BI-4020

BI-4020 is a fourth-generation, orally active, and non-covalent EGFR tyrosine kinase inhibitor. 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[1].

Product Specifications

CAS Number

[2664214-60-0]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

EGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bi-4020.html

Purity

99.30

Solubility

1M HCl : 100 mg/mL (ultrasonic; adjust pH to 1 with HCl) |DMSO : 250 mg/mL (ultrasonic)

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

Molecular Formula

C30H38N8O2

Molecular Weight

542.68

Precautions

H302, H315, H319, H335

References & Citations

[1]Engelhardt H, et al. Start selective and rigidify: The discovery path towards a next generation of EGFR tyrosine kinase inhibitors. J Med Chem. 2019 Nov 5.