| Identification | Back Directory | [Name]
Citarinostat | [CAS]
1316215-12-9 | [Synonyms]
CS-1760
HDAC-IN-2
Citarinostat
ACY-241(CITARINOSTAT)
Citarinostat (ACY-241)
Citarinostat(ACY-241,HDAC-IN-2)
ACY-241; ACY 241; ACY241; HDAC-IN-2; CITARINOSTAT.
2-[(2-Chlorophenyl)phenylamino]-N-[7-(hydroxyamino)-7-oxoheptyl]-5-pyrimidinecarboxamide
N-(6-(hydroxycarbamoyl)hexyl)-2-(N-(2-chlorophenyl)-N-phenylamino)pyrimidine-5-carboxamide
2-((2-Chlorophenyl)(phenyl)aMino)-N-(7-(hydroxyaMino)-7-oxoheptyl)pyriMidine-5-carboxaMide
5-Pyrimidinecarboxamide, 2-[(2-chlorophenyl)phenylamino]-N-[7-(hydroxyamino)-7-oxoheptyl]-
(Z)-2-((2-chlorophenyl)(phenyl)amino)-N-((Z)-7-hydroxy-7-(hydroxyimino)heptyl)pyrimidine-5-carbimidic acid
(Z)-2-((2-CHLOROPHENYL)(PHENYL)AMINO)-N-((Z)-7-HYDROXY-7-(HYDROXYIMINO)HEPTYL)PYRIMIDINE-5-CARBIMIDIC ACID;HDAC-IN-2 | [Molecular Formula]
C24H26ClN5O3 | [MDL Number]
MFCD28023593 | [MOL File]
1316215-12-9.mol | [Molecular Weight]
467.95 |
| Chemical Properties | Back Directory | [density ]
1.293±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≥23.4 mg/mL in DMSO; insoluble in H2O; ≥4.87 mg/mL in EtOH with ultrasonic | [form ]
solid | [pka]
9.47±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
ACY-241 is an inhibitor of histone deacetylase 6 (HDAC6; IC50 = 2.6 nM).1 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 (Item No. 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 (Item No. 24092), reduces hepatorenal cystogenesis in a rat model of polycystic liver disease.2 | [Uses]
Citarinostat is a HDAC inhibitor. | [storage]
Store at -20°C | [References]
[1]. quayle sn, almeciga-pinto i, tamang d, et al. selective hdac inhibition by ricolinostat (acy-1215) or acy-241 synergizes with imid? immunomodulatory drugs in multiple myeloma (mm) and mantle cell lymphoma (mcl) cells. in: proceedings of the 106th annual meeting of the american association for cancer research, 2015, philadelphia, pa. philadelphia (pa): aacr; cancer res 2015;75(15 suppl):abstract nr 5380.
[2]. huang p, almeciga-pinto i, jordan m, et al. selective hdac inhibition by acy-241 enhances the activity of paclitaxel in solid tumor models. in: proceedings of the 2015 aacr-nci-eortc international conference on molecular targets and cancer therapeutics; 2015 nov 5-9; boston, massachusetts. philadelphia (pa): aacr |
|
|