| Description | FR-167356 is a specific inhibitor of a3 isoform vacuolar type H⁺-ATPase with IC50s of 170 nM, 370 nM and 220 nM for osteoclast plasma membranes, renal brush border membranes and macrophage microsomes. FR-167356 reduces bone metastasis of B16-F10 cells. |
| In vivo | In male C57BL/6 mice with B16-F10 xenografts, FR-167356 (200 mg/kg) reduces bone metastasis, inhibits tumor growth, and reduces the expression of MMP9[1]. |
| Synonyms | FR167356, FR 167356 |
| molecular weight | 378.25 |
| Molecular formula | C19H17Cl2NO3 |
| CAS | 174185-16-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 22.5 mg/mL (7.08 mM) |
| 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. Morissette G, et al. Intracellular sequestration of amiodarone: role of vacuolar ATPase and macroautophagic transition of the resulting vacuolar cytopathology. Br J Pharmacol. 2009 Aug;157(8):1531-40. 3. Morissette G, Lodge R, Marceau F. Intense pseudotransport of a cationic drug mediated by vacuolar ATPase: procainamide-induced autophagic cell vacuolization. Toxicol Appl Pharmacol. 2008 May 1;228(3):364-77. 4. Niikura K, Takeshita N, Takano M. 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. Epub 2005 May 31. |