Gefitinib hydrochloride NEW
Price | $33 | $47 |
Package | 50mg | 100mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-07 |
Product Details
Product Name: Gefitinib hydrochloride | CAS No.: 184475-55-6 |
Supply Ability: 10g | Release date: 2024/11/07 |
Product Introduction
Bioactivity
名稱 | Gefitinib hydrochloride |
描述 | Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent and orally active EGFR tyrosine kinase inhibitor (EGFR-TKI) (IC 50 = 33 nM) that selectively inhibits EGF-stimulated tumor cell growth (IC 50 = 54 nM) and blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Additionally, it induces autophagy, demonstrating antitumor activity [1] [2]. |
體外活性 | Gefitinib, at concentrations ranging from 0.01 to 0.1 mM, enhances phosphotyrosine levels, ERK signaling, and promotes proliferation and anchorage-independent growth in EGFRvIII-expressing cells, likely through EGFRvIII dimerization after prolonged exposure. Conversely, at higher concentrations (1-2 mM), gefitinib significantly reduces phosphotyrosine levels, proliferation, and anchorage-independent growth mediated by EGFRvIII. Additionally, gefitinib (ZD1839) effectively inhibits the growth of monolayers of EGF-driven, untransformed cells with an IC50 of 20 nM, and similarly impedes CALU-3 and GLC82 cell proliferation, with an IC50 of 2 μM. |
體內(nèi)活性 | Gefitinib (150 mg/kg, p.o.), in combination with Metformin, significantly reduces tumor growth in nude mice implanted with H1299 or CALU-3 GEF-R cells as subcutaneous xenografts [3]. In irradiated rats, Gefitinib exacerbates lung inflammation by increasing inflammatory cell infiltration and pro-inflammatory cytokine expression, but mitigates fibrotic lung remodeling by inhibiting lung fibroblast proliferation [4]. |
存儲(chǔ)條件 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
關(guān)鍵字 | Gefitinib hydrochloride | Gefitinib Hydrochloride |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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