Ambeed.cn

首页 / / / 组蛋白去乙酰化酶 / Citarinostat/西他司他

Citarinostat/西他司他 {[allProObj[0].p_purity_real_show]}

货号:A207811 同义名: ACY241; HDAC-IN-2

Citarinostat是一种选择性HDAC6抑制剂,IC50为4 nM。它还可以抑制HDAC3(IC50 = 76 nM)。

Citarinostat/西他司他 化学结构 CAS号:1316215-12-9
Citarinostat/西他司他 化学结构
CAS号:1316215-12-9
Citarinostat/西他司他 3D分子结构
CAS号:1316215-12-9
Citarinostat/西他司他 化学结构 CAS号:1316215-12-9
Citarinostat/西他司他 3D分子结构 CAS号:1316215-12-9
规格 价格 会员价 库存 数量
{[ item.pr_size ]}

{[ getRatePriceInt(item.pr_rmb, 1,1) ]}

{[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}

{[ getRatePriceInt(item.pr_rmb, 1,1) ]}

{[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}
{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]} 现货 1周 咨询 - +
购物车0 收藏 询单

Citarinostat/西他司他 纯度/质量文件 产品仅供科研

货号:A207811 标准纯度: {[allProObj[0].p_purity_real_show]}
批次查询: 批次纯度:

全球学术期刊中引用的产品

Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
Cell, 2025. Ambeed. [ A122167 ]
Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >
产品名称 HD1 HD2 HDAC HDAC1 HDAC10 HDAC11 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 其他靶点 纯度
Givinostat HCl monohydrate ++++

