Belinostat/PXD101,PX105684/

Solubility:Soluble in DMSO/PBS

Storage:-20C 2 years

Biologieal

Belinostat (PXD101) is a novel hydroxamate-type inhibitor of histone deacetylase (HDAC) activity. Belinostat inhibits HDAC activity in HeLa cell extracts with an IC50 of 27 nM. PXD101 is cytotoxic in vitro in a number of tumor cell lines with IC50s in the range 0.2-3.4 ��M as determined by a clonogenic assay and induces apoptosis. Treatment of nude mice bearing human ovarian and colon tumor xenografts with PXD101 causes a significant dose-dependent growth delay with no obvious signs of toxicity to the mice.

Reference

1. Steele NL, Plumb JA, Vidal L, Tj rnelund J, Knoblauch P, Rasmussen A, Ooi CE, Buhl-Jensen P, Brown R, Evans TR, DeBono JS. A phase 1 pharmacokinetic and pharmacodynamic study of the histone deacetylase inhibitor belinostat in patients with advanced solid tumors. Clin Cancer Res. 2008 Feb 1;14(3):804-10.

 2. Buckley MT, Yoon J, Yee H, Chiriboga L, Liebes L, Ara G, Qian X, Bajorin DF, Sun TT, Wu XR, Osman I. The histone deacetylase inhibitor belinostat (PXD101) suppresses bladder cancer cell growth in vitro and in vivo. J Transl Med. 2007 Oct 12;5:49.

3. Qian X, LaRochelle WJ, Ara G, Wu F, Petersen KD, Thougaard A, Sehested M, Lichenstein HS, Jeffers M. Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies. Mol Cancer Ther. 2006 Aug;5(8):2086-95.