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866323-14-0

Supplier Related Products Identification Chemical Properties Hazard Information

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Identification

Name
PXD-101
CAS
866323-14-0
Synonyms
Belista
Belinostat(E)
PXD101;PX105684;PXD-101;PXD 101;PX-105684
(2E)-N-Hydroxy-3-[3-[(phenylamino)sulfonyl]phenyl]-2-propenamide
2-PropenaMide, N-hydroxy-3-[3-[(phenylaMino)sulfonyl]phenyl]-, (2E)-
Molecular Formula
C15H14N2O4S
MOL File
866323-14-0.mol
Molecular Weight
318.348

Chemical Properties

Melting point 
172 °C(Solv: ethyl acetate (141-78-6))
density 
1.427±0.06 g/cm3(Predicted)
storage temp. 
Sealed in dry,Room Temperature
pka
8.27±0.10(Predicted)

Hazard Information

Enzyme inhibitor
This synthetic epigenetic modulator (FW = 318.35 g/mol; CAS 866323-14- 0), also known as PXD101 and the IUPAC name, (2E) -N-hydroxy-3-[3- (phenylsulfamoyl) phenyl]prop-2-enamide, inhibits histone deacetylase (IC50 = 27 nM) and induces a concentration-dependent increase (over the 0.2–5 μM range) in histone H4 acetylation and alters expression of genes located on DNA associated with its parent histone octamer. A simple and sensitive high-performance liquid chromatography ultraviolet method has been developed for the quantification of PXD101 in human plasma. In Rhesus monkeys, belinostat is cleared rapidly from plasma with a half-life of 1.0 h, a mean residence time of 0.47 h, and a clearance of 425 mL/min/m2 . CSF drug exposure is <1% of plasma drug exposure and <10% of free (non-protein bound) plasma drug exposure. The DNA-methylation inhibitor decitabine and histone-deacetylase inhibitor belinostat increases the efficacy of chemotherapeutic agents in tumors that acquired drug resistance due to DNA methylation and gene silencing.
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