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EGFR/BRAF-IN-1

EGFR/BRAF-IN-1 (compound 21), a 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivative, is a potent EGFR/BRAF inhibitor with an IC50 of 45 nM for BRAFV600E. EGFR/BRAF-IN-1 inhibits cancer cell proliferation (GI50=35 nM) . EGFR/BRAF-IN-1 shows good antioxidant activity[1].

Product Specifications

CAS Number

[2906174-89-6]

UNSPSC

12352005

Target

EGFR; Raf

Type

Reference compound

Related Pathways

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-braf-in-1.html

Solubility

10 mM in DMSO

Smiles

CCOCC1=C2C(N(CC(N2C3=CC=C(C=C31)Cl)=O)CCC4=CC=C(C=C4)N5CCOCC5)=O

Molecular Formula

C26H28ClN3O4

Molecular Weight

481.97

References & Citations

[1]Hesham A M Gomaa, et al.Optimization and SAR investigation of novel 2,3-dihydropyrazino[1,2-a]indole-1,4-dione derivatives as EGFR and BRAF V600E dual inhibitors with potent antiproliferative and antioxidant activities. Bioorg Chem. 2022 Jan 19;120:105616.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

B-Raf; EGFR/ErbB1/HER1

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