BRAFV600E/ABL2-IN-1
BRAFV600E/ABL2-IN-1 is a BRAFV600E (IC50 = 0.088 μM)/ABL2 (IC50 = 0.3 μM) dual inhibitor. BRAFV600E/ABL2-IN-1 can diminish P-glycoprotein expression. BRAFV600E/ABL2-IN-1 effectively inhibits p-CrkL (Abl2 signaling) and p-ERK1/2 (BRAFV600E pathway) in A375-R melanoma cells. BRAFV600E/ABL2-IN-1 causes cell cycle arrest. BRAFV600E/ABL2-IN-1 significantly increases the percentage of late apoptotic cells. BRAFV600E/ABL2-IN-1 can be used for the study of melanoma.
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- Formule: C24H20BrClN4O3S
- Masse moléculaire:559.86
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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BRafV600E 0.088 μM (IC50) |
BRAFV600E/ABL2-IN-1 (Compound 8h) (0.01-100 μM, 48 h) exhibits the best activity towards SK-MEL5 cells at the melanoma panel, with a GI50 of 0.54 μM, demonstrating marked cytostatic activity against melanoma (SK-MEL-5; TGI = 19.95 μM) and colon cancer (HT29; TGI = 26.30 μM)[1].
BRAFV600E/ABL2-IN-1 (0.125-1 μM, 72 h) significantly downregulates P-gp expression in SK-MEL-5 cells[1].
BRAFV600E/ABL2-IN-1 (0.4-100 μM) demonstrates IC50 values of 6.888 μg/mL (~12.3 μM) in A375 cells (BRAFV600E mutant) and 11.242 μg/mL (~20.1 μM) in A375-R cells (vemurafenib-resistant), and 28.776 μM in WI-38 cells[1].
BRAFV600E/ABL2-IN-1 significantly reduces the phosphorylation levels of p-CrkL (downstream of ABL2) and p-ERK1/2 (downstream of BRAF), while total protein remains unchanged. p-CrkL decreases by 67.7%, and p-ERK1/2 decreases by 63.0% in A375- R cells[1].
BRAFV600E/ABL2-IN-1 (0.54 μM, 48 h) inhibits cell proliferation in SK-MEL-5 cells by inducing G1 phase arrest and apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SK-MEL-5 cells
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Concentration:0.125 μM, 0.25 μM, 0.5 μM, 1 μM
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Incubation Time:72 h
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Result:Showed approximately 67.4 % downregulation of P-gp expression in SK-MEL-5 cells.
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Cell Line:SK-MEL-5 cells
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Concentration:0.54 μM
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Incubation Time:48 h
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Result:Caused G0-G1 phase arrest (58.12% vs. control 44.63%), and reduced S and G2/M phases.
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Cell Line:SK-MEL-5 cells
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Concentration:0.54 μM
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Incubation Time:48 h
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Result:Increased early apoptosis (25.61% vs. control 0.33%) and late apoptosis (13.89% vs. control 0.15%).
Chemical Information
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Masse moléculaire 559.86
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Formule C24H20BrClN4O3S
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SMILES
O=C(N/N=C(C1=CC=C(Br)C=C1)\C)CN2C(C3=CC=C(S(=O)(C)=O)C=C3)=NC4=CC(Cl)=CC=C24
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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)
BRAFV600E/ABL2-IN-1 Related Classifications
HY-178382 Related Classifications
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