EGFR-IN-134

EGFR-IN-134 (compound 3f), a triazolo[3,4-a]isoquinoline derivative, is a potent EGFR inhibitor with an IC50 of 0.023 µM. EGFR-IN-134 induces apoptosis and necrosis. EGFR-IN-134 initiates cell cycle arrest at the G2/M and pre-G1 phases, downregulates anti-apoptotic protein Bcl2 and upregulates pro-apoptotic proteins: p53, Bax, and caspases 3, 8, and 9. EGFR-IN-134 shows antiproliferative and anticancer activity[1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; Bcl-2 Family; Caspase; EGFR; MDM-2/p53; Necroptosis

Type

Reference compound

Related Pathways

Apoptosis; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/egfr-in-134.html

Smiles

O=C(C1=NN(C2=CC=C([N+]([O-])=O)C=C2)C3N1CCC4=C3C=C(OC)C(OC)=C4)/C=C/C5=CN(C6=CC=CC=C6)N=C5C7=CC=CC=C7

Molecular Formula

C36H30N6O5

Molecular Weight

626.66

References & Citations

[1]Nesma Abdelaal, et al. Design, in silico studies and biological evaluation of novel chalcones tethered triazolo[3,4-a]isoquinoline as EGFR inhibitors targeting resistance in non-small cell lung cancer. Sci Rep. 2024 Nov 4;14 (1) :26647.