SMB00950
O-Desmethyl gefitinib
≥95%
Synonim(y):
4-[(3-Chloro-4-fluorophenyl)amino]-6-[3-(4-morpholinyl)propoxy]-7-quinazolinol, O-Desmethylgefitinib
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About This Item
Wzór empiryczny (zapis Hilla):
C21H22ClFN4O3
Numer CAS:
Masa cząsteczkowa:
432.88
Kod UNSPSC:
12352205
NACRES:
NA.77
Polecane produkty
pochodzenie biologiczne
synthetic
Poziom jakości
klasa czystości
research grade
Próba
≥95%
Postać
solid
metody
HPLC: suitable
kolor
light yellow to yellow
temp. przechowywania
−20°C
InChI
1S/C21H22ClFN4O3/c22-16-10-14(2-3-17(16)23)26-21-15-11-20(19(28)12-18(15)24-13-25-21)30-7-1-4-27-5-8-29-9-6-27/h2-3,10-13,28H,1,4-9H2,(H,24,25,26)
Klucz InChI
IFMMYZUUCFPEHR-UHFFFAOYSA-N
Opis ogólny
O-Desmethyl Gefitinib, a key metabolite of the anticancer drug gefitinib, belongs to the quinazoline family and is present in human plasma. Its formation is facilitated by the cytochrome P450 isoform CYP2D6. This compound exhibits significant activity as an inhibitor of tyrosine residue phosphorylation in EGFR, with an IC50 of 36 nM in subcellular assays. While its effectiveness is comparable to that of gefitinib, O-Desmethyl Gefitinib shows slightly reduced activity in whole-cell assays, with an IC50 of 760, in contrast to gefitinib′s 49 nM. Studies conducted in LoVo tumor mouse xenograft models have revealed that the tumor concentration of O-Desmethyl Gefitinib is notably lower than that of gefitinib, without causing a substantial reduction in tumor growth. Remarkably, increased plasma concentrations of O-Desmethyl Gefitinib in individuals homozygous for CYP2D6 do not lead to an increase in adverse effects. O-Desmethyl Gefitinib holds promise for biochemical and biomedical research, providing potential insights into drug development and cancer treatment.
Zastosowanie
O-Desmethyl Gefitinib finds application in metabolomics and drug discovery research, particularly in the investigation of cancer and tumor management.
Działania biochem./fizjol.
O-Desmethyl gefitinib is generated by the removal of a methyl group from gefitinib during the body′s metabolic processing of this compound within the body.
Cechy i korzyści
- High quality compound suitable for multiple research applications
- Compatible with a wide variety of chromatographic and spectrometry techniques
Inne uwagi
For additional information on our range of Biochemicals, please complete this form.
This product is intended for research purposes only, and it is not meant for human consumption.
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Hasło ostrzegawcze
Warning
Zwroty wskazujące rodzaj zagrożenia
Zwroty wskazujące środki ostrożności
Klasyfikacja zagrożeń
Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
Organy docelowe
Respiratory system
Kod klasy składowania
11 - Combustible Solids
Klasa zagrożenia wodnego (WGK)
WGK 3
Temperatura zapłonu (°F)
Not applicable
Temperatura zapłonu (°C)
Not applicable
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Masz już ten produkt?
Dokumenty związane z niedawno zakupionymi produktami zostały zamieszczone w Bibliotece dokumentów.
D McKillop et al.
Xenobiotica; the fate of foreign compounds in biological systems, 34(10), 901-915 (2005-03-15)
The pharmacokinetics of gefitinib and its metabolites in rat and dog were investigated in preclinical studies conducted to support the safety evaluation and clinical development of gefitinib, the first EGFR tyrosine kinase inhibitor approved for the treatment of non-small-cell lung
Minimal contribution of desmethyl-gefitinib, the major human plasma metabolite of gefitinib, to epidermal growth factor receptor (EGFR)-mediated tumour growth inhibition
McKillop et al.
Xenobiotica, 36, 29-39 (2006)
Hiroyuki Kobayashi et al.
Medical oncology (Northwood, London, England), 33(6), 57-57 (2016-05-08)
We investigated the effects of polymorphisms in CYP2D6, ABCB1, and ABCG2 and the side effects induced by gefitinib on the pharmacokinetics of O-desmethyl gefitinib, the active metabolite of gefitinib. On day 14 after beginning therapy with gefitinib, plasma concentrations of
Metabolic disposition of gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, in rat, dog and man
McKillop et al.
Xenobiotica,
34, 917-934 (2004)
Ping Fang et al.
Drug design, development and therapy, 11, 1283-1290 (2017-05-04)
Cytochrome P450 2D6 (CYP2D6), a member of the CYP450 enzyme super family, is a polymorphic enzyme that metabolizes ~25% of therapeutic drugs. CYP2D6 exhibits significant genetic polymorphisms which might cause adverse effects and therapeutic failures of some drugs. The purpose
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