1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK MAPK/ERK Pathway Apoptosis
  2. EGFR Raf Caspase Bcl-2 Family Apoptosis
  3. EGFR/BRAFV600E-IN-2

EGFR/BRAFV600E-IN-2 (compound 3g) is a potential multi-target inhibitor of EGFR, BRAFV600E, and EGFRT790M, and an inducer of apoptosis. EGFR/BRAFV600E-IN-2 can activate caspase-3, 8, and Bax, and downregulate the anti-apoptotic protein Bcl2, inducing apoptosis. EGFR/BRAF V600E-IN-2 also has antioxidant activity and DPPH free radical scavenging potency.

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EGFR/BRAFV600E-IN-2

EGFR/BRAFV600E-IN-2 Estructura química

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Descripciòn

EGFR/BRAFV600E-IN-2 (compound 3g) is a potential multi-target inhibitor of EGFR, BRAFV600E, and EGFRT790M, and an inducer of apoptosis. EGFR/BRAFV600E-IN-2 can activate caspase-3, 8, and Bax, and downregulate the anti-apoptotic protein Bcl2, inducing apoptosis. EGFR/BRAF V600E-IN-2 also has antioxidant activity and DPPH free radical scavenging potency[1].

IC50 & Target[1]

BRafV600E

 

EGFRT790M

 

Caspase-8

 

Caspase-3

 

Bcl-2

 

Bax

 

In Vitro

EGFR/BRAFV600E-IN-2 (comound 3g) effectively inhibits four human cancer cell lines: Panc-1 (pancreatic cancer cell line), MCF-7 (breast cancer cell line), HT-29 (colon cancer cell line), and A-549 (human epithelial cancer cell line), with better effective activity than Erlotinib (HY-50896)[1].
EGFR/BRAFV600E-IN-2 displays promising antioxidant activity at 10 µM, with DPPH radical scavenging of 70.6%[1].

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

Cell Viability Assay[1]

Cell Line: A-549, MCF-7, Panc-1, HT-29 cells
Concentration:
Incubation Time:
Result: Inhibited cell viability among above cancer cells, with IC50 of 24 nM (A-549), 28 nM (MCF-7), 26 nM (Panc-1), 26 nM (HT-29), respectively.
Peso molecular

406.44

Fòrmula

C25H18N4O2

SMILES

O=C1NC2=C(C=C(C)C=C2)C(N3N=NC(C(C4=CC=CC=C4)=O)=C3C5=CC=CC=C5)=C1

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Room temperature in continental US; may vary elsewhere.

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

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

Nombre del producto:
EGFR/BRAFV600E-IN-2
Cat. No.:
HY-149517
Cantidad:
MCE Japan Authorized Agent: