HDAC Inhibitors

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PXD101

Belinostat (PXD101) is a potent hydroxamate-type inhibitor of histone deacetylase activity that is cytotoxic in vitro, which enhances the effect of cytotoxic chemotherapy and delays growth in xenograft models of ovarian and colon cancer.

Belinostat

IUPAC Name: (2E)-3-[3-(anilinosulfonyl)phenyl]-N-hydroxyacrylamide
Molecular Weight: 318,35 g/mol
Molecular Formula: C15H14N2O4S
SMILES: ONC(=O)C=Cc1cc(ccc1)S(=O)(=O)Nc2ccccc2
Canonical SMILES: C1=CC=C(C=C1)NS(=O)(=O)C2=CC=CC(=C2)C=CC(=O)NO
InChIKey Identifier: NCNRHFGMJRPRSK-MDZDMXLPSA-N
CAS Number: 414864-00-9
Melting point: n/a °C
Solubility: : soluble in DMSO
2D Molfile: Get the molfile
Synonyms: PXD101; PX105684; Belinostat

PXD101 was found to inhibit in vitro cancer cell growth at sub- to low micromolar IC50 potency, exhibited synergistic activity when used in combination with relevant chemotherapeutics, and effectively inhibited the growth of multidrug-resistant cells.

Belinostat is currently under phase I/II testing in lymphoma, ovarian cancer and other solid tumors.

References:
1) Plumb JA, Finn PW, Williams RJ, et al. Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101. Mol Cancer Ther 2(8):721728
2) Qian X, LaRochelle WJ, et al. Activity of PXD101, a histone deacetylase inhibitor, in preclinical ovarian cancer studies. Mol Cancer Ther 5(8):20862095.
3) Paoluzzi L, et al. Romidepsin and belinostat synergize the antineoplastic effect of bortezomib in mantle cell lymphoma. Clin Cancer Res. 2010 Jan 15;16(2):554-65.

HDACs


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