ACY-241 (Synonyms: Citarinostat) |
Catalog No.GC10417
One-Click Copy Product Info
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ACY-241 (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). ACY-241 has anticancer effects.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1316215-12-9
Sample solution is provided at 25 µL, 10mM.
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ACY-241 is a new, selective and orally available inhibitor of HDAC6 [1][2].
Histone deacetylase 6 (HDAC6) is an enzyme that removes acetyl groups from an ε-N-acetyl lysine on a histone, allowing the histones to wrap the DNA more tightly. HDAC6 plays an important role in transcriptional regulation and cell cycle progression.
ACY-241 is a new, selective and orally available HDAC6 inhibitor. In MM and MCL cells, the addition of ACY-241 to either lenalidomide (len) or pomalidomide (pom) resulted in synergistic increases in apoptosis and further reduced the expression of transcription factors MYC and IRF4 [1]. In multiple solid tumor cell lines, combination treatment with ACY-241 and paclitaxel resulted in enhanced inhibition of cell proliferation and increased cell death, compared with either single agent alone [2].
In MM xenograft model, combination treatment with ACY-241 and pomalidomide was well tolerated with no overt toxicity and significantly extended survival [1]. In xenograft models of pancreatic and ovarian cancer, combination treatment with ACY-241 and paclitaxel significantly increased mitotic cells with multipolar spindles. ACY-241 dose-dependently increased α-tubulin hyperacetylation [2].
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
| Cell experiment [1]: | |
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Cell lines |
A2780 ovarian cancer cells |
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Preparation method |
The solubility of this compound in DMSO is >23.4mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
0.1, 0.3, 0.5, 1. 3 μM; dissolved in DMSO; 24 h |
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Applications |
In A2780 ovarian cancer cells, ACY-241 (0.3 μM) increased hyperacetylation of α-tubulin, consistent with inhibition of the tubulin deacetylase HDAC6. Hyperacetylation of histone H3, a target of Class I HDACs, was only observed at doses above 1 μM. ACY-241 preferentially induced hyperacetylation of α-tubulin relative to H3K56. |
| Animal experiment [1]: | |
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Animal models |
female athymic nude mice bearing MiaPaCa-2 pancreatic cancer xenografts |
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Dosage form |
ACY-241: 50 mg/kg once daily for five days, followed by two days off, for three consecutive weeks; intraperitoneal injectionPaclitaxel: 10 mg/kg once daily for five consecutive days; intraperitoneal injection |
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Application |
In female athymic nude mice bearing MiaPaCa-2 pancreatic cancer xenografts, ACY-241 (50 mg/kg) plus paclitaxel (10 mg/kg) inhibited tumor growth and did not result in body weight loss. ACY-241 was well tolerated in mice when dosed as a single agent and in combination with paclitaxel. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. 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 |
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| Cas No. | 1316215-12-9 | SDF | |
| Synonyms | Citarinostat | ||
| Chemical Name | (Z)-2-((2-chlorophenyl)(phenyl)amino)-N-((Z)-7-hydroxy-7-(hydroxyimino)heptyl)pyrimidine-5-carbimidic acid | ||
| Canonical SMILES | ClC1=CC=CC=C1N(C2=NC=C(/C(O)=N/CCCCCC/C(O)=N/O)C=N2)C3=CC=CC=C3 | ||
| Formula | C24H26ClN5O3 | M.Wt | 467.95 |
| Solubility | ≥ 23.4mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.137 mL | 10.6849 mL | 21.3698 mL |
| 5 mM | 427.4 μL | 2.137 mL | 4.274 mL |
| 10 mM | 213.7 μL | 1.0685 mL | 2.137 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 3 reference(s) in Google Scholar.)