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Citarinostat

Cat. No. M5259
Citarinostat Structure
Synonym:

ACY-241

Size Price Availability Quantity
5mg USD 135 In stock
10mg USD 220 In stock
50mg USD 810 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

In vitro: In cell lines from multiple solid tumor lineages, combination treatment with ACY-241 and paclitaxel enhances inhibition of proliferation and increases cell death relative to either single agent alone. Combination treatment with ACY-241 and paclitaxel also results in more frequent occurrence of mitotic cells with abnormal multipolar spindles and aberrant mitoses, and is associated with increased frequency of abnormal multipolar mitotic spindle formation, induction of aneuploidy, and increased cell death. In A2780 ovarian cancer cells, 24 hour treatment with 300 nM ACY-241 results in increased hyperacetylation of α-tubulin, consistent with inhibition of the tubulin deacetylase HDAC6. Low exposures of ACY-241 result in selective inhibition of HDAC6, while higher exposures lead to inhibition of Class I HDAC isozymes. In vivo: ACY-241 has a favourable safety profile than non-selective pan-HDAC inhibitors. It has the potential for a substantially reduced side effect profile versus current nonselective HDAC inhibitor drug candidates due to reduced potency against Class I HDACs while retaining the potential for anticancer effectiveness.

Protocol
Cell Experiment
Cell lines A2780 ovarian cancer cells
Preparation method A2780 cells are cultured with vehicle or a range of ACY-241 concentrations for 24 hours prior to immunoblotting.
Concentrations 0.1, 0.3, 0.5, 1, 3 μM
Incubation time 24 h
Animal Experiment
Animal models Female athymic nude mice (Crl:NU(NCr)-Foxn1nu)
Formulation
Dosages 50 mg/kg
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 467.95
Formula C24H26ClN5O3
CAS Number 1316215-12-9
Purity >99%
Solubility 93 mg/mL in DMSO
Storage at -20°C
References

Enhancement of pomalidomide anti-tumor response with ACY-241, a selective HDAC6 inhibitor.
North BJ, et al. PLoS One. 2017 Mar 6;12(3):e0173507. PMID: 28264055.

Selective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models.
Huang P, et al. Oncotarget. 2017 Jan 10;8(2):2694-2707. PMID: 27926524.

Deacetylase inhibitors as a novel modality in the treatment of multiple myeloma.
Richardson PG, et al. Pharmacol Res. 2017 Mar;117:185-191. PMID: 27884726.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Citarinostat, ACY-241 supplier, HDAC, inhibitors

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