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ACY-241 Sale

(Synonyms: 西他司他,Citarinostat) 目录号 : GC10417

An HDAC6 inhibitor

ACY-241 Chemical Structure

Cas No.:1316215-12-9

规格 价格 库存 购买数量
5mg
¥1,080.00
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Sample solution is provided at 25 µL, 10mM.

Description

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

实验参考方法

Cell experiment [1]:

Cell lines

A2780 ovarian cancer cells

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.

Reacting condition

0.1, 0.3, 0.5, 1. 3 μM; dissolved in DMSO; 24 h

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]:

Animal models

female athymic nude mice bearing MiaPaCa-2 pancreatic cancer xenografts

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

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.

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.

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

化学性质

Cas No. 1316215-12-9 SDF
别名 西他司他,Citarinostat
化学名 (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
分子式 C24H26ClN5O3 分子量 467.95
溶解度 ≥ 23.4mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.137 mL 10.6849 mL 21.3698 mL
5 mM 0.4274 mL 2.137 mL 4.274 mL
10 mM 0.2137 mL 1.0685 mL 2.137 mL
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