Belinostat

• CAT Number: I005210
• CAS Number: 866323-14-0
• Molecular Formula: C15H14N2O4S
• Molecular Weight: 318.35
• Purity: ≥95%
• Target: pan-HDAC
• Solubility: DMSO ≥60mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL
• Storage: Store at -20C
• IC50: 27 nM
• IUPAC Name: (E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
• 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: C1=CC=C(C=C1)NS(=O)(=O)C2=CC=CC(=C2)/C=C/C(=O)NO

Belinostat（Cat No.:I005210）is a histone deacetylase (HDAC) inhibitor approved for treating relapsed or refractory peripheral T-cell lymphoma. By inhibiting HDAC enzymes, belinostat alters gene expression, leading to cell cycle arrest, differentiation, and apoptosis in cancer cells. Its mechanism of action enhances the acetylation of histones and non-histone proteins, resulting in a more open chromatin structure and increased transcription of tumor suppressor genes. Clinical trials have demonstrated its efficacy in certain hematological malignancies, and ongoing research explores its potential in combination therapies and other cancer types.

Reference

[1]. Xiaozhong Qian et al. Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies Mol Cancer Ther August 2006 5; 2086
[2]. Nicola L. Steele et al. A Phase 1 Pharmacokinetic and Pharmacodynamic Study of the Histone Deacetylase Inhibitor Belinostat in Patients with Advanced Solid Tumors Clin Cancer Res February 1, 2008 14; 804
[3]. Dizon DS, Damstrup L, Finkler NJ, Lassen U, Celano P, Glasspool R, Crowley E, Lichenstein HS, Knoblach P, Penson RT.Phase II activity of belinostat (PXD-101), carboplatin, and paclitaxel in women with previously treated ovarian cancer.Int J Gynecol Cancer. 2012 Jul;22(6):979-86.
[4]. Gravina GL, Marampon F, Giusti I, Carosa E, Di Sante S, Ricevuto E, Dolo V, Tombolini V, Jannini EA, Festuccia C.Differential effects of PXD101 (belinostat) on androgen-dependent and androgen-independent prostate cancer models.Int J Oncol. 2012 Mar;40(3):711-20.
[5]. Cashen A, Juckett M, Jumonville A, Litzow M, Flynn PJ, Eckardt J, LaPlant B, Laumann K, Erlichman C, DiPersio J.Phase II study of the histone deacetylase inhibitor belinostat (PXD101) for the treatment of myelodysplastic syndrome (MDS).Ann Hematol. 2012 Jan;91(1):33-8. Epub 2011 May 3.