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Gefitinib (ZD1839) - ≥99%, high purity , Epidermal growth factor receptor erbB1 inhibitor, CAS No.184475-35-2, Epidermal growth factor receptor erbB1 inhibitor

Moligand™

≥99%

CAS#: 184475-35-2
Formula: C₂₂H₂₄ClFN₄O₃
Molecular Weight: 446.9
MDL number: MFCD04307832
PubChem CID: 123631

Item Number

G125799

Grouped product items
SKU	Size	Availability	Price
G125799-50mg	50mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$9.90
G125799-250mg	250mg	In stock	$26.90
G125799-1g	1g	In stock	$88.90
G125799-5g	5g	In stock	$177.90
G125799-10g	10g	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$320.90
G125799-25g	25g	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$720.90
G125799-100g	100g	In stock	$2,595.90

selective EGFR tyrosine kinase inhibitor

View related series

epidermal growth factor receptor Inhibitor

Basic Description

Synonyms	Gefitinib \| 184475-35-2 \| Iressa \| ZD1839 \| Irressat \| N-(3-Chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine \| gefitinib (zd1839) \| ZD 1839 \| ZD-1839 \| N-(3-chloro-4-fluorophenyl)-7-methoxy-6-[3-(morpholin-4-yl)propoxy]quinazolin-4-amine \| gefitinib
Specifications & Purity	Moligand™, ≥99%
Biochemical and Physiological Mechanisms	Gefitinib is an epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitor and has been shown to increase phosphorylation of c-Jun NH2-terminal kinase (JNK) and p38 mitogen-activated protein kinase (MAPK) in HaCaT cells. Studies suggest that gefiti
Storage Temp	Store at 2-8°C
Shipped In	Wet ice
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of action	Epidermal growth factor receptor erbB1 inhibitor
Note	Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description	Gefitinib (ZD-1839) 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. An EGFR-tyrosine kinase inhibitor

Product Properties

ALogP	4.1

Associated Targets(Human)

ERBB2 Tclin Receptor tyrosine-protein kinase erbB-2 (3 Activities)

Discover Target: ERBB2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

EGFR Tclin Epidermal growth factor receptor (128 Activities)

Discover Target: EGFR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GAK Tchem Cyclin-G-associated kinase (7 Activities)

Discover Target: GAK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RELA Tchem Transcription factor p65 (1 Activities)

Discover Target: RELA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RIPK2 Tchem Receptor-interacting serine/threonine-protein kinase 2 (1 Activities)

Discover Target: RIPK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABCG2 Tchem ATP-binding cassette sub-family G member 2 (1 Activities)

Discover Target: ABCG2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)

Discover Target: ABL1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

EGFR Tclin Epidermal growth factor receptor erbB1 (33727 Activities)

Discover Target: EGFR

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ESR1 Tclin Estrogen receptor alpha (17718 Activities)

Discover Target: ESR1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

NR3C1 Tclin Glucocorticoid receptor (14987 Activities)

Discover Target: NR3C1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

INSR Tclin Insulin receptor (5558 Activities)

Discover Target: INSR

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PGR Tclin Progesterone receptor (8562 Activities)

Discover Target: PGR

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ADRB2 Tclin Beta-2 adrenergic receptor (11824 Activities)

Discover Target: ADRB2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 Activities)

Discover Target: CHRM2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ADRB1 Tclin Beta-1 adrenergic receptor (6630 Activities)

Discover Target: ADRB1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 Activities)

Discover Target: HTR1A

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

AR Tclin Androgen Receptor (11781 Activities)

Discover Target: AR

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 Activities)

Discover Target: CHRM1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

TOP2A Tclin DNA topoisomerase II alpha (6317 Activities)

Discover Target: TOP2A

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

VDR Tclin Vitamin D receptor (26531 Activities)

Discover Target: VDR

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

IMPDH2 Tclin Inosine-5'-monophosphate dehydrogenase 2 (1326 Activities)

Discover Target: IMPDH2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

DRD2 Tclin Dopamine D2 receptor (23596 Activities)

Discover Target: DRD2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

GABRA1 Tclin GABA receptor alpha-1 subunit (399 Activities)

Discover Target: GABRA1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

MAOA Tclin Monoamine oxidase A (11911 Activities)

Discover Target: MAOA

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CNR1 Tclin Cannabinoid CB1 receptor (20913 Activities)

