EGFR/BRAFV600E-IN-1

EGFR/BRAFV600E-IN-1 (Compound 23) is a potent EGFR and BRAFV600E dual inhibitor with IC50s of 0.08 and 0.15 µM, respectively. EGFR/BRAFV600E-IN-1 induces apoptosis and cell cycle arrest in both pre-G1 and G2/M phases. EGFR/BRAFV600E-IN-1 exhibits antiproliferative activity againist A-549, MCF-7, Panc-1, HT-29 with IC50s of 1.2, 0.79, 1.3, and 1.23 µM, respectively[1].

Product Specifications

CAS Number

[2492429-45-3]

UNSPSC

12352005

Target

Apoptosis; EGFR; Raf

Type

Reference compound

Related Pathways

Apoptosis; JAK/STAT Signaling; MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/egfr-brafv600e-in-1.html

Solubility

10 mM in DMSO

Smiles

O=C1N(CCC2=CC=C(N3CCOCC3)C=C2)CC(N4C1=C(C)C5=C4C=CC(Cl)=C5)=O

Molecular Formula

C24H24ClN3O3

Molecular Weight

437.92

References & Citations

[1]Lamya H Al-Wahaibi, et al. Design and synthesis of novel 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivatives as antiproliferative EGFR and BRAF V600E dual inhibitors. Bioorg Chem. 2020 Nov;104:104260.