BI-4020

SKU: orb1940820

Description

BI-4020 is a fourth-generation, non-covalent, and orally active inhibitor of EGFR tyrosine kinase.(In Vitro):BI-4020 inhibits p-EGFR del19 T790M C797S ( IC50: 0.6 nM). BI-4020 inhibits not only the triple mutant EGFR (del19/T790M/C797S) variant (IC50=0.2 nM in BaF3 cell lines) but also the double mutant EGFR (del19/T790M) and primary mutant EGFR del19 (IC50: 1 nM). BI-4020 also shows activity against EGFR wt (IC50: 190 nM). BI-4020 shows high kinome selectivity and good DMPK properties.(In Vivo):In the human PC-9 (EGFR del19/T790M/C797S) triple mutant NSCLC xenograft model in mice, BI-4020 leads to tumor regressions.

Key Properties

• CAS Number: 2664214-60-0
• MW: 542.68
• Purity: >98% (HPLC)
• Formula: C₃₀H₃₈N₈O₂
• SMILES: O=C(C1=CC(C)=NC(C2=C(OCCC[C@@H](C)C3)N(C)N=C2)=C1)/N=C(N4)/N3C5=C4C=CC(CN6CCN(C)CC6)=C5
• Target: EGFR
• Solubility: In Vitro: DMSO : 250 mg/mL (460.68 mM)

Bioactivity

• In Vivo:
  BI-4020 leads to tumor regressions in the human PC-9 (EGFR del19 T790M C797S) triple mutant NSCLC xenograft model in mice.
• In Vitro:
  BI-4020 inhibits p-EGFR del19 T790M C797S with an IC50 of 0.6 nM.

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