FR-167356

Names

[ CAS No. ]:
174185-16-1

[ Name ]:
FR-167356

[Synonym ]:
unii-xf02b1hc8r

Biological Activity

[Description]:

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[1].

[Related Catalog]:

Research Areas >> Cancer
Research Areas >> Metabolic Disease
Signaling Pathways >> Membrane Transporter/Ion Channel >> Proton Pump

[In Vivo]

FR-167356 (200 mg/kg; 口服; 每天, 持续 10 天; 具有 B16-F10 异种移植物的雄性 C57BL/6 小鼠) 抑制肿瘤生长并降低 MMP9 表达[1]。 FR-167356 (200 mg/kg; 口服; 每天, 持续 10 天; 具有 B16-F10 异种移植物的雄性 C57BL/6 小鼠) 与未治疗组相比减少骨转移[1]。 Animal Model: male C57BL/6 mice with B16-F10 xenografts[1] Dosage: 200 mg/kg Administration: Oral administration; daily, for 10 days Result: Reduced the expression of MMP9 and reduced bone metastasis.

[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.  

Chemical & Physical Properties

[ Density]:
1.385 g/cm3

[ Boiling Point ]:
422.714ºC at 760 mmHg

[ Molecular Formula ]:
C19H17Cl2NO3

[ Molecular Weight ]:
378.24900

[ Flash Point ]:
209.45ºC

[ Exact Mass ]:
377.05900

[ PSA ]:
65.96000

[ LogP ]:
5.91170


Related Compounds