Discover Target: CNR1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

DRD1 Tclin Dopamine D1 receptor (9720 Activities)

Discover Target: DRD1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PTGS1 Tclin Cyclooxygenase-1 (9233 Activities)

Discover Target: PTGS1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

SLC6A2 Tclin Norepinephrine transporter (10102 Activities)

Discover Target: SLC6A2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HRH2 Tclin Histamine H2 receptor (5428 Activities)

Discover Target: HRH2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HTR2A Tclin Serotonin 2a (5-HT2a) receptor (14758 Activities)

Discover Target: HTR2A

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HTR2C Tclin Serotonin 2c (5-HT2c) receptor (11471 Activities)

Discover Target: HTR2C

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

AVPR2 Tclin Vasopressin V2 receptor (2912 Activities)

Discover Target: AVPR2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ADORA1 Tclin Adenosine A1 receptor (17603 Activities)

Discover Target: ADORA1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

AGTR1 Tclin Type-1 angiotensin II receptor (5176 Activities)

Discover Target: AGTR1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

SLC6A4 Tclin Serotonin transporter (12625 Activities)

Discover Target: SLC6A4

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ADRA1A Tclin Alpha-1a adrenergic receptor (8359 Activities)

Discover Target: ADRA1A

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PTGS2 Tclin Cyclooxygenase-2 (13999 Activities)

Discover Target: PTGS2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HRH1 Tclin Histamine H1 receptor (7573 Activities)

Discover Target: HRH1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

OPRM1 Tclin Mu opioid receptor (19785 Activities)

Discover Target: OPRM1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

DRD3 Tclin Dopamine D3 receptor (14368 Activities)

Discover Target: DRD3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

AVPR1A Tclin Vasopressin V1a receptor (5412 Activities)

Discover Target: AVPR1A

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

OPRD1 Tclin Delta opioid receptor (15096 Activities)

Discover Target: OPRD1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

OPRK1 Tclin Kappa opioid receptor (16155 Activities)

Discover Target: OPRK1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HTR3A Tclin Serotonin 3a (5-HT3a) receptor (3366 Activities)

Discover Target: HTR3A

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

SLC6A3 Tclin Dopamine transporter (10535 Activities)

Discover Target: SLC6A3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

GRIN1 Tclin Glutamate (NMDA) receptor subunit zeta 1 (122 Activities)

Discover Target: GRIN1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

KCNH2 Tclin HERG (29587 Activities)

Discover Target: KCNH2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PDE3A Tclin Phosphodiesterase 3A (3309 Activities)

Discover Target: PDE3A

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ERBB2 Tclin Receptor protein-tyrosine kinase erbB-2 (7851 Activities)

Discover Target: ERBB2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PDGFRB Tclin Platelet-derived growth factor receptor beta (5195 Activities)

Discover Target: PDGFRB

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ADRA2B Tclin Alpha-2b adrenergic receptor (4412 Activities)

Discover Target: ADRA2B

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ADRA2C Tclin Alpha-2c adrenergic receptor (4876 Activities)

Discover Target: ADRA2C

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CHRM3 Tclin Muscarinic acetylcholine receptor M3 (7750 Activities)

Discover Target: CHRM3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 Activities)

Discover Target: HTR2B

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

IGF1R Tclin Insulin-like growth factor I receptor (8605 Activities)

Discover Target: IGF1R

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

KIT Tclin Stem cell growth factor receptor (10667 Activities)

Discover Target: KIT

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Associated Targets(non-human)

Cdk4 Cyclin-dependent kinase 4 (3 Activities)

Discover Target: Cdk4

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Npy1r Neuropeptide Y receptor type 1 (8 Activities)

Discover Target: Npy1r

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Cruzipain (33337 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Cckar Cholecystokinin A receptor (90 Activities)

Discover Target: Cckar

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PIK3CA PI3-kinase p110-alpha subunit (51 Activities)

Discover Target: PIK3CA

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Pde4d Phosphodiesterase 4D (4 Activities)

Discover Target: Pde4d

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Pygl Liver glycogen phosphorylase (81 Activities)

Discover Target: Pygl

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Prkcd Protein kinase C delta (192 Activities)

Discover Target: Prkcd

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Prkcb Protein kinase C beta (2 Activities)

Discover Target: Prkcb

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Abcb1b P-glycoprotein 1 (174 Activities)

