EGFR-IN-12

SKU: orb1302033

Description

EGFR-IN-12 is a potent and selective cell-permeable inhibitor of EGFR kinase, demonstrating an IC50 of 21 nM. It effectively suppresses EGFR autophosphorylation in cellular assays and is a valuable tool for investigating EGFR-driven signaling pathways in both in vitro and in vivo cancer research models.

Research Area

Cardiovascular Research, Cell Biology, Signal Transduction

Key Properties

• CAS Number: 879127-07-8
• MW: 413.4
• Purity: 99.76% (May vary between batches)
• Formula: C₂₁H₁₈F₃N₅O
• SMILES: FC(F)(F)c1cccc(Nc2cc(Nc3cccc(NC(=O)C4CC4)c3)ncn2)c1
• Target: Apoptosis,EGFR
• Solubility: Ethanol:10 mg/mL (24.19 mM);DMSO:50 mg/mL (120.95 mM)

Bioactivity

• Target IC50:
  EGFR (L861Q):4 nM (cell free)|EGFR (L858R):63 nM (cell free)|EGFR:21 nM (cell free)|HER4:7640 nM
• In Vitro:
  EGFR Inhibitor possesses an enzymatic IC50= 21 nM against EGFR kinase in vitro and blocks receptor autophosphorylation in cells. EGFR Inhibitor also potently inhibits two EGFR mutants associated with clinical response to gefitinib: L858R (IC50: 63 nM) and L861Q (IC50: 4 nM), but displays much weaker activity against Her 4 (IC50: 7640 nM).

Storage & Handling

• Storage: 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

4,6-disubstituted, AKT, anti-proliferation, antitumor, autophosphorylation, Apoptosis, inhibit, kinases, Inhibitor, HER1, Epidermal growth factor receptor, EGFR (L861Q), EGFR (L858R), EGFR IN 12, EGFRIN12, EGFR-IN-12, EGFR Inhibitor, EGFR, ErbB-1, pyrimidine, Tyrosine

Compound Identifiers

PubChem CID

9549299