Gefitinib hydrochloride

SKU: orb1909577

Description

Gefitinib hydrochloride is a potent and selective oral EGFR tyrosine kinase inhibitor. It is widely used in oncology research to study its antitumor effects, including the inhibition of EGF-driven cell proliferation, induction of autophagy, and modulation of inflammation and fibrosis in both cellular and animal models.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 184475-55-6
• MW: 483.36
• Purity: 99.80% (May vary between batches)
• Formula: C₂₂H₂₅Cl₂FN₄O₃
• SMILES: Cl.FC1=CC=C(C=C1Cl)NC=2N=CN=C3C=C(OC)C(OCCCN4CCOCC4)=CC32
• Target: EGFR
• Solubility: DMSO:< 0.1 mg/mL (insoluble);H2O:4 mg/mL (8.28 mM)

Bioactivity

• Target IC50:
  GLC82 cells:2 μM|non-transformed cells:20 nM|Calu3 (cells):2 μM
• In Vivo:
  Gefitinib hydrochloride (150 mg/kg, orally) in combination with metformin significantly inhibited the growth of tumor xenografts formed by subcutaneous transplantation of H1299 or CALU-3 GEF-R cells in nude mice. In rats treated with radiation therapy, Gefitinib hydrochloride exacerbated the inflammatory response in the lungs, including the infiltration of inflammatory cells and the increase of pro-inflammatory factors, whereas Gefitinib hydrochloride served to slow down the fibrotic remodeling of the lungs by inhibiting the proliferation of lung fibroblasts.
• In Vitro:
  Gefitinib hydrochloride (0.01-0.1 mM) increased phosphotyrosine loading of the receptor by inducing EGFRvIII dimerization, enhanced ERK signaling, and stimulated cell proliferation and anchorage-independent growth, especially upon prolonged exposure of EGFRvIII-expressing cells. In contrast, Gefitinib hydrochloride (1-2 mM) significantly reduced phosphotyrosine loading of EGFRvIII and inhibited EGFRvIII-mediated proliferation and anchorage-independent growth. Gefitinib hydrochloride inhibited monolayer growth of non-transformed cells driven by EGF with an IC50 of 20 nM. Gefitinib hydrochloride also inhibited the proliferation of CALU-3 and GLC82 cells with an IC50 of 2 μM.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ZD1839 hydrochloride, ZD-1839 hydrochloride, EGFR

Compound Identifiers

PubChem CID

19077490