Discover Target: Abcb1b

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Mapk1 MAP kinase ERK2 (650 Activities)

Discover Target: Mapk1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Hdac1 Histone deacetylase 1 (93 Activities)

Discover Target: Hdac1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Hdac6 Histone deacetylase 6 (222 Activities)

Discover Target: Hdac6

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Fgfr4 Fibroblast growth factor receptor 4 (138 Activities)

Discover Target: Fgfr4

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)

Discover Target: Fgfr3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Camk2g CaM kinase II gamma (1 Activities)

Discover Target: Camk2g

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HD1 Histone deacetylase (38 Activities)

Discover Target: HD1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Tec Tyrosine-protein kinase TEC (25 Activities)

Discover Target: Tec

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Ulk3 ULK3 kinase (23 Activities)

Discover Target: Ulk3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Staphylococcus aureus (210822 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Mycobacterium tuberculosis (203094 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Saccharomyces cerevisiae (19171 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Plasmodium falciparum (966862 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Toxoplasma gondii (4585 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Mus musculus (284745 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Rattus norvegicus (775804 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Vaccinia virus (4609 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

BaF3 (4657 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CHO-K1 (1115 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

MDCK (10148 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Vero (26788 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Ehrlich (1318 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

H4 (48 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

NIH3T3 (5395 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

L929 (3802 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Lewis lung carcinoma cell line (1243 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

B16-F10 (4610 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

AIRC Multifunctional protein ADE2 (8 Activities)

Discover Target: AIRC

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

norA Quinolone resistance protein norA (2171 Activities)

Discover Target: norA

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

rep Replicase polyprotein 1ab (378 Activities)

Discover Target: rep

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Brain (1 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Blood (6 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Plasma (328 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Cerebrospinal fluid (288 Activities)

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Mapt Microtubule-associated protein tau (6 Activities)

Discover Target: Mapt

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

pknB Serine/threonine-protein kinase pknB (356 Activities)

Discover Target: pknB

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CDPK1 Calcium-dependent protein kinase 1 (793 Activities)

Discover Target: CDPK1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CRK2 Cell division control protein 2 homolog (194 Activities)

Discover Target: CRK2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Septin9 Septin-9 (1 Activities)

Discover Target: Septin9

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Acadvl Very long-chain specific acyl-CoA dehydrogenase, mitochondrial (1 Activities)

Discover Target: Acadvl

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Names and Identifiers

IUPAC Name	N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine
INCHI	InChI=1S/C22H24ClFN4O3/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)
InChi Key	XGALLCVXEZPNRQ-UHFFFAOYSA-N
Canonical SMILES	COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4
Isomeric SMILES	COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4
PubChem CID	123631
Molecular Weight	446.9

Database links

DrugBank Ligand	DB00317
Wikipedia	Gefitinib
ChEBI	CHEBI:49668
CAS Registry No.	184475-35-2
DiscoveRx TREEspot	Gefitinib\|
PubChem CID	123631
ChEMBL Ligand	CHEMBL939
RCSB PDB Ligand	IRE
PEP	gefitinib
Reactome Reaction	R-HSA-9665121, R-HSA-1220610
Reactome Drug	R-ALL-1169429
DrugCentral Ligand	1282

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

14 results found

Lot Number	Certificate Type	Date	Item
D2409083	Certificate of Analysis	Mar 02, 2024	G125799
L2312045	Certificate of Analysis	Dec 21, 2023	G125799
L2129202	Certificate of Analysis	Oct 10, 2023	G125799
L2129283	Certificate of Analysis	Oct 10, 2023	G125799
L2129286	Certificate of Analysis	Oct 10, 2023	G125799
L2129287	Certificate of Analysis	Oct 10, 2023	G125799
L2129291	Certificate of Analysis	Oct 10, 2023	G125799
K2112570	Certificate of Analysis	Aug 17, 2023	G125799
B2328181	Certificate of Analysis	Dec 10, 2021	G125799
B2328182	Certificate of Analysis	Dec 10, 2021	G125799
F2404021	Certificate of Analysis	Dec 10, 2021	G125799
H2311043	Certificate of Analysis	Dec 10, 2021	G125799
H2311045	Certificate of Analysis	Dec 10, 2021	G125799
I2306064	Certificate of Analysis	Dec 10, 2021	G125799

