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].

BIEGi-1 (25 nM, 12 h) effectively disrupts the interaction between EGFR and Rheb in PC9 cells (EGFR-mutant)^[1].
BIEGi-1 (25 nM, 12 h) robustly inhibits EGFR kinase activity (reduces p-Y1068-EGFR) and mTORC1 activation (reduces p-T389-S6K1) in EGFR-mutant PC9 and HCC827 cells^[1].
BIEGi-1 (0.01-10000 nM, 72 h) exerts strong antiproliferative effects on PC9 and HCC827 cells, with IC₅₀ values of 17 nM and 20 nM, respectively^[1].
BIEGi-1 (200 nM, 24 h) inhibits mTORC1 activation induced by lysosome-localized LAMP2-V5-EGFR-TKD (WT and KD) in serum-starved HEK-293T cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

615.72

C₃₆H₃₇N₇O₃

1429497-30-2

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

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• [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.  [Content Brief]