HD1-B, IC50: 7.5 nM

HD1-A, IC50: 16 nM

+++

HD2, IC50: 10 nM

99%+
MC1568 ++

HD1-B (Maize), IC50: 3.4 μM

HD1-A (Maize), IC50: 100 nM

96%
Trichostatin A ++++

HDAC, IC50: ~1.8 nM

99%+
Scriptaid 99%+
Valproic acid sodium Autophagy 97%
AR-42 +++

HDAC, IC50: 30 nM

99%+
Dacinostat +++

HDAC, IC50: 32 nM

98+%
CUDC-101 ++++

HDAC, IC50: 4.4 nM

++++

HDAC1, IC50: 4.5 nM

+++

HDAC10, IC50: 26.1 nM

+++

HDAC2, IC50: 12.6 nM

++++

HDAC3, IC50: 9.1 nM

+++

HDAC4, IC50: 13.2 nM

+++

HDAC5, IC50: 11.4 nM

++++

HDAC6, IC50: 5.1 nM

+

HDAC7, IC50: 373 nM

++

HDAC8, IC50: 79.8 nM

++

HDAC9, IC50: 67.2 nM

EGFR,HER2 99%+
M344 ++

HDAC, IC50: 100 nM

99%+
Splitomicin +

Sir2p, IC50: 60 μM

99%
Panobinostat ++++

HDAC (Reh cells), IC50: 20 nM

HDAC (MOLT-4 cells), IC50: 5 nM

98%
Sodium 4-Phenylbutyrate 98%
Vorinostat +++

HDAC, IC50: ~10 nM

98%
Curcumin Nrf2,NF-κB 98%
Belinostat +++

HDAC, IC50: 27 nM

98%
RG-2833 ++

HDAC1, Ki: 32 nM

++

HDAC3, Ki: 5 nM

98%
Valproic acid +

HDAC1, IC50: 0.4 mM

98%
BG45 +

HDAC1, IC50: 2 μM

+

HDAC2, IC50: 2.2 μM

+

HDAC3, IC50: 289 nM

99%+
Entinostat +

HDAC1, IC50: 0.51 μM

+

HDAC3, IC50: 1.7 μM

98%
Resminostat +++

HDAC1, IC50: 42.5 nM

++

HDAC3, IC50: 50.1 nM

++

HDAC6, IC50: 71.8 nM

98+%
Romidepsin +++

HDAC1, IC50: 36 nM

+++

HDAC2, IC50: 47 nM

99%+
Parthenolide NF-κB,p53 97% HPLC
Tacedinaline +

HDAC1, IC50: 0.9 μM

+

HDAC2, IC50: 0.9 μM

+

HDAC3, IC50: 1.2 μM

98%
Mocetinostat ++

HDAC1, IC50: 0.15 μM

+

HDAC11, IC50: 0.59 μM

+

HDAC2, IC50: 0.29 μM

+

HDAC3, IC50: 1.66 μM

98%
WT-161 ++++

HDAC1, IC50: 8.35 nM

+++

HDAC2, IC50: 15.4 nM

++++

HDAC6, IC50: 0.4 nM

99%+
Fimepinostat ++++

HDAC1, IC50: 1.7 nM

++++

HDAC10, IC50: 2.8 nM

++++

HDAC11, IC50: 5.4 nM

++++

HDAC2, IC50: 5.0 nM

++++

HDAC3, IC50: 1.8 nM

+++

HDAC6, IC50: 27 nM

99%+
Tucidinostat ++

HDAC1, IC50: 95 nM

++

HDAC10, IC50: 78 nM

++

HDAC2, IC50: 160 nM

++

HDAC3, IC50: 67 nM

99%+
Santacruzamate A ++++

HDAC2, IC50: 119 pM

99%+
(E,E)-RGFP966 ++

HDAC3, IC50: 80 nM

99%+
LMK-235 +++

HDAC4, IC50: 11.9 nM

++++

HDAC5, IC50: 4.2 nM

99%+
Tasquinimod 99%+
CAY10603 ++++

HDAC6, IC50: 2 pM

98%
Tubastatin A +++

HDAC6, IC50: 15 nM

98%
Tubacin ++++

HDAC6, IC50: 4 nM

99%+
ACY-738 ++++

HDAC6, IC50: 1.7 nM

99%+
Nexturastat A ++++

HDAC6, IC50: 5 nM

99%+
BRD73954 +++

HDAC6, IC50: 36 nM

++

HDAC8, IC50: 120 nM

99%
Tubastatin A HCl +++

HDAC6, IC50: 15 nM

+

HDAC8, IC50: 854 nM

98%
PCI-34051 +++

HDAC8, IC50: 10 nM

99%+
Ricolinostat ++

HDAC1, IC50: 58 nM

++

HDAC2, IC50: 48 nM

++

HDAC3, IC50: 51 nM

++++

HDAC6, IC50: 4.7 nM

++

HDAC8, IC50: 100 nM

99%+
Droxinostat +

HDAC3, IC50: 16.9 μM

+

HDAC6, IC50: 2.47 μM

+

HDAC8, IC50: 1.46 μM

99%+
Abexinostat ++++

HDAC1, Ki: 7 nM

+++

HDAC10, IC50: 24 nM

+++

HDAC2, Ki: 19 nM

++++

HDAC3/SMRT, Ki: 8.2 nM

+++

HDAC6, Ki: 17 nM

+

HDAC8, IC50: 280 nM

98%+
Citarinostat +++

HDAC1, IC50: 35 nM

+++

HDAC2, IC50: 45 nM

+++

HDAC3, IC50: 46 nM

++++

HDAC6, IC50: 2.6 nM

