[CAS NO. 1316215-12-9] Citarinostat (ACY-241)

Name: Citarinostat (ACY-241)
Brand: Arctom Scientific
SKU: SLK-S8464

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PRODUCTS SPECIFICATIONS [1316215-12-9]

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Catalog

SLK-S8464

Brand

Selleck

CAS

1316215-12-9

DESCRIPTION [1316215-12-9]

Overview

MDL	MFCD28023593
Molecular Weight	467.95
Molecular Formula	C24H26ClN5O3
SMILES	O=C(C1=CN=C(N(C2=CC=CC=C2Cl)C3=CC=CC=C3)N=C1)NCCCCCCC(NO)=O

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume 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
50 mM	0.0427 mL	0.2137 mL	0.4274 mL

Description

Citarinostat (ACY-241, HDAC-IN-2) is an orally available selective inhibitor with IC50 of 2.6 nM and 46 nM for HDAC6 and HDAC3, respectively. It has 13 to 18-fold selectivity towards HDAC6 in comparison to HDAC1-3.

Targets

HDAC6 ^[1] (Cell-free assay)	HDAC1 ^[1] (Cell-free assay)	HDAC2 ^[1] (Cell-free assay)	HDAC3 ^[1] (Cell-free assay)	HDAC8 ^[1] (Cell-free assay)
2.6 nM	35 nM	45 nM	46 nM	137 nM

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.

References

[1] Huang P, et al. Oncotarget. 2017, 8(2):2694-2707.