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
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, protect from light)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
Frequently Asked Questions
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