Dual inhibitor of the Rho GTPases Rac (IC50 = 103 nM) and Cdc42 (IC50 = 78 nM).1 It inhibits breast cancer cell migration, viability, and mammosphere formation. MBQ-167 induced polarity loss resulting in 95% cell rounding and detachment from the substratum in metastatic MDA-MB-231 cells and was active in GFP-HER2-BM, MDA-MB-468, and Hs578t breast cancer cells as well as Mia-PaCa-2 pancreatic cancer cells, SKOV3 ovarian cancer cells, AGS and NCI-N87 gastric cancer cells, and SH-SY5Y neuroblastoma cells. Non-cancerous mammary epithelial MCF10A and epithelial breast cancer MCF-7 cells were resistant to MBQ-167. MBQ-167 inhibited viability and induced apoptosis in gefitinib and lapatinib resistant SKBR3 breast cancer cells.2 MBQ-167 inhibited triple negative breast cancer tumor growth and lung metastasis in a mouse model.3 Active in vivo.
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