EGFR-IN-1 hydrochloride

SKU: orb1709793

Description

EGFR-IN-1 hydrochloride is an irreversible, mutant-selective EGFR inhibitor targeting the L858R/T790M variants with high potency in cellular assays. It demonstrates significant antiproliferative effects in models like H1975 and HCC827 cells, supporting its utility in oncology research for studying resistance mechanisms and targeted therapy approaches.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 2227455-78-7
• MW: 551.04
• Purity: 99.80%
• Formula: C₂₈H₃₁ClN₆O₄
• SMILES: Cl.O=C(C=C)NC1=CC=CC(=C1)N2C(=O)C=C(C=3C=NC(=NC32)NC4=CC=C(OCCN(C)C)C=C4OC)C
• Target: EGFR
• Solubility: DMSO:10 mg/mL (18.15 mM)

Bioactivity

• Target IC50:
  p-EGFR:4-9nM
• In Vivo:
  In female athymic nude mice with H1975 Tumor Xenograft, gavage administration of EGFR-IN-1 hydrochloride (30 mg/kg) significantly inhibits the tumor growth without observed loss in body weight. EGFR-IN-1 shows a >50% inhibition of phosphorylation of EGFR and a systemic exposure (AUC0-inf.) of 0.33 μM. h.
• In Vitro:
  EGFR-IN-1 is highly selective against a panel of 100 kinases and inhibits p-EGFR in H1975 and HCC827 cells with IC50s of 4 and 9 nM, respectively.

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

EGFRL858R/T790M, EGFRIN1 hydrochloride, EGFR-IN-1 Hydrochloride, EGFR IN 1 hydrochloride, EGFR (L858R/T790M)

Compound Identifiers

PubChem CID

146026038