Gefitinib

SKU: orb1225856

Description

A potent, selective, orally active EGFR inhibitor with IC50 of 23 nM; inhibits EGF-stimulated proliferation of KB cells with IC50 of 80 nM; blocks the growth of GEO colon cancer, ZR-75-1 and MCF-10A Ha-ras breast cancer, and OVCAR-3 ovarian cancer cell lines with IC50 of 0.2-0.4 uM; significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth; has been used to treat advanced (or recurrent) non-small cell lung cancer.Lung Cancer Approved(In Vitro):Gefitinib (0.01-0.1 μM, 72 h) results in increased phosphotyrosine load of the receptor, increased signalling to ERK and stimulation of proliferation and anchorage-independent growth.Gefitinib (1-2 μM, 72 h) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth.Gefitinib (0.62 μM, 24-72 h) inhibits IL-13-induced M2-like polarization of RAW 264.7 cells through the STAT6-dependent signaling pathway.Gefitinib (0.62 μM, 72 h) inhibits M2-like macrophage-promoted invasion and migration.Gefitinib (0-10 μM, 72 h) induces apoptosis (induction of BIM protein) in NSCLC Cell Lines (H3255 and HCC827 cells).Gefitinib (100 nM, 24 h) suppresses macropinocytosis and increases the cellular uptake of extracellular vesicles( EVs) in HCC827 and A549 cells.Gefitinib (1.5-60 μM, 48 h) increases inhibition of proliferation in H358R and A549R cells (Cisplatin-resistant wtEGFR NSCLC cell lines).(In Vivo):Gefitinib (Oral administration, 75 mg/kg/d, 21 days) inhibits the M2-like polarization of macrophages in LLC mice metastasis model.Gefitinib (Oral administration, 75 mg/kg for the initial week, daily for 5 consecutive days per week) eliminates phosphorylation of HER2 and HER3 and signaling through MAPK and Akt in lobular hyperplasias and carcinomas, increases MAPK activity and cytokine production in splenocytes and lymph nodes. Gefitinib (Oral gavage, 150 mg/kg, daily) enhances the anti-tumor effect of Cisplatin in H358R xenograft.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 184475-35-2
• MW: 446.9024
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₄ClFN₄O₃
• SMILES: COC1=CC2=NC=NC(NC3=CC=C(F)C(Cl)=C3)=C2C=C1OCCCN4CCOCC4
• Target: EGFR
• Solubility: DMSO: ≥ 30 mg/mL

Bioactivity

• In Vitro:
  Gefitinib (GMP) abolishes the effect of EGF-induced dedifferentiation of astrocytes into astrocyte precursor cells (APCs). Gefitinib (3 μM) can produce a subgroup of EGFR-mutant NSCLC cell lines (Gefitinib-resistant cells) that undergo cellular reprogramming, such as HCC827 cells.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ZD-1839

Quick Database Links

Gene Symbol

EGFR