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  1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. HDAC Apoptosis
  3. Tacedinaline

Tacedinaline  (Synonyms: N-acetyldinaline; CI-994; Goe-5549)

目錄號(hào): HY-50934 純度: 99.32%
COA 產(chǎn)品使用指南 技術(shù)支持

Tacedinaline (N-acetyldinaline) 是組蛋白脫乙酰酶(HDAC)的抑制劑,抑制重組 HDAC 1, 2 和 3 的 IC50 值分別為 0.9,0.9,1.2 μM。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào),我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Tacedinaline Chemical Structure

Tacedinaline Chemical Structure

CAS No. : 112522-64-2

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  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Tacedinaline (N-acetyldinaline) is an inhibitor of the histone deacetylase (HDAC) with IC50s of 0.9, 0.9, 1.2 μM for recombinant HDAC 1, 2 and 3 respectively.

IC50 & Target[1]

HD1

0.9 μM (IC50)

HD2

0.9 μM (IC50)

HD3

1.2 μM (IC50)

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
A-375 IC50
11.29 μM
Compound: CI994
Antiproliferative activity against human A375 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human A375 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 31003060]
A-375 IC50
11.29 μM
Compound: CI994
Antiproliferative activity against human A375 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human A375 cells after 72 hrs by CCK-8 assay
[PMID: 29202397]
A-375 IC50
11.3 μM
Compound: Tacedinaline
Antiproliferative activity against human A375 cells after 72 hrs CCK8 assay
Antiproliferative activity against human A375 cells after 72 hrs CCK8 assay
[PMID: 30108928]
A-375 IC50
9.64 μM
Compound: 5; CI994
Antiproliferative activity against human A375 cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human A375 cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
[PMID: 31103900]
A549 IC50
10.17 μM
Compound: 2
Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay
[PMID: 30045621]
A549 IC50
15.96 μM
Compound: CI-994
Cytotoxicity against human A549 cells assessed as decrease in cell viability measured after 72 hrs by CellTiter-Glo Luminescent assay
Cytotoxicity against human A549 cells assessed as decrease in cell viability measured after 72 hrs by CellTiter-Glo Luminescent assay
[PMID: 31223439]
A549 IC50
16.45 μM
Compound: 5; CI994
Antiproliferative activity against human A549 cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
[PMID: 31103900]
A549 IC50
20.1 μM
Compound: CI994
Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 31003060]
A549 IC50
20.1 μM
Compound: 6; CI994
Antiproliferative activity against human A549 cells after 72 hrs by CCK-8 reagent based assay
Antiproliferative activity against human A549 cells after 72 hrs by CCK-8 reagent based assay
[PMID: 28391133]
A549 IC50
20.1 μM
Compound: Tacedinaline
Antiproliferative activity against human A549 cells after 72 hrs CCK8 assay
Antiproliferative activity against human A549 cells after 72 hrs CCK8 assay
[PMID: 30108928]
Epithelial cell IC50
> 50 μM
Compound: 18, pfizer,CI-994
Cytotoxicity against human mammary epithelial cells by MTT assay
Cytotoxicity against human mammary epithelial cells by MTT assay
[PMID: 17941625]
HCT-116 IC50
10 μM
Compound: 5; CI-994
Cytotoxicity in human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity in human HCT116 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 28885834]
HCT-116 IC50
4 μM
Compound: 18, pfizer,CI-994
Cytotoxicity against human HCT116 cells by MTT assay
Cytotoxicity against human HCT116 cells by MTT assay
[PMID: 17941625]
HCT-116 IC50
6.39 μM
Compound: 5; CI994
Antiproliferative activity against human HCT116 cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human HCT116 cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
[PMID: 31103900]
HCT-116 IC50
7.71 μM
Compound: CI994
Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HCT116 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 31003060]
HCT-116 IC50
7.71 μM
Compound: CI994
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 assay
[PMID: 29202397]
HCT-116 IC50
7.71 μM
Compound: 6; CI994
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 reagent based assay
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK-8 reagent based assay
[PMID: 28391133]
HCT-116 EC50
8.4 μM
Compound: Cl-994
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 48 hrs by cell-titer glo assay
Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 48 hrs by cell-titer glo assay
[PMID: 35293758]
HCT-116 IC50
9.83 μM
Compound: 2
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay
[PMID: 30045621]
HeLa IC50
1.81 μM
Compound: 5; CI994
Inhibition of HDAC in human HeLa cell nuclear extract assessed as decrease in deacetylation of FLUOR DE LYS Green substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence based assay
Inhibition of HDAC in human HeLa cell nuclear extract assessed as decrease in deacetylation of FLUOR DE LYS Green substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence based assay
[PMID: 31103900]
HeLa IC50
1.81 μM
Compound: CI994
Inhibition of HDAC in human HeLa cell nuclear extract using fluor-de-lys-green as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence assay
Inhibition of HDAC in human HeLa cell nuclear extract using fluor-de-lys-green as substrate preincubated for 10 mins followed by substrate addition and measured after 30 mins by fluorescence assay
[PMID: 31003060]
HeLa IC50
13.43 μM
Compound: 5; CI994