++

HDAC8, IC50: 137 nM

99%+
HPOB +

HDAC1, IC50: 2.9 μM

+

HDAC10, IC50: 3.0 μM

+

HDAC2, IC50: 4.4 μM

+

HDAC3, IC50: 1.7 μM

++

HDAC6, IC50: 56 nM

+

HDAC8, IC50: 2.8 μM

97%
Quisinostat 2HCl ++++

HDAC1, IC50: 0.11 nM

++++

HDAC10, IC50: 0.46 nM

++++

HDAC11, IC50: 0.37 nM

++++

HDAC2, IC50: 0.33 nM

++++

HDAC3, IC50: 4.86 nM

++++

HDAC4, IC50: 0.64 nM

++++

HDAC5, IC50: 3.69 nM

++++

HDAC8, IC50: 4.26 nM

97%
Domatinostat +

HDAC1, IC50: 1.20 μM

+

HDAC10, IC50: 21 μM

+

HDAC11, IC50: 9.7 μM

+

HDAC2, IC50: 1.12 μM

+

HDAC3, IC50: 0.57 μM

+

HDAC5, IC50: 11.3 μM

+

HDAC9, IC50: 50 μM

99%+
TMP269 ++

HDAC4, IC50: 157 nM

++

HDAC5, IC50: 97 nM

+++

HDAC7, IC50: 43 nM

+++

HDAC9, IC50: 23 nM

99%+
Pracinostat ++

HDAC1, IC50: 49 nM

+++

HDAC10, IC50: 40 nM

++

HDAC11, IC50: 93 nM

++

HDAC2, IC50: 96 nM

+++

HDAC3, IC50: 43 nM

++

HDAC4, IC50: 56 nM

+++

HDAC5, IC50: 47 nM

+

HDAC6, IC50: 1.008 μM

++

HDAC7, IC50: 137 nM

++

HDAC8, IC50: 140 nM

++

HDAC9, IC50: 70 nM

99%+
TMP195 ++

HDAC4, Ki: 59 nM

++

HDAC5, Ki: 60 nM

+++

HDAC7, Ki: 26 nM

+++

HDAC9, Ki: 15 nM

99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Citarinostat/西他司他 生物活性

靶点
  • HDAC8

    HDAC8, IC50:137 nM

  • HDAC3

    HDAC3, IC50:46 nM

  • HDAC6

    HDAC6, IC50:2.6 nM

  • HDAC2

    HDAC2, IC50:45 nM

  • HDAC1

    HDAC1, IC50:35 nM

描述 Citarinostat (ACY241) is an orally available, and highly selective inhibitor of HDAC6, showing an IC50 of 2.6 nM. Its selectivity extends across other HDAC isoforms as well, with IC50 values of 35 nM, 45 nM, 46 nM, and 137 nM for HDAC1, HDAC2, HDAC3, and HDAC8, respectively, suggesting its potential for anticancer applications[1].
体内研究

Furthermore, in vivo studies reveal that Citarinostat, dosed at 50 mg/kg via intraperitoneal injection once daily for five days followed by a two-day break for three weeks, significantly inhibits tumor growth. This effect is observed in female athymic nude mice when Citarinostat is used in conjunction with NSC 125973, highlighting its therapeutic potential in cancer treatment when possibly combined with other anticancer agents.

体外研究

When administered to A2780 cells at a concentration of 300 nM for 24 hours, Citarinostat leads to notable hyperacetylation of α-tubulin, indicating the inhibition of HDAC6's tubulin deacetylase activity. Conversely, significant hyperacetylation of histone H3, a Class I HDAC target, is observed only at concentrations exceeding 1 μM. This delineates Citarinostat's capability for selective inhibition of HDAC6 at lower doses, while higher doses inhibit Class I HDAC isozymes[1].

In terms of cytotoxicity, Citarinostat's IC50 values span from 4.6 to 6.1 μM in A2780 and TOV-21G ovarian cancer cells, as well as in MDA-MB-231 breast cancer cells. The data indicate that lower doses of Citarinostat up to 3 μM modestly reduce cell proliferation without triggering apoptosis. However, a higher dose of 10 μM markedly induces apoptosis and entirely halts proliferation[1].

