatment of non-small cell
lung cancer (NSCLC). Whether progression-free survival is prolonged is
not clear from this statement. AstraZeneca also withdrew their
application to market gefitinib in Europe shortly after this
announcement.
Erlotinib is another EGFR tyrosine kinase inhibitor that works in the
same way as gefitinib. Given the lack of survival advantage for
gefitinib and the positive results for erlotinib, erlotinib has replaced
gefitinib in the United States (except in patients where gefitinib has
had a proven response).
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