ACY-241

ACY-241 is an inhibitor of histone deacetylase 6 (HDAC6, IC50 = 2.6 nM). It is selective for HDAC6 over HDAC1-3, HDAC7, and HDAC9 (IC50s = 35, 45, 46, 7,300, and 137 nM, respectively), as well as HDAC4, HDAC5, and HDAC9 (IC50 = >20,000 nM for all). It reduces proliferation of A2780, TOV-21G, and MDA-MB-231 cells when used at a concentration of 3 µM and completely inhibits it and induces apoptosis at a concentration of 10 µM. ACY-241, when used in combination with paclitaxel (Cay-10461), inhibits proliferation in MiaPaCa-2, TOV-21G, and T47D cells. It also reduces tumor growth in a MiaPaCa-2 mouse xenograft model when administered at a dose of 50 mg/kg in combination with paclitaxel. ACY-241, in combination with the somatostatin receptor agonist pasireotide (Cay-24092), reduces hepatorenal cystogenesis in a rat model of polycystic liver disease.Formal Name: 2-[(2-chlorophenyl)phenylamino]-N-[7-(hydroxyamino)-7-oxoheptyl]-5-pyrimidinecarboxamide. CAS Number: 1316215-12-9. Synonyms: Citarinostat. Molecular Formula: C24H26ClN5O3. Formula Weight: 468.0. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/ml, DMSO: 5 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 284 nm. SMILES: ClC1=C(N(C2=CC=CC=C2)C3=NC=C(C(NCCCCCCC(NO)=O)=O)C=N3)C=CC=C1. InChi Code: InChI=1S/C24H26ClN5O3/c25-20-12-7-8-13-21(20)30(19-10-4-3-5-11-19)24-27-16-18(17-28-24)23(32)26-15-9-2-1-6-14-22(31)29-33/h3-5,7-8,10-13,16-17,33H,1-2,6,9,14-15H2,(H,26,32)(H,29,31). InChi Key: VLIUIBXPEDFJRF-UHFFFAOYSA-N.