Citarinostat
Based on 3 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.55%
- CAS No.: 1316215-12-9
- Formula: C24H26ClN5O3
- Molecular Weight:467.95
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Citarinostat
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Biological Activity
|
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) |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| BV-173 | IC50 |
0.9 μM
Compound: Citarinostat
|
Anti-proliferative activity against human BV-173 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human BV-173 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
|
[PMID: 33576627] |
| Fibroblast | IC50 |
5.7 μM
Compound: 6
|
Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method
Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method
|
[PMID: 32615502] |
| Fibroblast | IC50 |
5.7 μM
Compound: ACY-241
|
Cytotoxicity against primary normal human fibroblast cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against primary normal human fibroblast cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
|
[PMID: 35119267] |
| Fibroblast | IC50 |
5.74 μM
Compound: ACY-241
|
Cytotoxicity against human normal fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human normal fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
|
[PMID: 34101461] |
| Fibroblast | IC50 |
7.4 μM
Compound: 6
|
Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method
Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method
|
[PMID: 32615502] |
| Fibroblast | IC50 |
7.4 μM
Compound: ACY-241
|
Cytotoxicity against human primary pooled fibroblasts cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human primary pooled fibroblasts cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
|
[PMID: 35119267] |
| Fibroblast | IC50 |
7.44 μM
Compound: ACY-241
|
Cytotoxicity against primary pooled human fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against primary pooled human fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
|
[PMID: 34101461] |
| HeLa | IC50 |
7 μM
Compound: Citarinostat
|
Anti-proliferative activity against human HeLa cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human HeLa cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
|
[PMID: 33576627] |
| HuT78 | IC50 |
1.78 μM
Compound: ACY-241
|
Cytotoxicity against human Hut78 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human Hut78 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
|
[PMID: 34101461] |
| HUVEC | IC50 |
4.86 μM
Compound: ACY-241
|
Cytotoxicity against human HUVEC cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human HUVEC cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
|
[PMID: 34101461] |
| HUVEC | IC50 |
4.9 μM
Compound: 6
|
Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method
|
[PMID: 32615502] |
| HUVEC | IC50 |
4.9 μM
Compound: ACY-241
|
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
|
[PMID: 35119267] |
| Jurkat | IC50 |
1.2 μM
Compound: Citarinostat
|
Anti-proliferative activity against human Jurkat cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human Jurkat cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
|
[PMID: 33576627] |
| L02 | IC50 |
15.2 μM
Compound: ACY-241
|
Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay
Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay
|
[PMID: 37463038] |
| MM1.S | IC50 |
1.52 μM
Compound: 6
|
Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method
|
[PMID: 32615502] |
| MM1.S | IC50 |
1.6 μM
Compound: Citarinostat
|
Anti-proliferative activity against human MM1.S cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human MM1.S cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
|
[PMID: 33576627] |
| MM1.S | IC50 |
1.61 μM
Compound: ACY-241
|
Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
|
[PMID: 35119267] |
| MM1.S | IC50 |
2 μM
Compound: ACY-241
|
Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human MM1.S cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay
|
[PMID: 37463038] |
| MOLM-13 | IC50 |
13.5 μM
Compound: Citarinostat
|
Anti-proliferative activity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
|
[PMID: 33576627] |
| MOLT-4 | IC50 |
1.72 μM
Compound: ACY-241
|
Cytotoxicity against human MOLT-4 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human MOLT-4 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
|
[PMID: 34101461] |
| MV4-11 | IC50 |
1.2 μM
Compound: Citarinostat
|
Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
|
[PMID: 33576627] |
| MV4-11 | IC50 |
1.24 μM
Compound: 6
|
Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method
|
[PMID: 32615502] |
| MV4-11 | IC50 |
1.24 μM
Compound: ACY-241
|
Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
|
[PMID: 35119267] |
| MV4-11 | IC50 |
1.34 μM
Compound: ACY-241
|
