EGFR-IN-176

EGFR-IN-176 is an orally active and ATP-competitive EGFR mutant inhibitor (particularly C797S-mediated EGFR triple mutant) . EGFR-IN-176 effectively inhibits subsequent AKT signaling and induces apoptosis in Ba/F3 and PC-9 cells expressing EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S. EGFR-IN-176 selectively inhibits EGFR signaling in cell lines harboring EGFR triple mutation and shows no inhibitory effect against A431 cells that express wild-type EGFR. EGFR-IN-176 can effectively inhibit the enzymatic activity of ALK (IC50 [1].

Product Specifications

CAS Number

[2754394-10-8]

UNSPSC

12352005

Target

Akt; Anaplastic lymphoma kinase (ALK) ; Apoptosis; EGFR

Related Pathways

Apoptosis; JAK/STAT Signaling; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

O=S(N(C)C1=C2N=CC=NC2=CC=C1NC3=C4C=CNC4=NC(NC5=C(OC)C=C(N6CCC(CC6)N7CCN(CC7)C)C(CC)=C5)=N3)(C)=O

Molecular Formula

C35H45N11O3S

Molecular Weight

699.87

References & Citations

[1]Wu Z, et al. Discovery of Potent and Selective Pyrrolo[2,3-d]pyrimidine Derivatives as Fourth-Generation EGFR Inhibitors Targeting Triple Mutation. J Med Chem. 2025 Sep 25;68 (18) :19205-19228.