Antiproliferative activity against human HeLa cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human HeLa cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
[PMID: 31103900]
HeLa IC50
18.02 μM
Compound: CI994
Antiproliferative activity against human HeLa cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human HeLa cells after 72 hrs by CCK-8 assay
[PMID: 29202397]
HeLa IC50
18.78 μM
Compound: CI994
Antiproliferative activity against human HeLa cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human HeLa cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 31003060]
HepG2 IC50
10 μM
Compound: 5; CI-994
Cytotoxicity in human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity in human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 28885834]
HepG2 IC50
18.5 μM
Compound: Tacedinaline
Antiproliferative activity against human HepG2 cells after 72 hrs CCK8 assay
Antiproliferative activity against human HepG2 cells after 72 hrs CCK8 assay
[PMID: 30108928]
HepG2 IC50
18.51 μM
Compound: 6; CI994
Antiproliferative activity against human HepG2 cells after 72 hrs by CCK-8 reagent based assay
Antiproliferative activity against human HepG2 cells after 72 hrs by CCK-8 reagent based assay
[PMID: 28391133]
LNCaP IC50
7.4 μM
Compound: 3, CI-994
Antiproliferative activity against human LNCap by MTT assay
Antiproliferative activity against human LNCap by MTT assay
[PMID: 18166465]
MCF7 IC50
13.16 μM
Compound: 2
Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay
[PMID: 30045621]
MDA-MB-231 GI50
0.17 μM
Compound: 1
Growth inhibition of human MDA-MB-231 cells after 5 days by MTT assay
Growth inhibition of human MDA-MB-231 cells after 5 days by MTT assay
[PMID: 18543902]
MGC-803 IC50
11.6 μM
Compound: CI994
Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 assay
[PMID: 29202397]
MGC-803 IC50
11.6 μM
Compound: 6; CI994
Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 reagent based assay
Antiproliferative activity against human MGC803 cells after 72 hrs by CCK-8 reagent based assay
[PMID: 28391133]
NCI-H1299 IC50
33.79 μM
Compound: CI994
Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK-8 assay
Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK-8 assay
[PMID: 29202397]
NCI-H1299 IC50
33.8 μM
Compound: Tacedinaline
Antiproliferative activity against human H1299 cells after 72 hrs CCK8 assay
Antiproliferative activity against human H1299 cells after 72 hrs CCK8 assay
[PMID: 30108928]
NCI-H1299 IC50
6.79 μM
Compound: 2
Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human NCI-H1299 cells after 72 hrs by CCK8 assay
[PMID: 30045621]
NCI-H460 IC50
9.7 μM
Compound: Tacedinaline
Antiproliferative activity against human H460 cells after 72 hrs CCK8 assay
Antiproliferative activity against human H460 cells after 72 hrs CCK8 assay
[PMID: 30108928]
NCI-H661 IC50
20 μM
Compound: CI-994
Antiproliferative activity against human NCI-H661 cells after 48 hrs
Antiproliferative activity against human NCI-H661 cells after 48 hrs
[PMID: 18692397]
NIH3T3 IC50
9.05 μM
Compound: CI994
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 48 hrs by CCK8 assay
[PMID: 31003060]
NIH3T3 IC50
9.05 μM
Compound: 5; CI994
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay
Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay
[PMID: 31103900]
PC-3 GI50
0.29 μM
Compound: 1
Growth inhibition of human PC3 cells after 5 days by MTT assay
Growth inhibition of human PC3 cells after 5 days by MTT assay
[PMID: 18543902]
Sf9 IC50
147 nM
Compound: 27; CI-994
Inhibition of recombinant human full length C-terminal FLAG-tagged HDAC2 expressed in Sf9 insect cells using FAM-labeled acetylated peptide A as substrate preincubated for 3 hrs followed by substrate addition and measured after 60 mins by fluorescence ass
Inhibition of recombinant human full length C-terminal FLAG-tagged HDAC2 expressed in Sf9 insect cells using FAM-labeled acetylated peptide A as substrate preincubated for 3 hrs followed by substrate addition and measured after 60 mins by fluorescence ass
[PMID: 30735902]
Sf9 IC50
41 nM
Compound: 27; CI-994
Inhibition of recombinant human full length C-terminal His/FALG-tagged HDAC1 expressed in Sf9 insect cells using FAM-labeled acetylated peptide A as substrate preincubated for 3 hrs followed by substrate addition and measured after 60 mins by fluorescence
Inhibition of recombinant human full length C-terminal His/FALG-tagged HDAC1 expressed in Sf9 insect cells using FAM-labeled acetylated peptide A as substrate preincubated for 3 hrs followed by substrate addition and measured after 60 mins by fluorescence
[PMID: 30735902]
SMMC-7721 IC50
> 32 μM
Compound: CI994
Antiproliferative activity against human SMMC7721 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
Antiproliferative activity against human SMMC7721 cells assessed as reduction in cell growth incubated for 72 hrs by CCK-8 assay
[PMID: 31003060]
SMMC-7721 IC50
14.06 μM
Compound: 5; CI994
Antiproliferative activity against human SMMC7721 cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
Antiproliferative activity against human SMMC7721 cells assessed as decrease in cell viability after 72 hrs by CCK-8 assay
[PMID: 31103900]
SMMC-7721 IC50
16.9 μM
Compound: Tacedinaline
Antiproliferative activity against human SMMC7721 cells after 72 hrs CCK8 assay
Antiproliferative activity against human SMMC7721 cells after 72 hrs CCK8 assay
[PMID: 30108928]
體外研究
(In Vitro)

