PXD-101

Product NamePXD-101
CAS866323-14-0
MFC15H14N2O4S
MW318.35
EINECS
MOL File866323-14-0.mol

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
solubility	DMSO:64.0(Max Conc. mg/mL);201.4(Max Conc. mM)
form	powder to crystal
pka	8.27±0.10(Predicted)
color	White to Light yellow to Light orange

Safety Information

HS Code

2935.90.6000

Usage And Synthesis

Uses

Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.

Definition

ChEBI: Belinostat is a hydroxamic acid-type histone deacetylase (HDAC) inhibitor with antineoplastic activity. It has a role as an antineoplastic agent and an EC 3.5.1.98 (histone deacetylase) inhibitor. It is a hydroxamic acid, a sulfonamide and an olefinic compound.

Biological Activity

Belinost at (PX105684; PXD101) is a potent, hydroxamate class pan-selective histone deacetylases (HDACs) inhibitor (IC50: class I HDAC1/2/3/8 = 41/125/30/216 nM, class IIA HDAC4/7/9 = 115/67/128 nM, class IIB HDAC6 = 82 nM) with anti-cancer efficacy in vitro and in vivo.

in vivo

Treatment of nude mice bearing human ovarian and colon tumor xenografts with 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 mice. Growth delay is also observed for xenografts of cisplatin-resistant ovarian tumor cells. A marked increase in acetylation of H4 is detected in blood and tumor of mice 3 h after treatment with Belinostat (PXD101). The inhibition of growth of human tumor xenografts in mice, with no apparent toxicity^[1]. Belinostat (PXD101) displays single-agent antitumor activity on human A2780 ovarian cancer s.c. xenografts which is enhanced via combination therapy with Carboplatin^[2].

IC 50

HDAC6: 82 nM (IC₅₀); HDAC: 27 nM (IC₅₀, Hela cell)

References

[1] Plumb JA, et al. Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histonedeacetylase inhibitor PXD101. Mol Cancer Ther. 2003 Aug;2(8):721-8. PMID:12939461
[2] Qian X, et al. Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies. Mol Cancer Ther. 2006 Aug;5(8):2086-95. DOI:10.1158/1535-7163.MCT-06-0111
[3] Chia S, et al. Phenotype-driven precision oncology as a guide for clinical decisions one patient at a time. Nat Commun. 2017 Sep 5;8(1):435. DOI:10.1038/s41467-017-00451-5

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