PXD-101
PXD-101 Basic information
- Product Name:
- PXD-101
- Synonyms:
-
- (2E)-N-Hydroxy-3-[3-[(phenylamino)sulfonyl]phenyl]-2-propenamide
- 2-PropenaMide, N-hydroxy-3-[3-[(phenylaMino)sulfonyl]phenyl]-, (2E)-
- Belista
- PXD101;PX105684;PXD-101;PXD 101;PX-105684
- Belinostat（E）
- 3-[3-(phenylsulfamoyl)phenyl]prop-2-enehydroxamic acid
- (e)-n-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
- Belinostat Impurity
- CAS:
- 866323-14-0
- MF:
- C15H14N2O4S
- MW:
- 318.35
- Mol File:
- 866323-14-0.mol
PXD-101 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
- InChI
- InChI=1S/C15H14N2O4S/c18-15(16-19)10-9-12-5-4-8-14(11-12)22(20,21)17-13-6-2-1-3-7-13/h1-11,17,19H,(H,16,18)/b10-9+
- InChIKey
- NCNRHFGMJRPRSK-MDZDMXLPSA-N
- SMILES
- C(NO)(=O)/C=C/C1=CC=CC(S(NC2=CC=CC=C2)(=O)=O)=C1
PXD-101 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
PXD-101Supplier
- Tel
- +86-21-20908456
- sales@BioChemBest.com
- Tel
- 17366295326
- puxinpharma_2017@126.com
- Tel
- 400-6009262 16621234537
- chenyj@titansci.com
- Tel
- 18030648795
- sales@cdforestchem.com
- Tel
- 021-58950125
- info@chemexpress.com