1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK MAPK/ERK Pathway Apoptosis
  2. EGFR Raf Apoptosis
  3. EGFR/BRAFV600E-IN-4

EGFR/BRAFV600E-IN-4 (Compound 10f) is a dual EGFR and BRAFV600E inhibitor with IC50 values of 61 nM and 43 nM, respectively. EGFR/BRAFV600E-IN-4 arrests cell cycle, induces apoptosis in both early and late stages and inhibits cancer cells growth in vitro, and has a broad anticancer activity.

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EGFR/BRAFV600E-IN-4 Chemical Structure

EGFR/BRAFV600E-IN-4 Chemical Structure

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Description

EGFR/BRAFV600E-IN-4 (Compound 10f) is a dual EGFR and BRAFV600E inhibitor with IC50 values of 61 nM and 43 nM, respectively. EGFR/BRAFV600E-IN-4 arrests cell cycle, induces apoptosis in both early and late stages and inhibits cancer cells growth in vitro, and has a broad anticancer activity[1].

IC50 & Target[1]

BRafV600E

43 nM (IC50)

EGFR

61 nM (IC50)

In Vitro

EGFR/BRAFV600E-IN-4 (0.01-100 μM) has broad-spectrum anti-proliferative activity with GI50 values ranging from 1.66 to >100 μM. EGFR/BRAFV600E-IN-4 (1.56-100 nM, 48 h) inhibits cells growth of A-549, Panc-1, HT-29, MCF-7 with IC50 values ranging from 24 nM to 27 nM, but exhibits a safety profile versus MCF-10 A cells with cell viability of 91%. EGFR/BRAFV600E-IN-4 (24 nM, 24 h) arrests cells at the G0/G1 phase and block the transition from the G1 phase to the S and G2/M phases, induces apoptosis in both early and late stages.

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

Cell Proliferation Assay[1]

Cell Line: A-549, Panc-1, HT-29, MCF-7
Concentration: 1.56, 3.125, 6.25, 12.5, 25, 50, 100 nM
Incubation Time: 48 h
Result: Displayed significant anti-proliferative activity on A-549, Panc-1, HT-29, MCF-7with IC50 values of 24 nM, 25 nM, 25 nM, 27 nM, respectively.

Cell Cycle Analysis[1]

Cell Line: A-549
Concentration: 24 nM
Incubation Time: 24 h
Result: Revealed an increase in the percentage of accumulation of cells in the G0-G1 phase by 64.18 %.
The percentages of cell accumulation in the S and G2/M phases decreased from 31.44 % and 13.27 % in untreated cells to 24.05 % and 11.77 %, respectively.

Apoptosis Analysis[1]

Cell Line: A-549
Concentration: 24 nM
Incubation Time: 24 h
Result: Increased cells that entered both early and late apoptosis by 19.44 % and 11.13 %, respectively, while cells that got necrosis were only 3.3 %, indicating anti-proliferative activity.
Molecular Weight

384.45

Formula

C22H16N4OS

SMILES

C1(SCC2=CC=CC=C2)=NN=C(C3=CC=C4NC(C5=CC=CC=C5)=NC4=C3)O1

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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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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Product Name:
EGFR/BRAFV600E-IN-4
Cat. No.:
HY-173164
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