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Merck

SML1657

Gefitinib

≥98% (HPLC), powder, EGFR TK inhibitor

Synonyme(s) :

N-(3-Chloro-4-fluoro-phenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine, ZD1839

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A propos de cet article

Formule empirique (notation de Hill) :
C22H24ClFN4O3
Numéro CAS:
Poids moléculaire :
446.90
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Service technique
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Nom du produit

Gefitinib, ≥98% (HPLC)

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear

storage temp.

room temp

SMILES string

COC(C=C(N=CN=C1NC2=CC(Cl)=C(F)C=C2)C1=C3)=C3OCCCN4CCOCC4

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

Gene Information

human ... EGFR(1956)

Application

Gefitinib has been used :
  • To study its effective use in endometrial cancer therapy
  • Cell proliferation, cell cycle and apoptosis assays
  • Cell viability assay and colony formation assay

Biochem/physiol Actions

Gefitinib is a selective epidermal growth factor receptor tyrosine kinase (EGFR TK) inhibitor. Gefitinib has antineoplastic activity, and has been approved for the treatment on non-small cell lung cancer (NSCLC).
Gefitinib has a higher affinity for ATP (adenosine triphosphate) binding site in the EGFR tyrosine kinase domain than ATP. Hence, gefitinib is known to inhibit the progression of endometrial cancer.


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Danger

Hazard Classifications

Acute Tox. 4 Oral - Aquatic Chronic 1 - Carc. 2 - Eye Dam. 1 - Repr. 1B - Skin Irrit. 2 - STOT RE 2 Oral

Classe de stockage

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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Baodan Yu et al.
Molecular medicine reports, 24(4) (2021-08-17)
Tyrosine kinase inhibitors, such as gefitinib, are currently widely used as targeted therapeutics for non‑small cell lung cancer (NSCLC). Although drug resistance has become a major obstacle to successful treatment, mechanisms underlying resistance to gefitinib remain unclear. Therefore, the present
Brian S Bogdanowicz et al.
Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners, 23(3), 203-214 (2016-02-26)
Purpose The approval history, pharmacology, pharmacokinetics, clinical trials, efficacy, dosing recommendations, drug interactions, safety, place in therapy, and economic considerations of gefitinib are reviewed. Summary Lung cancer is one of the most commonly diagnosed cancers and is the leading cause
Hisanori Isomura et al.
Cancer science, 112(4), 1614-1623 (2021-01-29)
We previously reported that ROR1 is a crucial downstream gene for the TTF-1/NKX2-1 lineage-survival oncogene in lung adenocarcinoma, while others have found altered expression of ROR1 in multiple cancer types. Accumulated evidence therefore indicates ROR1 as an attractive molecular target