Chemical and Physical Properties

Solubility	Soluble in DMSO (89 mg/ml at 25 °C), methanol (20 mg/ml), ethanol (4 mg/ml at 25 °C), DMF (20 mg/ml), and water (<1 mg/ml at 25 °C).
Sensitivity	Heat Sensitive
Specific Rotation[α]	1.62
Boil Point(°C)	586.8 °C
Melt Point(°C)	194.0 to 198.0 °C

Safety and Hazards(GHS)

Pictogram(s)	GHS08, GHS09, GHS05, GHS07
Signal	Danger
Hazard Statements	H315:Causes skin irritation H351:Suspected of causing cancer H373:Causes damage to organs through prolonged or repeated exposure H411:Toxic to aquatic life with long lasting effects H302:Harmful if swallowed H318:Causes serious eye damage H400:Very toxic to aquatic life H361:Suspected of damaging fertility or the unborn child
Precautionary Statements	P273:Avoid release to the environment. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P270:Do not eat, drink or smoke when using this product. P362+P364:Take off contaminated clothing and wash it before reuse. P391:Collect spillage. P330:Rinse mouth. P203:Obtain, read and follow all safety instructions before use. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P301+P317:IF SWALLOWED: Get medical help. P305+P354+P338:IF IN EYES: Immediately rinse with water for several minutes. Remove contact lenses if present and easy to do. Continue rinsing. P318:if exposed or concerned, get medical advice. P317:Get emergency medical help. P332+P317:If skin irritation occurs: Get medical help. P319:Get medical help if you feel unwell.

Citations of This Product

1. Jiali Wang, Xianhai He, Zhirong Jia, Aiwen Yan, Kang Xiao, Shuo Liu, Mengjun Hou, Yaling Long & Xuansheng Ding. (2023) Shenqi Fuzheng injection restores the sensitivity to gefitinib in non-small cell lung cancer by inhibiting the IL-22/STAT3/AKT pathway. Pharmaceutical Biology, 1 (61): (33-41). [PMID:38100532]
2. Yong Huang, Yi Lin, Bowen Li, Fu Zhang, Chenyue Zhan, Xin Xie, Zhuo Yao, Chongzhi Wu, Yuan Ping, Jianliang Shen. (2023) Combination therapy to overcome ferroptosis resistance by biomimetic self-assembly nano-prodrug. Asian Journal of Pharmaceutical Sciences, (100844). [PMID:37915761]
3. Yao Liu, Zhichao He, Heng Liang, Minzhen Han, Jinxingyi Wang, Qian Liu, Yanping Guan. (2023) A high-throughput UHPLC-MS/MS method for the determination of eight anti-tumor drugs in plasma. ANALYTICAL BIOCHEMISTRY, 676 (115230). [PMID:37429484]
4. Fangjun Chen, Wenda Chen, Zhenxin Wang, Yingfei Peng, Beili Wang, Baishen Pan, Wei Guo. (2023) Development and clinical application of a liquid chromatography-tandem mass spectrometry-based assay to quantify eight tyrosine kinase inhibitors in human plasma. Journal of Mass Spectrometry and Advances in the Clinical Lab, 29 (2). [PMID:37234251]
