A potent FAK inhibitor
PND1186 is a potent reversible focal adhesion kinase (FAK) inhibitor with an IC50 value of 1.5 nM against the recombinant enzyme and 100 nM in breast carcinoma cells.1 It promotes 4T1 breast carcinoma and ID8 ovarian carcinoma cell apoptosis when grown in anchorage-independent 3D cultures but had limited efficacy in 2D cultures. It is orally bioavailable, reducing orthotopic breast cancer tumor growth in mouse models.2
1.Tanjoni, I., Walsh, C., Uryu, S., et al.PND-1186 FAK inhibitor selectively promotes tumor cell apoptosis in three-dimensional environmentsCancer Biol. Ther.9(10)764-777(2010) 2.Walsh, C., Tanjoni, I., Uryu, S., et al.Oral delivery of PND-1186 FAK inhibitor decreases tumor growth and spontaneous breast to lung metastasis in pre-clinical modelsCancer Biol. Ther.9(10)778-790(2010)
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