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  2. Cell Cycle/DNA Damage Epigenetics
  3. HDAC
  4. Citarinostat

Citarinostat (ACY241) 是第二代有效的，口服活性，高選擇性的 HDAC6 抑制劑，IC50 為 2.6 nM (HDAC1，HDAC2，HDAC3 和 HDAC8 的 IC50 分別為 35 nM，45 nM，46 nM 和 137 nM)。Citarinostat 具有抗癌作用。

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Citarinostat Chemical Structure

Citarinostat Chemical Structure

CAS No. : 1316215-12-9

1.  客戶無需承擔(dān)相應(yīng)的運輸費用。

2.  同一機構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機構(gòu)（單位）一年內(nèi)

     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥772
In-stock
1 mg ￥449
In-stock
5 mg ￥750
In-stock
10 mg ￥1200
In-stock
25 mg ￥2450
In-stock
50 mg ￥4060
In-stock
100 mg 現(xiàn)貨 詢價
200 mg   詢價  
500 mg   詢價  

* Please select Quantity before adding items.

Customer Review

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Citarinostat (ACY241) is a second generation potent, orally active and high-selective HDAC6 inhibitor with an IC50 of 2.6 nM (IC50s of 35 nM, 45 nM, 46 nM and 137 nM for HDAC1, HDAC2, HDAC3 and HDAC8, respectively). Citarinostat has anticancer effects[1].

IC50 & Target[1]

HDAC6

2.6 nM (IC50)

HDAC1

35 nM (IC50)

HDAC2

45 nM (IC50)

HDAC3

46 nM (IC50)

HDAC8

137 nM (IC50)

HDAC7

7300 nM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
BV-173 IC50
0.9 μM
Compound: Citarinostat
Anti-proliferative activity against human BV-173 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human BV-173 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
Fibroblast IC50
5.7 μM
Compound: 6
Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method
Cytotoxicity against human fibroblasts measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
Fibroblast IC50
5.7 μM
Compound: ACY-241
Cytotoxicity against primary normal human fibroblast cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against primary normal human fibroblast cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
Fibroblast IC50
5.74 μM
Compound: ACY-241
Cytotoxicity against human normal fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human normal fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
Fibroblast IC50
7.4 μM
Compound: 6
Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method
Cytotoxicity against pooled human fibroblasts measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
Fibroblast IC50
7.4 μM
Compound: ACY-241
Cytotoxicity against human primary pooled fibroblasts cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human primary pooled fibroblasts cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
Fibroblast IC50
7.44 μM
Compound: ACY-241
Cytotoxicity against primary pooled human fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against primary pooled human fibroblast assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
HeLa IC50
7 μM
Compound: Citarinostat
Anti-proliferative activity against human HeLa cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human HeLa cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
HuT78 IC50
1.78 μM
Compound: ACY-241
Cytotoxicity against human Hut78 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human Hut78 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
HUVEC IC50
4.86 μM
Compound: ACY-241
Cytotoxicity against human HUVEC cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human HUVEC cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
HUVEC IC50
4.9 μM
Compound: 6
Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human HUVEC cells measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
HUVEC IC50
4.9 μM
Compound: ACY-241
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
Jurkat IC50
1.2 μM
Compound: Citarinostat
Anti-proliferative activity against human Jurkat cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human Jurkat cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
MM1.S IC50
1.52 μM
Compound: 6
Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human MM1.S cells measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
MM1.S IC50
1.6 μM
Compound: Citarinostat
Anti-proliferative activity against human MM1.S cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human MM1.S cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
MM1.S IC50
1.61 μM
Compound: ACY-241
Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
MOLM-13 IC50
13.5 μM
Compound: Citarinostat
Anti-proliferative activity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
MOLT-4 IC50
1.72 μM
Compound: ACY-241
Cytotoxicity against human MOLT-4 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human MOLT-4 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
MV4-11 IC50
1.2 μM
Compound: Citarinostat
Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
MV4-11 IC50
1.24 μM
Compound: 6
Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human MV4-11 cells measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
MV4-11 IC50
1.24 μM
Compound: ACY-241
Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
MV4-11 IC50
1.34 μM
Compound: ACY-241
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human MV4-11 cells assessed as cell viability incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
MV4-11 IC50
1.34 μM
Compound: ACY-241
Cytotoxicity against human MV4-11 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human MV4-11 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
NSC IC50
4.35 μM
Compound: ACY-241
Cytotoxicity against human fetal neuronal stem cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
Cytotoxicity against human fetal neuronal stem cells assessed as inhibition of cell growth incubated for 72 hrs measured by spectrophotometer analysis
[PMID: 35119267]
OCI-AML-3 IC50
7.7 μM
Compound: Citarinostat
Anti-proliferative activity against human AML-3 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human AML-3 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
RPMI-8226 IC50
3.16 μM
Compound: 6
Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method
Cytotoxicity against human RPMI-8226 cells measured after 72 hrs by spectrophotometer method
[PMID: 32615502]
RPMI-8226 IC50
6.5 μM
Compound: Citarinostat
Anti-proliferative activity against human RPMI-8226 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human RPMI-8226 cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
Sf9 IC50
> 1 μM
Compound: Citarinostat
Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 1.5 hrs by electrophoretic mobility shift assay
[PMID: 31938464]
Sf9 IC50
0.318 μM
Compound: Citarinostat
Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
Inhibition of recombinant full length human HDAC2 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 17 hrs by electrophoretic mobility shift assay
[PMID: 31938464]
Sf9 IC50
2.6 nM
Compound: ACY-241
Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substrate a
Inhibition of recombinant human full length N-terminal GST-tagged HDAC6 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substrate a
[PMID: 31414801]
Sf9 IC50
35 nM
Compound: ACY-241
Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substr
Inhibition of recombinant human full length C-terminal His/FLAG-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in release of 7-amino-4-methoxycoumarin using FTS as substrate preincubated for 10 mins followed by substr
[PMID: 31414801]
SU-DHL-1 IC50
4.56 μM
Compound: ACY-241
Cytotoxicity against human SU-DHL-1 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
Cytotoxicity against human SU-DHL-1 cells assessed as reduction in cell growth incubated for 72 hrs by Cell titer-blue assay
[PMID: 34101461]
U-87MG ATCC IC50
9.1 μM
Compound: Citarinostat
Anti-proliferative activity against human U87G cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
Anti-proliferative activity against human U87G cells assessed as cell viability measured after 72 hrs by Cell-Titer assay
[PMID: 33576627]
體外研究
(In Vitro)