5. Zhenzhen Pan, Qiufang Chen, Xiulan Zheng, Kai Wang, Yalei Duan, Kang Xiao, Zhirong Jia, Xuansheng Ding. (2023) JuBei Oral Liquid Induces Mitochondria-Mediated Apoptosis in NSCLC Cells. OncoTargets and Therapy, [PMID:32821122]
6. Jiabin Zhou, Yuhan Liu, Jun Chen, Nanxiang Xiong, Dongye Yi. (2023) Kaempferol suppresses glioma progression and synergistically enhances the antitumor activity of gefitinib by inhibiting the EGFR/SRC/STAT3 signaling pathway. DRUG DEVELOPMENT RESEARCH, 84 (3): (582-600). [PMID:36852868]
7. Yin Xiaoting, Ma Suzhen, Li Mengyuan, Lu Shuaifei, Zhang Changjing, Liu Hui, Li Caiyin, Su Pan, Bai Ming, Li Yucheng. (2023) Study on the hepatotoxicity and potential mechanism of gefitinib based on CYP450 in mice and AML12 cells. JOURNAL OF PHARMACY AND PHARMACOLOGY, 75 (3): (407-414). [PMID:36656101]
8. Hao Chi, Sheng Tian, Xiu Li, Yuchu Chen, Qiumin Xu, Qixiao Wang, Wenwan Shi, Michael Adu-Frimpong, Shanshan Tong. (2023) Construction of lipid raft-coupled agarose gels as bioaffinity chromatography materials and validation with tropomyosin-related kinase A-targeted drugs. JOURNAL OF CHROMATOGRAPHY A, 1691 (463803). [PMID:36731332]
9. Jianbo Lin, Rujie Zheng, Liping Huang, Yuanrong Tu, Xu Li, Jianfeng Chen. (2022) Folic acid-mediated MSNs@Ag@Geb multifunctional nanocomposite heterogeneous platform for combined therapy of non-small cell lung cancer. COLLOIDS AND SURFACES B-BIOINTERFACES, 217 (112639). [PMID:35759894]
10. Yulin Jiang, Jing Wang, Juehan Wang, Yi Zhuang, Lin Qi, Ganjun Feng, Li Zhang. (2022) Fabrication of novel PNIPAM@GO microspheres loaded with dual drugs featuring on-demand drug release capability. JOURNAL OF APPLIED POLYMER SCIENCE, 139 (27): (e52444). [PMID:]
11. Pan Zhenzhen, Wang Kai, Wang Xiniao, Jia Zhirong, Yang Yuqi, Duan Yalei, Huang Lianzhan, Wu Zhuo-Xun, Zhang Jian-ye, Ding Xuansheng. (2022) Cholesterol promotes EGFR-TKIs resistance in NSCLC by inducing EGFR/Src/Erk/SP1 signaling-mediated ERRα re-expression. Molecular Cancer, 21 (1): (1-17). [PMID:35303882]
12. Yan Zhang, Pei Ma, Zhiguang Duan, Yannan Liu, Yu Mi, Daidi Fan. (2022) Ginsenoside Rh4 Suppressed Metastasis of Lung Adenocarcinoma via Inhibiting JAK2/STAT3 Signaling. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 23 (4): (2018). [PMID:35216134]
13. Yuqin Zhou, Weitong Hu, Xiangli Zhang, Yi Wang, Wenya Zhuang, Fengzhi Li, Qingyong Li. (2021) Cellular Uptake and Transport Characteristics of FL118 Derivatives in Caco-2 Cell Monolayers. CHEMICAL & PHARMACEUTICAL BULLETIN, 69 (11): (1054-1060). [PMID:34719586]

