Belinostat

Belinostat is an inhibitor of class I histone deacetylases (HDACs, IC50s = 0.041, 0.125, 0.03, and 0.216 µM for HDAC1, -2, -3, and -8, respectively) and class II HDACs (IC50s = 0.115, 0.082, 0.067, and 0.128 µM for HDAC4, -6, -7, and -9, respectively). It inhibits HDAC activity in HeLa cell lysates (IC50 = 0.027 µM) and the proliferation of A2780 ovarian, HCT116 colon, Calu-3 lung, and Hs 852.T melanoma cells (IC50s = 0.2, 0.2, 0.66, and 3.37 µM, respectively). It reduces tumor growth in an A2780 mouse xenograft model when administered at doses of 10, 20, and 40 mg/kg. Formulations containing belinostat have been used in the treatment of relapsed or refractory peripheral T cell lymphoma.Formal Name: (2E)-N-hydroxy-3-[3-[(phenylamino)sulfonyl]phenyl]-2-propenamide. CAS Number: 866323-14-0. Synonyms: PXD 101, PX 105684. Molecular Formula: C15H14N2O4S. Formula Weight: 318.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml, Ethanol: 25 mg/ml. lambdamax: 224, 270 nm. SMILES: O=S(NC1=CC=CC=C1)(C2=CC(/C=C/C(NO)=O)=CC=C2)=O. InChi Code: 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+. InChi Key: NCNRHFGMJRPRSK-MDZDMXLPSA-N.