EGFR/BRAFV600E-IN-7 

EGFR/BRAFV600E-IN-7 is a dual EGFR and BRAF^V600E kinase inhibitor with human IC₅₀ values of 0.12 μM, 0.80 μM, 1.20 μM for EGFR and 0.05 μM, 0.22 μM, 0.78 μM for BRAF^V600E.EGFR/BRAFV600E-IN-7 interacts with key ATP-binding site residues of EGFR and BRAF^V600E, including hydrogen bonding with EGFR Met769 and BRAF^V600E Cys532.EGFR/BRAFV600E-IN-7 induces apoptosis via caspase-3/8/9 activation, modulates Bax and Bcl-2 expression, scavenges free radicals, and exhibits antiproliferative activity against human cancer cell lines.EGFR/BRAFV600E-IN-7 displays drug-likeness with no PAINS/Brenk structural alerts per in silico predictions.EGFR/BRAFV600E-IN-7 can be used for the research of colon cancer, pancreatic cancer, lung cancer, breast cancer^[1].

EGFR/BRAFV600E-IN-7 (compound 7c) (50 μM; 4 days) exhibits no cytotoxicity toward human mammary gland epithelial MCF-10A cells, preserving 88% of cell viability^[1].
EGFR/BRAF^V600E-IN-7 exhibits potent antiproliferative activity against human colon cancer HT-29 (IC₅₀=8 μM), human breast cancer MCF-7 (IC₅₀=4 μM), human lung cancer A-549 (IC₅₀=6 μM), and human pancreatic cancer Panc-1 (IC₅₀=7 μM) cells, with an average GI₅₀ of 6 μM^[1].
EGFR/BRAFV600E-IN-7 activates both intrinsic and extrinsic apoptotic pathways in human breast cancer MCF-7 cells, inducing an 8-fold increase in caspase-3, 15-fold increase in caspase-8, and 21-fold increase in caspase-9 protein levels relative to untreated controls^[1].
EGFR/BRAFV600E-IN-7 modulates apoptotic protein expression in human breast cancer MCF-7 cells, inducing a 27-fold increase in pro-apoptotic Bax levels and a 6-fold reduction in anti-apoptotic Bcl-2 levels relative to untreated controls^[1].
EGFR/BRAFV600E-IN-7 (10-100 μM) exhibits potent antioxidant activity, with DPPH radical scavenging rates of 90.8% at 100 μM, 80.5% at 50 μM, and 68.4% at 10 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

507.56

C₂₈H₂₁N₅O₃S

3120155-78-1

O=C(NC1=CC=C(C2=CC(C3=CC=C(OC)C=C3)=C(C#N)C(N2)=O)C=C1)CSC4=NC5=CC=CC=C5N4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Al-Wahaibi L H, et al. Design, synthesis, apoptotic antiproliferative, and antioxidant activities of a new series of 2-mercaptobenzimidazole/3-cyanopyridin-2-one hybrids as dual EGFR/BRAFV600E inhibitors[J]. Bioorganic Chemistry, 2025: 109329.