References

1. Wakeling AE, Guy SP, Woodburn JR, Ashton SE, Curry BJ, Barker AJ, Gibson KH. (2002) ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy.. Cancer Res, 62 (20): (5749-54). [PMID:12384534]
2. Gan CJ et al.. (2020) EGF receptor inhibitors comprehensively suppress hepatitis B virus by downregulation of STAT3 phosphorylation.. Biochem Biophys Rep, 22 (100763). [PMID:32322693]
3. Yan J et al.. (2020) GOLM1 upregulates expression of PD-L1 through EGFR/STAT3 pathway in hepatocellular carcinoma.. Am J Cancer Res, 10 (11): (3705-3720). [PMID:33294262]
4. Devaraj V & Bose B. (2019) Morphological State Transition Dynamics in EGF-Induced Epithelial to Mesenchymal Transition.. J Clin Med, 8 (7): [PMID:31247884]
5. Jiali Wang, Xianhai He, Zhirong Jia, Aiwen Yan, Kang Xiao, Shuo Liu, Mengjun Hou, Yaling Long & Xuansheng Ding. (2023) Shenqi Fuzheng injection restores the sensitivity to gefitinib in non-small cell lung cancer by inhibiting the IL-22/STAT3/AKT pathway. Pharmaceutical Biology, 1 (61): (33-41). [PMID:38100532]
6. Yong Huang, Yi Lin, Bowen Li, Fu Zhang, Chenyue Zhan, Xin Xie, Zhuo Yao, Chongzhi Wu, Yuan Ping, Jianliang Shen. (2023) Combination therapy to overcome ferroptosis resistance by biomimetic self-assembly nano-prodrug. Asian Journal of Pharmaceutical Sciences, (100844). [PMID:37915761]
7. Yao Liu, Zhichao He, Heng Liang, Minzhen Han, Jinxingyi Wang, Qian Liu, Yanping Guan. (2023) A high-throughput UHPLC-MS/MS method for the determination of eight anti-tumor drugs in plasma. ANALYTICAL BIOCHEMISTRY, 676 (115230). [PMID:37429484]
8. Fangjun Chen, Wenda Chen, Zhenxin Wang, Yingfei Peng, Beili Wang, Baishen Pan, Wei Guo. (2023) Development and clinical application of a liquid chromatography-tandem mass spectrometry-based assay to quantify eight tyrosine kinase inhibitors in human plasma. Journal of Mass Spectrometry and Advances in the Clinical Lab, 29 (2). [PMID:37234251]
9. Zhenzhen Pan, Qiufang Chen, Xiulan Zheng, Kai Wang, Yalei Duan, Kang Xiao, Zhirong Jia, Xuansheng Ding. (2023) JuBei Oral Liquid Induces Mitochondria-Mediated Apoptosis in NSCLC Cells. OncoTargets and Therapy, [PMID:32821122]
10. Jiabin Zhou, Yuhan Liu, Jun Chen, Nanxiang Xiong, Dongye Yi. (2023) Kaempferol suppresses glioma progression and synergistically enhances the antitumor activity of gefitinib by inhibiting the EGFR/SRC/STAT3 signaling pathway. DRUG DEVELOPMENT RESEARCH, 84 (3): (582-600). [PMID:36852868]
11. Yin Xiaoting, Ma Suzhen, Li Mengyuan, Lu Shuaifei, Zhang Changjing, Liu Hui, Li Caiyin, Su Pan, Bai Ming, Li Yucheng. (2023) Study on the hepatotoxicity and potential mechanism of gefitinib based on CYP450 in mice and AML12 cells. JOURNAL OF PHARMACY AND PHARMACOLOGY, 75 (3): (407-414). [PMID:36656101]
12. Hao Chi, Sheng Tian, Xiu Li, Yuchu Chen, Qiumin Xu, Qixiao Wang, Wenwan Shi, Michael Adu-Frimpong, Shanshan Tong. (2023) Construction of lipid raft-coupled agarose gels as bioaffinity chromatography materials and validation with tropomyosin-related kinase A-targeted drugs. JOURNAL OF CHROMATOGRAPHY A, 1691 (463803). [PMID:36731332]
13. Jianbo Lin, Rujie Zheng, Liping Huang, Yuanrong Tu, Xu Li, Jianfeng Chen. (2022) Folic acid-mediated MSNs@Ag@Geb multifunctional nanocomposite heterogeneous platform for combined therapy of non-small cell lung cancer. COLLOIDS AND SURFACES B-BIOINTERFACES, 217 (112639). [PMID:35759894]
14. Yulin Jiang, Jing Wang, Juehan Wang, Yi Zhuang, Lin Qi, Ganjun Feng, Li Zhang. (2022) Fabrication of novel PNIPAM@GO microspheres loaded with dual drugs featuring on-demand drug release capability. JOURNAL OF APPLIED POLYMER SCIENCE, 139 (27): (e52444). [PMID:]
15. Pan Zhenzhen, Wang Kai, Wang Xiniao, Jia Zhirong, Yang Yuqi, Duan Yalei, Huang Lianzhan, Wu Zhuo-Xun, Zhang Jian-ye, Ding Xuansheng. (2022) Cholesterol promotes EGFR-TKIs resistance in NSCLC by inducing EGFR/Src/Erk/SP1 signaling-mediated ERRα re-expression. Molecular Cancer, 21 (1): (1-17). [PMID:35303882]
16. Yan Zhang, Pei Ma, Zhiguang Duan, Yannan Liu, Yu Mi, Daidi Fan. (2022) Ginsenoside Rh4 Suppressed Metastasis of Lung Adenocarcinoma via Inhibiting JAK2/STAT3 Signaling. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 23 (4): (2018). [PMID:35216134]
17. Yuqin Zhou, Weitong Hu, Xiangli Zhang, Yi Wang, Wenya Zhuang, Fengzhi Li, Qingyong Li. (2021) Cellular Uptake and Transport Characteristics of FL118 Derivatives in Caco-2 Cell Monolayers. CHEMICAL & PHARMACEUTICAL BULLETIN, 69 (11): (1054-1060). [PMID:34719586]

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