| Identification | Back Directory | [Name]
Gefitinib-d6 | [CAS]
1228664-49-0 | [Synonyms]
Gefitinib-d6
[2H6]-Gefitinib
Hexadeuterated gefitinib | [Molecular Formula]
C22H24ClFN4O3 | [MDL Number]
MFCD21363632 | [MOL File]
1228664-49-0.mol | [Molecular Weight]
446.91 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. | [storage]
Store at -20°C | [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.
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