BI-4020

SKU: orb1309929

Description

BI-4020 is a potent, orally bioavailable, and non-covalent fourth-generation EGFR tyrosine kinase inhibitor. It demonstrates high activity against resistant triple (del19/T790M/C797S) and double mutants, with selectivity over wild-type EGFR and a favorable kinome/DMPK profile. This profile supports its investigation in preclinical models of non-small cell lung cancer (NSCLC) driven by EGFR mutations.

Research Area

Cardiovascular Research, Signal Transduction

Key Properties

• CAS Number: 2664214-60-0
• MW: 542.68
• Purity: 98.44%
• Formula: C₃₀H₃₈N₈O₂
• SMILES: C[C@@H]1CCCOc2c(cnn2C)-c2cc(cc(C)n2)C(=O)\N=C2/Nc3ccc(CN4CCN(C)CC4)cc3N2C1
• Target: EGFR
• Solubility: DMSO:240 mg/mL (442.25 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (9.21 mM)

Bioactivity

• Target IC50:
  EGFR (del19):1 nM|EGFR (WT):190 nM|EGFR (T790M/C797S/del19):0.2 nM
• In Vivo:
  In the human PC-9 (EGFR del19/T790M/C797S) triple mutant NSCLC xenograft model in mice, BI-4020 leads to tumor regressions.
• In Vitro:
  BI-4020 inhibits p-EGFR del19 T790M C797S (IC50: 0.6 nM) and the triple mutant EGFR (del19/T790M/C797S) variant (IC50=0.2 nM in BaF3 cell lines), as well as the double mutant EGFR (del19/T790M) and primary mutant EGFR del19 (IC50: 1 nM), with activity against EGFR wt (IC50: 190 nM), and exhibits high kinome selectivity and good DMPK properties.

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

BI4020, BI-4020, BI 4020, inhibit, EGFR (del19), EGFR (del19/T790M), EGFR (del19/T790M/C797S), EGFR, EGFR (wt), EGFRdel19, EGFRdel19 T790M, EGFRdel19 T790M C797S, EGFRWT, Epidermal growth factor receptor, ErbB-1, Inhibitor, HER1

Compound Identifiers

PubChem CID

139600318