1. Cell Cycle/DNA Damage
    Epigenetics
  2. HDAC
  3. Citarinostat

Citarinostat (Synonyms: ACY241)

Cat. No.: HY-15994 Purity: 99.02%
Handling Instructions

Citarinostat (ACY241) is a second generation potent, orally active and high-selective HDAC6 inhibitor with an IC50 of 2.6 nM (IC50s of 35 nM, 45 nM, 46 nM and 137 nM for HDAC1, HDAC2, HDAC3 and HDAC8, respectively). Citarinostat has anticancer effects.

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Citarinostat Chemical Structure

Citarinostat Chemical Structure

CAS No. : 1316215-12-9

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10 mM * 1 mL in DMSO USD 154 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Citarinostat (ACY241) is a second generation potent, orally active and high-selective HDAC6 inhibitor with an IC50 of 2.6 nM (IC50s of 35 nM, 45 nM, 46 nM and 137 nM for HDAC1, HDAC2, HDAC3 and HDAC8, respectively). Citarinostat has anticancer effects[1].

IC50 & Target[1]

HDAC6

2.6 nM (IC50)

HDAC1

35 nM (IC50)

HDAC2

45 nM (IC50)

HDAC3

46 nM (IC50)

HDAC8

137 nM (IC50)

HDAC7

7300 nM (IC50)

In Vitro

Citarinostat (ACY241; 0-3 μM; 24 hours; A2780 cells) treatment with 300 nM results in increased hyperacetylation of α-tubulin, consistent with inhibition of the tubulin deacetylase HDAC6. In contrast, hyperacetylation of histone H3, a target of Class I HDACs, is only observed at doses above 1 μM. Low exposures of Citarinostat result in selective inhibition of HDAC6, while higher exposures lead to inhibition of Class I HDAC isozymes[1].
The single agent viability IC50 of Citarinostat (ACY241) ranged from 4.6-6.1 μM in A2780 and TOV-21G ovarian cancer and MDA-MD-231 breast cancer cells. Consistent with the viability assay, single agent Citarinostat modestly reduces proliferation at doses up to 3 μM without inducing apoptosis, while 10 μM of Citarinostat causes significant induction of apoptosis and completely suppresses proliferation[1].

Western Blot Analysis[1]

Cell Line: A2780 cells
Concentration: 0 μM, 0.1 μM, 0.3 μM, 0.5μM, 1 μM, 3 μM
Incubation Time: 24 hours
Result: Resulted in increased hyperacetylation of α-tubulin, consistent with inhibition of the tubulin deacetylase HDAC6. In contrast, hyperacetylation of histone H3, a target of Class I HDACs, was only observed at doses above 1 μM.
In Vivo

Citarinostat (ACY241; 50 mg/kg; intraperitoneal injection; once daily for five days, followed by two days off; for 3 weeks; female athymic nude mice) significantly suppresses tumor growth in combination with NSC 125973[1].

Animal Model: Female athymic nude mice (7-week-old) injected with TOV-21G cells[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; once daily for five days, followed by two days off; for 3 weeks
Result: Combination treatment with NSC 125973 resulted in significantly suppression of tumor growth.
Clinical Trial
Molecular Weight

467.95

Formula

C₂₄H₂₆ClN₅O₃

CAS No.

1316215-12-9

SMILES

O=C(C1=CN=C(N(C2=CC=CC=C2Cl)C3=CC=CC=C3)N=C1)NCCCCCCC(NO)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (64.11 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1370 mL 10.6849 mL 21.3698 mL
5 mM 0.4274 mL 2.1370 mL 4.2740 mL
10 mM 0.2137 mL 1.0685 mL 2.1370 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.02%

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Keywords:

CitarinostatACY241ACY 241ACY-241HDACHistone deacetylasesHDAC6anticanceranti-proliferationα-tubulincombinationmultiple. myelomaInhibitorinhibitorinhibit

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