Tacedinaline (N-acetyldinaline) 是一種新型口服化合物,在臨床前模型中具有廣譜抗腫瘤活性。作用機(jī)制可能涉及抑制組蛋白去乙酰化和細(xì)胞周期停滯。Tacedinaline (N-acetyldinaline) 與常用于非小細(xì)胞肺癌細(xì)胞系管理的抗腫瘤藥物聯(lián)合使用,在 Tacedinaline (N-acetyldinaline) (40 μM) 和吉西他濱 (0.01 μM) 在處理 48 和 72 小時(shí)[2]。
Tacedinaline (N-acetyldinaline) 抑制有絲分裂原刺激的血淋巴細(xì)胞增殖,IC50 值為 3 μM[4]

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

體內(nèi)研究
(In Vivo)

Tacedinaline (CI-994) 可在大鼠單次口服后 1 天內(nèi)影響淋巴組織,這種影響通常在 7 天內(nèi)可逆[4]

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

Clinical Trial
分子量

269.30

Formula

C15H15N3O2

CAS 號(hào)
性狀

固體

顏色

White to gray

中文名稱

乙酰地那林;他地那蘭

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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(shí)驗(yàn): 

DMSO 中的溶解度 : ≥ 50 mg/mL (185.67 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.7133 mL 18.5667 mL 37.1333 mL
5 mM 0.7427 mL 3.7133 mL 7.4267 mL
查看完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)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(dòng)物實(shí)驗(yàn):

請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)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(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

  • 方案 一

    請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.28 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。

    1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)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。
動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的動(dòng)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(guò) 2%。
方案所需 助溶劑 包括:DMSO, ,均可在 MCE 網(wǎng)站選購(gòu)。 ,Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)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(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)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(guò)半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
請(qǐng)確保第一步儲(chǔ)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: 99.32%

參考文獻(xiàn)
Animal Administration
[4]

Rats: To characterize the effects of Tacedinaline (CI-994) on lymphoid tissue, male rats are administered single oral doses at 0 (vehicle control), 10, 23, and 45 mg/kg and killed up to 7 days after dosing for evaluation of white blood cell differentials, bone marrow differentials, lymphoid tissue weights, and selected histopathology of lymphoid tissue[4].

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

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?年內(nèi)使用, -20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?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 3.7133 mL 18.5667 mL 37.1333 mL 92.8333 mL
5 mM 0.7427 mL 3.7133 mL 7.4267 mL 18.5667 mL
10 mM 0.3713 mL 1.8567 mL 3.7133 mL 9.2833 mL
15 mM 0.2476 mL 1.2378 mL 2.4756 mL 6.1889 mL
20 mM 0.1857 mL 0.9283 mL 1.8567 mL 4.6417 mL
25 mM 0.1485 mL 0.7427 mL 1.4853 mL 3.7133 mL
30 mM 0.1238 mL 0.6189 mL 1.2378 mL 3.0944 mL
40 mM 0.0928 mL 0.4642 mL 0.9283 mL 2.3208 mL
50 mM 0.0743 mL 0.3713 mL 0.7427 mL 1.8567 mL
60 mM 0.0619 mL 0.3094 mL 0.6189 mL 1.5472 mL
80 mM 0.0464 mL 0.2321 mL 0.4642 mL 1.1604 mL
100 mM 0.0371 mL 0.1857 mL 0.3713 mL 0.9283 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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