BI-4732

BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC) [1].

Product Specifications

CAS Number

[2769715-68-4]

UNSPSC

12352005

Target

Akt; EGFR; ERK; Ribosomal S6 Kinase (RSK)

Type

Reference compound

Related Pathways

JAK/STAT Signaling; MAPK/ERK Pathway; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/bi-4732.html

Purity

99.30

Solubility

DMSO : 2 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CC1=C(C=NN2C3=NC(N4C[C@@H]5OC[C@H]4C5)=C6C(N(C)C(N7C[C@@H](CCC8)N8CC7)=N6)=C3)C2=CC(C9=C(OC)C=CN=C9)=N1

Molecular Formula

C32H36N10O2

Molecular Weight

592.69

References & Citations

[1]Eun Ji Lee, et al. Discovery of a novel potent EGFR inhibitor against EGFR activating mutations and on-target resistance in NSCLC. Clin Cancer Res. 2024 Feb 8.