信号转导通路: HDAC-HSP-Aurora >> HDAC >> HDAC YZ剂 >> Belinostat (PXD101)
http://selleck.cn/belinostat-S1085.html
技术数据:
分子量(MW): 318.35
化学式:
C15H14N2O4S
溶解度: DMSO ≥64mg/mL Water <1mg/mL Ethanol <1mg/mL
纯度: >99%
稳定性: at -20℃ 2 years
CAS号: 414864-00-9
生物活性
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.[1] PXD101 is cytotoxic in vitro in a number of tumor cell lines with IC50s in the range of 0.2-3.4 μM as determined by a clonogenic assay and induces apoptosis. [2] 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. [3,4]
参考文献
Pharmacodynamic Response and Inhibition of Growth of Human Tumor Xenografts by the Novel Histone Deacetylase Inhibitor PXD101 Paul W. Finn, Robert J. Williams, et al. Mol Cancer Ther 2003;2:721-728
A Phase 1 Pharmacokinetic and Pharmacodynamic Study of the Histone Deacetylase Inhibitor Belinostat in Patients with Advanced Solid Tumors Jane A. Plumb, Laura Vidal, et al. Clin Cancer Res 2008;14:804-810
The histone deacetylase inhibitor belinostat (PXD101) suppresses bladder cancer cell growth in vitro and in vivo Michael T Buckley,Joanne Yoon,et al. Journal of Translational Medicine 2007;5:49
Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies William J. LaRochelle, Gulshan Ara, et al. Mol Cancer Ther 2006;5:2086-2095
客户反馈数据
MDA-MB-231 Breast cancer cells were pretreated with Acetyl-H3 and H3, and then treated with the indicated concentrations of PXD101.
HDACIs That Simultaneously Inhibit HDACs 1 and 6 Showed Greater Antileukemic Activities than HDACIs that Don’t at Cmax Concentrations. THP-1 cells were treated with LBH-589, PXD101, SAHA, VPA, MS-275 and MGCD0103 at Cmax concentrations for 3 h and 24 h, respectively. The cells post 3 h treatments were washed three times with complete medium and divided into two halves. One half of the cells was resuspended in complete media and cultured for up to 24 h to determine the effects of the 3 h treatments on cell proliferation and apoptosis. The other half of the cells was used to prepare whole cell lysates. Whole cell lysates from the 3 h and 24 h treatments were extracted and subjected to Western blots probed by anti-ac-tubulin or –b-actin antibody (panels A&B), or subjected to HDAC1 enzymatic assays post IP as described in the Materials and Methods (Panels C&D). The effects of the 3 h and 24 h HDACI treatments on cell proliferation, as reflected by percent decrease of live cells relative to untreated cells (panel E), and apoptosis (panel F) were determined by flow cytometry analysis as described in the Materials and Methods.
Induction of DNA Damage and Bim Is Critical for HDACI-Induced Apoptosis in Pediatric AML Cells. THP-1 cells were treated with the HDACIs at Cmax concentrations for 3 (panel A) and 24 h (panel B), respectively. Whole cell lysates were extracted and subjected to Western blots probed by anti-p21, -c-Myc, -cH2AX, -Bim, or -b-actin antibody.
Inhibition of LSD1 activity by HDAC inhibitors. a MDA-MB-231 and MDA-MB-468 cells were exposed to indicated HDAC inhibitors for 24 h.
LSD1 and HDAC inhibitors exhibit synergistic growth inhibition. Cells were simultaneously treated with pargyline or HDAC inhibitors for 48 h.
如果需要长期保存，请于零下二十度低温保存。
禁止用于人体及ZL！
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