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Belinostat (PXD101) is an inhibitor of hydroxamic acid-type histone deacetylase (HDAC, IC50 of 27 nM in HeLa cell extracts),and with antineoplastic activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $40 | In Stock | |
10 mg | $63 | In Stock | |
25 mg | $98 | In Stock | |
50 mg | $147 | In Stock | |
100 mg | $217 | In Stock | |
200 mg | $323 | In Stock | |
500 mg | $546 | In Stock | |
1 mL x 10 mM (in DMSO) | $57 | In Stock |
Description | Belinostat (PXD101) is an inhibitor of hydroxamic acid-type histone deacetylase (HDAC, IC50 of 27 nM in HeLa cell extracts),and with antineoplastic activity. |
Targets&IC50 | HDAC6:82 nM , HDAC:27 nM (Hela cell) |
In vitro | Belinostat is a novel hydroxamate-type inhibitor of histone deacetylase activity that inhibits histone deacetylase activity in HeLa cell extracts with an IC(50) of 27 nM and induces a concentration-dependent (0.2-5 micro M) increase in acetylation of histone H4 in tumor cell lines.Belinostat is cytotoxic in vitro in a number of tumor cell lines with IC(50)s in the range 0.2-3.4 micro M as determined by a clonogenic assay and induces apoptosis. |
In vivo | Treatment of nude mice bearing human ovarian and colon tumor xenografts with PXD101 (10-40 mg/kg/day i.p.) for 7 days results in a significant, dose-dependent growth delay without obvious signs of toxicity. Growth delay is also observed in xenografts of cisplatin-resistant ovarian tumor cells. A significant increase in acetylation of H4 is detected in blood and tumor tissues 3 hours after treatment. These findings suggest that PXD101 has potential as a novel antitumor agent. |
Alias | PXD-101, PXD101, PX105684 |
Molecular Weight | 318.35 |
Formula | C15H14N2O4S |
Cas No. | 866323-14-0 |
Smiles | S(NC1=CC=CC=C1)(=O)(=O)C2=CC(/C=C/C(NO)=O)=CC=C2 |
Relative Density. | 1.427 g/cm3 (Predicted) |
Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 135 mg/mL (424.068 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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