FR-167356 is a potent, orally active and selective vacuolar ATPase inhibitor with IC50 values of 170, 220, 370, and 1200 nM for osteoclast plasma membranes, macrophage microsomes, renal brush border membranes, and liver lysosomal membranes, respectively. FR-167356 inhibits bone resorption and ovariectomy-induced bone loss.
FR-167356 (200 mg/kg; p.o.; daily, for 10 days; male C57BL/6 mice with B16-F10 xenografts) inhibits tumor growth and reduces MMP9 expression[1].
FR-167356 (200 mg/kg; p.o.; daily, for 10 days; male C57BL/6 mice with B16-F10 xenografts) reduces bone metastasis compared to untreated group[1].
References:
[1]. Nishisho T, et, al. The a3 isoform vacuolar type H⁺-ATPase promotes distant metastasis in the mouse B16 melanoma cells. Mol Cancer Res. 2011 Jul;9(7):845-55.
[2]. Niikura K, et, al. A vacuolar ATPase inhibitor, FR167356, prevents bone resorption in ovariectomized rats with high potency and specificity: potential for clinical application. J Bone Miner Res. 2005 Sep;20(9):1579-88.