Citarinostat (ACY241;300 nM;24小時;A2780細(xì)胞)導(dǎo)致 α-微管蛋白高乙?；黾?，與微管蛋白去乙?；?HDAC6 的抑制一致。Citarinostat低劑量可選擇性抑制 HDAC6，而高劑量暴露可抑制 I 類 HDAC 同型酶[1]。
Citarinostat 在 A2780、TOV-21G 卵巢癌和 MDA-MD-231 乳腺癌細(xì)胞中的IC50 范圍為4.6 ~ 6.1 μM[1]。
Citarinostat在 3 μM劑量下抑制細(xì)胞增殖，不誘導(dǎo)細(xì)胞凋亡，10 μM 時顯著誘導(dǎo)細(xì)胞凋亡，完全抑制細(xì)胞增殖[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: A2780 cells
Concentration: 0 μM, 0.1 μM, 0.3 μM, 0.5μM, 1 μM, 3 μM
Incubation Time: 24 hours
Result: Resulted 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, was only observed at doses above 1 μM.
體內(nèi)研究
(In Vivo)

Citarinostat (ACY241；50 mg/kg；腹腔注射；每天一次，持續(xù) 5 天，隨后停藥兩天；持續(xù) 3 周；雌性無胸腺裸鼠) 與 NSC 125973 聯(lián)合使用顯著抑制腫瘤生長[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic nude mice (7-week-old) injected with TOV-21G cells[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; once daily for five days, followed by two days off; for 3 weeks
Result: Combination treatment with NSC 125973 resulted in significantly suppression of tumor growth.
Clinical Trial
分子量

467.95

Formula

C24H26ClN5O3
CAS 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實驗： 

DMSO 中的溶解度 : ≥ 30 mg/mL (64.11 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.34 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.34 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.30%

參考文獻(xiàn)

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1370 mL 10.6849 mL 21.3698 mL 53.4245 mL
5 mM 0.4274 mL 2.1370 mL 4.2740 mL 10.6849 mL
10 mM 0.2137 mL 1.0685 mL 2.1370 mL 5.3425 mL
15 mM 0.1425 mL 0.7123 mL 1.4247 mL 3.5616 mL
20 mM 0.1068 mL 0.5342 mL 1.0685 mL 2.6712 mL
25 mM 0.0855 mL 0.4274 mL 0.8548 mL 2.1370 mL
30 mM 0.0712 mL 0.3562 mL 0.7123 mL 1.7808 mL
40 mM 0.0534 mL 0.2671 mL 0.5342 mL 1.3356 mL
50 mM 0.0427 mL 0.2137 mL 0.4274 mL 1.0685 mL
60 mM 0.0356 mL 0.1781 mL 0.3562 mL 0.8904 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
Citarinostat
目錄號：
HY-15994
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