General
Preferred name
GEFITINIB
Synonyms
Iressa ()
ZD-1839 ()
Iressa, ZD-1839 ()
ZD1839 ()
ZD1839 hydrochloride ()
ZD-1839 hydrochloride ()
Gefitinib (Iressa) ()
Gefitinib (hydrochloride) ()
Iressa,ZD1839 ()
Gefitinib hydrochloride ()
Gefitinib (ZD1839) ()
GefitinibIressaZD1839N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine ()
NSC-759856 ()
Gefitinib-d6 ()
Gefitinib mylan ()
GEFITINIB MYLAN ()
P&D ID
PD003385
CAS
184475-35-2
184475-55-6
1228664-49-0
Tags
available
probe
drug
obsolete probe
Approved by
FDA
First approval
2003
Drug indication
non-small cell lung carcinoma
Urethral cancer
Head and neck cancer
Solid tumour/cancer
Drug Status
approved
withdrawn
investigational
Max Phase
4.0
Probe info
Probe type
calculated probe
Probe sources
Probe Miner (suitable probes)
Probe targets
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
MOA Gefitinib is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase that binds to the adenosine triphosphate (ATP)-binding site of the enzyme. EGFR is often shown to be overexpressed in certain human carcinoma cells, such as lung and breast cancer cells. Overexpression leads to enhanced activation of the anti-apoptotic Ras signal transduction cascades, subsequently resulting in increased survival of cancer cells and uncontrolled cell proliferation. Gefitinib is the first selective inhibitor of the EGFR tyrosine kinase which is also referred to as Her1 or ErbB-1. By inhibiting EGFR tyrosine kinase, the downstream signaling cascades are also inhibited, resulting in inhibited malignant cell proliferation.
DESCRIPTION Gefitinib is an orally active Type-1 kinase inhibitor and was first approved by the US FDA in 2003. Gefitinib has selectivity for the EGFR . (GtoPdb)
PRICE 29
DESCRIPTION Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer [1][2][5].
PRICE 29
DESCRIPTION inhibitor of EGFR and AKT1 (Informer Set)
DESCRIPTION For the continued treatment of patients with locally advanced or metastatic non-small cell lung cancer after failure of either platinum-based or docetaxel chemotherapies. (PKIDB)
DESCRIPTION Selective Chk2 inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Orally active, selective EGFR inhibitor (Tocriscreen Plus)
DESCRIPTION Orally active, selective EGFR inhibitor (Tocriscreen Total)
DESCRIPTION Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor. It appear to be most efficacious in treating certain EGFR gene mutations prevalent in Asian populations. (Enamine Bioactive Compounds)
DESCRIPTION Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation. (TargetMol Bioactive Compound Library)
DESCRIPTION Gefitinib Hcl(ZD-1839 Hcl) is an EGFR inhibitor, which interrupts signaling through the epidermal growth factor receptor (EGFR) in target cells. (BOC Sciences Bioactive Compounds)
DESCRIPTION Gefitinib hydrochloride (ZD-1839 hydrochloride) is an orally active selective and potent tyrosine kinase (EGFR) inhibitor. Gefitinib hydrochloride exhibits antitumor activity, selectively inhibits EGF-stimulated tumor cell growth, induces cellular autophagy, improves lung dysfunction, and inhibits inflammation. Gefitinib hydrochloride has antitumor activity, selectively inhibits EGF-stimulated tumor cell growth, induces cellular autophagy, ameliorates lung dysfunction, and inhibits the progression of inflammation and fibrosis. (TargetMol Bioactive Compound Library)
Cell lines
623
Organisms
2
Compound Sets
44
AdooQ Bioactive Compound Library
A10422
Axon Medchem Screening Library
1393
BOC Sciences Bioactive Compounds
gefitinib-hydrochloride-cas-184475-55-6-340967
Cayman Chemical Bioactives
13166
22364
CeMM library of unique drugs (CLOUD)
ChEMBL Approved Drugs
CHEMBL939
ChEMBL Drugs
CHEMBL939
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
4941
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB00317
DrugBank Approved Drugs
DB00317
DrugCentral
1282
DrugCentral Approved Drugs
1282
DrugMAP
DM15F0X
DrugMAP Approved Drugs
DM15F0X
DrugMatrix
Enamine Bioactive Compounds
EBC-07543
Enamine BioReference Compounds
EUbOPEN Chemogenomics Library
EUB0000649
Guide to Pharmacology
4941
Informer Set
52926
Ki Database
Iressa
LINCS compound set
10098-101
10098-999
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL939
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL939
MedChem Express Bioactive Compound Library
HY-50895
HY-50895A
NCATS Inxight Approved Drugs
S65743JHBS
NIH Approved Oncology Drugs
532631
NPC Screening Collection
Obsolete Compounds
gefitinib
PKIDB
Prestwick Chemical Library
Probe Miner (suitable probes)
O14976/337949
ReFrame library
Selleckchem Bioactive Compound Library
Gefitinib
gefitinib-hydrochloride
TargetMol Bioactive Compound Library
T1181
T1181L
The Spectrum Collection
Tocris Bioactive Compound Library
3000
Tocriscreen Plus
3000
Tocriscreen Total
Welcome Trust Cancer Drugs
1010
Withdrawn 2.0
895
External IDs
72
Properties
(calculated by RDKit )
Molecular Weight
446.15
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
1
Rotatable Bonds
8
Ring Count
4
Aromatic Ring Count
3
cLogP
4.28
TPSA
68.74
Fraction CSP3
0.36
Chiral centers
0.0
Largest ring
6.0
QED
0.52
Structural alerts
3
aggregator (Aggregator Advisor)
Aggregators
historic compounds (Chemical Probes.org)
Obsolete
aggregator (ZINC)
Aggregators
Related compounds
Custom attributes
(extracted from source data)
Target
AKT1
EGFR
Epidermal growth factor receptor erbB1
Apoptosis
Apoptosis related,Autophagy,EGFR
Tyr1173 (NR6W cells)
Tyr1173 (NR6wtEGFR cells)
Tyr992
Tyr992 (NR6W cells)
Tyr992 (NR6wtEGFR cells)
Compound status
FDA
Target Type
Enzyme-Linked Receptors
Pathway
EGFR signaling
Angiogenesis
Autophagy
JAK/STAT Signaling
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
MOA
receptor protein-tyrosine kinase inhibitor
Inhibitor
EGFR inhibitor
Indication
non-small cell lung cancer (NSCLC)
ATC
L01XE02
Therapeutic Class
Anticancer Agents
Recommended Cell Concentration
None
Source data