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
|
[PMID: 34101461] |
| MV4-11 | IC50 |
1.34 μM
Compound: ACY-241
|
Cytotoxicity against human MV4-11 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human MV4-11 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
|
[PMID: 34101461] |
| NSC | IC50 |
4.35 μM
Compound: ACY-241
|
Cytotoxicity against human fetal neuronal stem cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human fetal neuronal stem cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
|
[PMID: 35119267] |
| OCI-AML-3 | IC50 |
7.7 μM
Compound: Citarinostat
|
Anti-proliferative activity against human AML-3 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human AML-3 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
|
[PMID: 33576627] |
| RPMI-8226 | IC50 |
3.16 μM
Compound: 6
|
Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method
|
[PMID: 32615502] |
| RPMI-8226 | IC50 |
3.5 μM
Compound: ACY-241
|
Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay
|
[PMID: 37463038] |
| RPMI-8226 | IC50 |
6.5 μM
Compound: Citarinostat
|
Anti-proliferative activity against human RPMI-8226 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human RPMI-8226 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
|
[PMID: 33576627] |
| Sf9 | IC50 |
>1 μM
Compound: Citarinostat
|
Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay
|
[PMID: 31938464] |
| Sf9 | IC50 |
0.318 μM
Compound: Citarinostat
|
Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
|
[PMID: 31938464] |
| Sf9 | IC50 |
2.6 nM
Compound: ACY-241
|
Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substrate a
Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substrate a
|
[PMID: 31414801] |
| Sf9 | IC50 |
35 nM
Compound: ACY-241
|
Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substr
Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substr
|
[PMID: 31414801] |
| SU-DHL-1 | IC50 |
4.56 μM
Compound: ACY-241
|
Cytotoxicity against human SU-DHL-1 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human SU-DHL-1 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
|
[PMID: 34101461] |
| U-266 | IC50 |
4.3 μM
Compound: ACY-241
|
Antiproliferative activity against human U-266 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay
Antiproliferative activity against human U-266 cells assessed as inhibition of cell proliferation incubated for 48 hrs by CCK8 assay
|
[PMID: 37463038] |
| U-87MG ATCC | IC50 |
9.1 μM
Compound: Citarinostat
|
Anti-proliferative activity against human U87G cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human U87G cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
|
[PMID: 33576627] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A2780 cells
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Concentration:0 μM, 0.1 μM, 0.3 μM, 0.5μM, 1 μM, 3 μM
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Incubation Time:24 hours
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female athymic nude mice (7-week-old) injected with TOV-21G cells[1]
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Dosage:50 mg/kg
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Administration:Intraperitoneal injection; once daily for five days, followed by two days off; for 3 weeks
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Result:Combination treatment with NSC 125973 resulted in significantly suppression of tumor growth.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1316215-12-9
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Appearance Solid
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Molecular Weight 467.95
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Formula C24H26ClN5O3
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Color White to off-white
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SMILES
O=C(C1=CN=C(N(C2=CC=CC=C2Cl)C3=CC=CC=C3)N=C1)NCCCCCCC(NO)=O
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Synonyms
ACY241
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
DMSO : 100 mg/mL (213.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1370 mL | 10.6849 mL | 21.3698 mL | 53.4245 mL |
| 5 mM | 0.4274 mL | 2.1370 mL | 4.2740 mL | 10.6849 mL | |
| 10 mM | 0.2137 mL | 1.0685 mL | 2.1370 mL | 5.3425 mL | |
| 15 mM | 0.1425 mL | 0.7123 mL | 1.4247 mL | 3.5616 mL | |
| 20 mM | 0.1068 mL | 0.5342 mL | 1.0685 mL | 2.6712 mL | |
| 25 mM | 0.0855 mL | 0.4274 mL | 0.8548 mL | 2.1370 mL | |
| 30 mM | 0.0712 mL | 0.3562 mL | 0.7123 mL | 1.7808 mL | |
| 40 mM | 0.0534 mL | 0.2671 mL | 0.5342 mL | 1.3356 mL | |
| 50 mM | 0.0427 mL | 0.2137 mL | 0.4274 mL | 1.0685 mL | |
| 60 mM | 0.0356 mL | 0.1781 mL | 0.3562 mL | 0.8904 mL | |
| 80 mM | 0.0267 mL | 0.1336 mL | 0.2671 mL | 0.6678 mL | |
| 100 mM | 0.0214 mL | 0.1068 mL | 0.2137 mL | 0.5342 mL |