EGFR-IN-181

EGFR-IN-181 is an orally active, potent, brain-penetrant EGFRL858R/T790M/C797S triple mutations inhibitor (IC50 = 1.32 nM) . EGFR-IN-181 can inhibit EGFR phosphorylation (p-EGFR) and phosphorylation of its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK) . EGFR-IN-181 can induce apoptosis and cause G2 phase arrest. EGFR-IN-181 can be used for the study of non-small cell lung cancer (NSCLC) and brain metastases[1].

Product Specifications

UNSPSC

12352005

Target

Akt; Apoptosis; EGFR; PERK

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; JAK/STAT Signaling; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK

Field of Research

Cancer; Neurological Disease

Smiles

CP(C)(C1=CC=CC=C1NC2=NC(NC3=CC4=C(N(CCN(C)C)C=C4)C=C3)=NC=C2Cl)=O

Molecular Formula

C24H28ClN6OP

Molecular Weight

482.95

References & Citations

[1]Zhao L, et al. Discovery of a brain-penetrant fourth-generation EGFR inhibitor to overcome the human triple (L858R/T790 M/C797S) mutation. Eur J Med Chem. 2025 Oct 14;302 (Pt 1) :118256.