EGFR Inhibitor

SKU: orb1221162

Description

EGFR inhibitor is a cell permeable and selective inhibitor of EGFR kinase (IC50: 21 nM) and blocks receptor autophosphorylation in cells.

Research Area

Pharmacology & Drug Discovery; Cell Biology

Key Properties

• CAS Number: 879127-07-8
• MW: 413.4
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₈F₃N₅O
• SMILES: FC(F)(F)c1cccc(Nc2cc(Nc3cccc(NC(=O)C4CC4)c3)ncn2)c1
• Target: EGFR
• Solubility: DMSO: 25 mg/mL;Ethanol: 10 mg/mL

Bioactivity

• In Vitro:
  EGFR-IN-12 (EGFR inhibitor 324674; 0-2 μM; 48 hours; HT29 and SW480 cells) treatment efficiently induces apoptosis at lower concentrations. EGFR-IN-12 (EGFR inhibitor 324674; 0-3 μM; 3 hours; HT29 and SW480 cells) treatment inhibits EGFR activation and the downstream AKT signaling pathway in a dose-dependent manner. EGFR-IN-12 (EGFR inhibitor 324674) inhibits HT29 and SW480 cell proliferation with with IC50s of 1.96 μM and 1.04 μM, respectively. Pretreatment of cells with EGFR-IN-12 (compound 1; 10 μM) results in complete inhibition of wild-type receptor autophosphorylation in U-2OS cells. And the T766M mutant receptor is completely resistant to inhibition by EGFR-IN-12. Apoptosis Analysis Cell line: HT29 and SW480 cells. Concentration: 0 μM, 1 μM, 2 μM. Incubation time: 48 hours. Result: Induced apoptosis in HT29 cells and SW480 cells. Western blot analysis. Cell line: HT29 and SW480 cells. Concentration: 0 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM Incubation time: 3 hours. Result: Inhibited EGFR activation and the downstream AKT signaling pathway in a dose-dependent manner.

Storage & Handling

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

Quick Database Links

Gene Symbol

EGFR