EGFR-IN-131

EGFR-IN-131 (compound 3a) is a potent and cross the blood-brain barrier EGFR inhibitor with an IC50 value of 272.9 nM. EGFR-IN-131 shows antiproliferative activity. EGFR-IN-131 induces apoptosis and cell cycle arrest at G0/G1 phase. EGFR-IN-131 decreases the protein expression of p-EGFR[1].

Product Specifications

UNSPSC

12352101

Target

Apoptosis; EGFR

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-131.html

Smiles

CC(C1=CC(NC2=CC3=CC=N2)=CC=C1)OCCCC(NC4=NC(C5=CC=C(C=C5)F)=C3S4)=O

Molecular Formula

C26H23FN4O2S

Molecular Weight

474.55

References & Citations

[1]Wu G, et al. Discovery of novel Macrocyclic small molecules Based on 2-Amino-4-thiazolylpyridineas selective EGFR inhibitors with high Blood-Brain barrier penetration for the treatment of glioblastoma. Bioorg Chem. 2024 Oct 23;153:107905.