Gefitinib-d6 Chemical Properties

storage temp. 

Store at -20°C

solubility 

DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 0.3 mg/ml

form 

A solid

color 

White to off-white

Gefitinib-d6 Usage And Synthesis

Description

Gefitinib-d₆ is intended for use as an internal standard for the quantification of gefitinib by GC- or LC-MS. Gefitinib is an EGFR inhibitor (IC₅₀s = 0.023-0.079 μM). It inhibits colony formation of GEO colon, ZR-75-1 and MCF-10A breast, and OVCAR-3 ovarian cancer cell lines in soft agar assays (IC₅₀s = 0.2-0.4 μM). Gefitinib (0.1 to 1 μM) induces apoptosis and inhibits EGFR autophosphorylation in the same cells. In vivo, gefitinib (1.25, 2.5, and 5 mg/kg) reduces tumor volume and increases survival in a GEO mouse xenograft model. Formulations containing gefitinib have been used in the treatment of non-small cell lung cancer (NSCLC).

Uses

Gefitinib-d6 is the labeled version of Gefitinib (G304000), which is an antineoplastic.

References

[1] JOHN MENDELSOHN  Jose B. The EGF receptor family as targets for cancer therapy[J]. Oncogene, 2000, 19 56: 6550-6565. DOI: 10.1038/sj.onc.1204082
[2] F CIARDIELLO. 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.[J]. Clinical Cancer Research, 2000, 6 5: 2053-2063.

Gefitinib-d6(1228664-49-0)Related Product Information

• 4-(3-Chloropropyl)morpholine
• 4,4'-(propane-1,3-diyl)bismorpholine
• Gefitinib N-Oxide
• 4-Defluoro-4-hydroxy Gefitinib
• Gefitinib
• 3-Hydroxy-4-methoxybenzonitrile
• 3-Chloro-4-fluoroaniline
• 2-Amino-4-methoxy-5-(3-morpholinopropoxy)benzonitrile
• 7-Methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4(3H)-one
• 2-aMino-4-Methoxy-5-(3-Morpholinopropoxy)benzaMide
• 6-Hydroxy-7-methoxy-3,4-dihydroquinazolin-4-one
• 3,4-Dichloroaniline
• N-(3-chloro-4-fluorophenyl)-7 -methoxy-6-(3-morpholinopropoxy)-N-(3-morpholinopropyl)quinazolin-4-amine
• Gefitinib 3,4-Difluoro Impurity HCl
• 6,7-Dimethoxy-3,4-dihydroquinazoline-4-one
• 4-(3-Chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-ol
• 3-Deschloro-4-Desfluoro-4-Chloro-3-Fluorogefitinib
• 4-(3-Chloro-4-fluorophenylamino)-7-methoxyquinazolin-6-yl acetate