Belinostat (PXD101) |
Katalog-Nr.GC15962 |
Belinostat (PXD101) is a novel hydroxamate-type inhibitor of histone deacetylase (HDAC) activity in HeLa cell extracts with an IC50 of 27 nM.
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Cas No.: 414864-00-9
Sample solution is provided at 25 µL, 10mM.
Belinostat (PXD101) is a novel hydroxamate-type inhibitor of histone deacetylase (HDAC) activity in HeLa cell extracts with an IC50 of 27 nM [1].
Belinostat(1-5 μM)for 48 h caused a dose-dependent inhibition of proliferation, with the most potent inhibitory effect occurring on 5637 cells (IC50 of 1.0 μM), and the least effect occurring on RT4 cells (IC50 of 10.0 μM). T24 and J82 cell lines had an IC50 of 3.5 and 6.0 μM, respectively [2]. Belinostat inhibited the proliferation of human bladder cancer T24 cells with IC50 of 3.5μM [3].
Belinostat (10-40 mg/kg/day i.p.) daily for 7 days causes a significant dose-dependent growth delay with no obvious signs of toxicity to the colon tumor xenografts mice [1]. Gene expression analysis of belinostat-treated mice showed increased p21WAF1 gene transcript expression [3]. Belinostat monotherapy induced dose-proportional antitumor effects. When administered at 100 mg/kg, belinostat inhibited tumor size by 47% at day 15 on human ovarian cancer xenografts [4].
References:
[1]. Plumb J A, Finn P W, Williams R J, et al. Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101[J]. Molecular cancer therapeutics, 2003, 2(8): 721-728.
[2]. Buckley M T, Yoon J, Yee H, et al. The histone deacetylase inhibitor belinostat (PXD101) suppresses bladder cancer cell growth in vitro and in vivo[J]. Journal of Translational Medicine, 2007, 5(1): 1-12.
[3]. Buckley M T, Yoon J, Yee H, et al. The histone deacetylase inhibitor belinostat (PXD101) suppresses bladder cancer cell growth in vitro and in vivo[J]. Journal of Translational Medicine, 2007, 5(1): 1-12.
[4]. Qian X, LaRochelle W J, Ara G, et al. Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies[J]. Molecular cancer therapeutics, 2006, 5(8): 2086-2095.
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