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Cat. No. Name Size Price Add Cart
KI0028Belinostat10 mg$200
Belinostat50 mg$640
Belinostat100 mg$1040
Belinostat200 mg$1800

Chemical Characteristic

Product NameBelinostat
SynonymsPXD101
CAS No.414864-00-9
Molecular Weight 318.35
FormulaC15H14N2O4S
Chemical Name2-Propenamide, N-hydroxy-3-[3-[(phenylamino)sulfonyl]phenyl]-
SmilesC(=O)(/C=C/c1cc(ccc1)S(=O)(=O)Nc1ccccc1)NO
Chemical Structure

Biological activities

Belinostat is a novel hydroxamate-type inhibitor of histone deacetylase activity. Belinostat inhibits histone deacetylase activity in HeLa cell extracts with an IC50 of 27 nM. Belinostat induces a concentration-dependent (0.2-5 µM) increase in acetylation of histone H4 in tumor cell lines. After removal of belinostat, acetylation is maintained for 30 minutes but markedly reduced after incubation in drug-free medium for 1 hour and has returned to basal levels by 3 hours. There is a clear concentration-dependent increase in levels of acetylated histone H4 in A2780 cells treated for 3 hours with belinostat. Belinostat induces apoptosis as determined by measurement of PARP cleavage after drug incubation for 24 hours. Belinostat induces expression of the cyclin-dependent kinase inhibitor p21(Cip1/WAF1) in HCT116 colon tumor cells. [1] Incubation with belinostat down-regulates thymidylate synthase expression in HCT116 cells.[2] In vitro proliferation assays demonstrates that belinostat potently inhibits the growth of prostate cancer cell lines. Belinostat induces G2/M arrest and increased the percentage of cells with subG1 DNA content, thus confirming the growth-inhibitory and cytotoxic effects of belinostat. Belinostat also increases the expression of p21 and decreased the expression of potentially oncogenic proteins (mutant p53 and ERG).[3] Belinostat at a dose of 10 mg/kg/day significantly produces growth delay in xenografts of A2780.[1] In xenografted mice, belinostat in combination with irinotecan dramatically suppresses tumor growth without causing additive toxicity.[4]

Protocols

Belinostat is prepared as a 50 mg/mL stock in belinostat vehicle (pH∼9.4) .[1]

References

[1] Qian X, et al. Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies. Mol Cancer Ther. 2006, 5(8): 2086-2095.
[2] Tumber A, et al. The histone deacetylase inhibitor PXD101 synergises with 5-fluorouracil to inhibit colon cancer cell growth in vitro and in vivo. Cancer Chemother Pharmacol. 2007, 60(2): 275-283.
[3] Qian X, et al. Activity of the histone deacetylase inhibitor belinostat (PXD101) in preclinical models of prostate cancer. Int J Cancer. 2008, 122(6):1400-1410.
[4] Na YS, et al. The histone deacetylase inhibitor PXD101 increases the efficacy of irinotecan in in vitro and in vivo colon cancer models. Cancer Chemother Pharmacol. 2011, 68(2): 389-398.

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