Citarinostat,1316215-12-9

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Citarinostat

CAS No. : 1316215-12-9

MCE 国际站：Citarinostat

产品活性：Citarinostat (ACY241) 是第二代有效的，口服活性，高选择性的 HDAC6 抑制剂，IC₅₀ 为 2.6 nM (HDAC1，HDAC2，HDAC3 和 HDAC8 的 IC₅₀ 分别为 35 nM，45 nM，46 nM 和 137 nM)。Citarinostat 具有抗癌作用。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics

作用靶点：HDAC

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.
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.

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.

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