Citarinostat/西他司他 细胞实验

Cell Line
Concentration Treated Time Description References
S1 cells 2.82 ± 0.40 µM 72 hours Evaluate the cytotoxicity of Citarinostat on S1 cells Int J Mol Sci. 2021 Mar 5;22(5):2592.
MM.1s 100-500 nM 18 hours To evaluate the selectivity of ACY-241 in MM cells. Results showed that ACY-241 selectively increased acetylation of α-Tubulin at low concentrations and increased acetylation of Histone-H3 at higher concentrations. PLoS One. 2017 Mar 6;12(3):e0173507.
KP lung cancer cells 10 µg/ml 36 hours To evaluate the effect of ACY241 and Oxaliplatin on the effector function of tumor-associated T cells, results showed that ACY241 or Oxaliplatin alone enhanced the ability of CD8+ T cells to secrete TNFα and IFNγ, and the combination treatment had a more pronounced effect. Oncoimmunology. 2022 Feb 22;11(1):2042065.
CD4+ CD127loCD25+ Tregs 500nM 72 hours To evaluate the impact of HDAC6-selective inhibitors on regulatory T-cells (Tregs). Results showed that ACY-241 reduced Treg frequencies and FOXP3 expression and decreased their suppressive function. J Immunother Cancer. 2019 Feb 6;7(1):33.
R482-HEK293 cells 20.11 ± 2.48 µM 72 hours Evaluate the cytotoxicity of Citarinostat on R482-HEK293 cells Int J Mol Sci. 2021 Mar 5;22(5):2592.
MDR19-HEK293 cells 33.83 ± 3.21 µM 72 hours Evaluate the cytotoxicity of Citarinostat on MDR19-HEK293 cells Int J Mol Sci. 2021 Mar 5;22(5):2592.
HEK293 cells 3.01 ± 0.44 µM 72 hours Evaluate the cytotoxicity of Citarinostat on HEK293 cells Int J Mol Sci. 2021 Mar 5;22(5):2592.
S1-M1-80 cells 59.66 ± 10.32 µM 72 hours Evaluate the cytotoxicity of Citarinostat on S1-M1-80 cells Int J Mol Sci. 2021 Mar 5;22(5):2592.
KB-V-1 cells 57.96 ± 5.56 µM 72 hours Evaluate the cytotoxicity of Citarinostat on KB-V-1 cells Int J Mol Sci. 2021 Mar 5;22(5):2592.
KB-3-1 cells 3.98 ± 0.73 µM 72 hours Evaluate the cytotoxicity of Citarinostat on KB-3-1 cells Int J Mol Sci. 2021 Mar 5;22(5):2592.
T-cells from melanoma patient PBMCs 500nM 72 hours To evaluate the impact of HDAC6-selective inhibitors on T-cell viability and function. Results showed that ACY-241 did not impair T-cell viability at concentrations up to 1uM and reduced Th2 cytokine production (i.e. IL-4, IL-5, IL-6, IL-10 and IL-13). J Immunother Cancer. 2019 Feb 6;7(1):33.
Granta-519 0, 0.5, 1, 2, 4 µM 24-48 hours To evaluate the cytotoxicity of Citarinostat and Momelotinib alone and in combination on Granta-519 cells. Results showed that Granta-519 cells were less sensitive to the combination treatment (CI > 1), exhibiting an antagonistic effect. Apoptosis. 2020 Jun;25(5-6):370-387.
WSU-NHL 0, 0.5, 1, 2, 4 µM 24-48 hours To evaluate the cytotoxicity of Citarinostat and Momelotinib alone and in combination on lymphoid malignant cell lines. Results showed that the combination of Citarinostat and Momelotinib exhibited synergistic effects (CI < 1) in most cell lines, significantly inhibiting cell viability and inducing apoptosis. Apoptosis. 2020 Jun;25(5-6):370-387.

Citarinostat/西他司他 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
CB.17 SCID mice H929 MM xenograft model Intraperitoneal injection 50 mg/kg (ACY-241), 1 mg/kg (pomalidomide) Once daily for 42 consecutive days To evaluate the effect of combination treatment with ACY-241 and pomalidomide on tumor growth in the H929 MM xenograft model. Results showed that combination treatment significantly inhibited tumor growth without significant toxicity or adverse effects. PLoS One. 2017 Mar 6;12(3):e0173507.
Mice KP lung cancer model Intraperitoneal injection 25 mg/kg (ACY241), 10 mg/kg (Oxaliplatin) ACY241 3 times/week for 3 weeks; Oxaliplatin 1 time/week for 6 weeks To evaluate the therapeutic effect of ACY241 alone or in combination with Oxaliplatin, results showed that combination therapy significantly prolonged the survival of mice and enhanced the effector function of tumor-associated T cells. Oncoimmunology. 2022 Feb 22;11(1):2042065.

Citarinostat/西他司他 参考文献

[1]Huang P, et al. Selective HDAC inhibition by ACY-241 enhances the activity of NSC 125973 in solid tumor models. Oncotarget. 2017 Jan 10;8(2):2694-2707.

Citarinostat/西他司他 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.14mL

0.43mL

0.21mL

10.68mL

2.14mL

1.07mL

21.37mL

4.27mL

2.14mL

Citarinostat/西他司他 技术信息

CAS号1316215-12-9
分子式C24H26ClN5O3
分子量 467.95
SMILES Code O=C(C1=CN=C(N(C2=CC=CC=C2Cl)C3=CC=CC=C3)N=C1)NCCCCCCC(NO)=O
MDL No. MFCD28023593
别名 ACY241; HDAC-IN-2
运输蓝冰
InChI Key VLIUIBXPEDFJRF-UHFFFAOYSA-N
Pubchem ID 53340426
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 30 mg/mL(64.11 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
AmBeed 相关网站 AmBeed.cn AmBeed.com
AmBeed
关于我们
联系我们
资讯中心
网站地图
产品手册
  • 批次文件查询
  • 客户支持
    技术支持
    专业术语
    缩略词释义
    质量手册
    产品咨询
    计算器
    活动政策
    订购方法
    积分商城
    活动声明
    联系我们
    400-920-2911 sales@ambeed.cn tech@ambeed.cn
    AmBeed 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务,不为任何个人或者非科研性质用途提供服务。