184475-35-2
184475-35-2
Chemical Structure
Gefitinib
Synonym(s): ZD1839
- CAS No.: 184475-35-2
- Formula:C22H24ClFN4O3
- Molecular Weight:446.90
IUPAC Name: N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholinopropoxy)quinazolin-4-amine
InChIKey: XGALLCVXEZPNRQ-UHFFFAOYSA-N
SMILES: ClC1=C(C=CC(NC2=NC=NC3=C2C=C(C(OC)=C3)OCCCN4CCOCC4)=C1)F
Biological Activity: Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer [1][2][5].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
Gefitinib | 99.99% | Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer . | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Gefitinib (GMP) | Gefitinib (ZD1839) (GMP) is Gefitinib (HY-50895) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Gefitinib is a potent, selective and orally active EGFR tyrosine kinase inhibitor. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Gefitinib (Standard) | 99.94% | Gefitinib (Standard) is the analytical standard of Gefitinib. This product is intended for research and analytical applications. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer . | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Gefitinib-d8 | 98.42% | Gefitinib-d8 (ZD1839-d8) is a deuterium labeled Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Gefitinib-d3 | 98.39% | Gefitinib-d3 (ZD1839-d3) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Gefitinib-d6 | 98.0% | Gefitinib-d6 is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
O-Desmethyl gefitinib | 99.40% | O-Desmethyl gefitinib is an active metabolite of Gefitinib in human plasma. The formation of O-desmethyl gefitinib is dependent on CYP2D6 activity. O-desmethyl gefitinib inhibits EGFR with an IC50 of 36 nM in subcellular assays. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Gefitinib N-oxide | Gefitinib N-oxide is the N-oxide derivative of Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Larotinib | 99.50% | Larotinib is a potent broad-spectrum and orally active tyrosine kinase inhibitor (TKI) with EGFR as the main target with an IC50 of 0.6 nM. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
EGFR ligand-11 | EGFR ligand-11 is a target protein ligand for EGFR and can be used to synthesize PROTAC MS154 (HY-141640). | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
NRC-2694 | 99.84% | NRC-2694 is an epidermal growth factor receptor (EGFR) antagonist with anti-cancer and anti-proliferative properties. NRC-2694 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Gefitinib hydrochloride (Standard) | 99.46% | Gefitinib (hydrochloride) (Standard) is the analytical standard of Gefitinib (hydrochloride). This product is intended for research and analytical applications. Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
Gefitinib dihydrochloride | Gefitinib (ZD 1839) dihydrochloride is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib dihydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib dihydrochloride also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer . | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
EGFR ligand-15 | EGFR ligand-15 is a EGFR PROTACligand. EGFR ligand-15 can be used to synthesize PROTAC EGFR degrader MS9427 (HY-147941) . | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
|
|
M387783 | M387783 is an oxidative metabolite of Gefitinib (HY-50895). M387783 is commonly used in pharmacokinetic and metabolic pathway studies. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
References
- [1]. Wakeling AE, et al. ZD1839: an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res. 2002 Oct 15;62(20):5749-54. [Content Brief]
- [2]. Pedersen MW, et al. Differential response to gefitinib of cells expressing normal EGFR and the mutant EGFRvIII. Br J Cancer. 2005 Oct 17;93(8):915-23. [Content Brief]
- [5]. Marie P Piechocki, et al. Gefitinib prevents cancer progression in mice expressing the activated rat HER2/neu. Int J Cancer. 2008 Apr 15;122(8):1722-9. [Content Brief]
