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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- Formule: C22H16N4OS
- Masse moléculaire:384.45
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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BRafV600E 43 nM (IC50) |
EGFR 61 nM (IC50) |
EGFR/BRAFV600E-IN-4 (0.01-100 μM) has broad-spectrum anti-proliferative activity with GI50 values ranging from 1.66 to >100 μM[1].
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%[1].
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A-549, Panc-1, HT-29, MCF-7
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Concentration:1.56, 3.125, 6.25, 12.5, 25, 50, 100 nM
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Incubation Time:48 h
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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.
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Cell Line:A-549
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Concentration:24 nM
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Incubation Time:24 h
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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.
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Cell Line:A-549
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Concentration:24 nM
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Incubation Time:24 h
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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.
Chemical Information
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Masse moléculaire 384.45
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Formule C22H16N4OS
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SMILES
C1(SCC2=CC=CC=C2)=NN=C(C3=CC=C4NC(C5=CC=CC=C5)=NC4=C3)O1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR/BRAFV600E-IN-4 Related Classifications
HY-173164 Related Classifications
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