BRAFV600E/ABL2-IN-1

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 (BRAF^V600E 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.