BIEGi-1
BIEGi-1 is an EGFR inhibitor. BIEGi-1 effectively disrupts the EGFR-Rheb interaction in cells. BIEGi-1 robustly inhibits EGFR kinase activity (reduces p-Y1068-EGFR) as well as mTORC1 activation (reduces p-T389-S6K1) in EGFR-mutant cells. BIEGi-1 shows strong antiproliferative effects on EGFR-mutant PC9 and HCC827 cells with IC50 values of 17 nM and 20 nM, respectively. BIEGi-1 can be used for the study of cancers harboring EGFR mutations, such as non-small cell lung cancer (NSCLC) [1].
Product Specifications
CAS Number
[1429497-30-2]
UNSPSC
12352005
Target
EGFR; mTOR
Related Pathways
JAK/STAT Signaling; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK
Field of Research
Cancer
Smiles
O=C1N(C2=CC(NC(/C=C/C)=O)=CC=C2)C3=NC(NC4=C(C=C(N5CCN(CC5)C)C=C4)OC)=NC=C3C=C1CC6=CC=CC=C6
Molecular Formula
C36H37N7O3
Molecular Weight
615.72
References & Citations
[1]He X, et al. Lysosomal EGFR acts as a Rheb-GEF independent of its kinase activity to activate mTORC1. Cell Res. 2025 Jul;35 (7) :497-509.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
MTORC1
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