1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. Tucidinostat

Tucidinostat  (Synonyms: 西达本胺; Chidamide; HBI-8000; CS 055)

目录号: HY-109015 纯度: 98.60%
COA 产品使用指南

Tucidinostat (Chidamide) 是一种有效的,可口服的 HDAC 第 I 类 HDAC1/2/3 和第 IIb 类 HDAC10 的抑制剂,IC50 值分别为 95,160,67 和 78 nM,对 HDAC8HDAC11 的作用较弱 (IC50,733 nM,432 nM),对 HDAC4/5/6/7/9 无作用。

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Tucidinostat Chemical Structure

Tucidinostat Chemical Structure

CAS No. : 1616493-44-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥770
In-stock
5 mg ¥700
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10 mg ¥1100
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25 mg ¥2000
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50 mg ¥3200
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100 mg ¥4813
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Customer Review

Other Forms of Tucidinostat:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tucidinostat (Chidamide) is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9[1].

IC50 & Target[1]

HDAC3

67 nM (IC50)

HDAC10

78 nM (IC50)

HDAC1

95 nM (IC50)

HDAC2

160 nM (IC50)

HDAC11

432 nM (IC50)

HDAC8

733 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
786-0 IC50
0.63 μM
Compound: chidamide
Antiproliferative activity against human 786-O cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human 786-O cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
A549 IC50
2.79 μM
Compound: chidamide
Antiproliferative activity against human A549 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human A549 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
CCRF-CEM IC50
0.63 μM
Compound: Chidamide
Cytotoxicity against human CCRF-CEM cells by MTT assay
Cytotoxicity against human CCRF-CEM cells by MTT assay
[PMID: 31078410]
CCRF-CEM IC50
0.83 μM
Compound: chidamide
Antiproliferative activity against human CCRF-CEM cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human CCRF-CEM cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
CCRF-CEM IC50
1 μM
Compound: Chidamide
Cytotoxicity against human CCRF-CEM cells measured after 72 hrs by MTT assay
Cytotoxicity against human CCRF-CEM cells measured after 72 hrs by MTT assay
[PMID: 34986303]
COLO-678 IC50
> 10 μM
Compound: chidamide
Antiproliferative activity against human COLO-678 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human COLO-678 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
CWR22R IC50
1.08 μM
Compound: chidamide
Antiproliferative activity against human 22Rv1 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human 22Rv1 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
DOHH-2 IC50
0.53 μM
Compound: chidamide
Antiproliferative activity against human DOHH-2 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human DOHH-2 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
EBC-1 IC50
2.9 μM
Compound: CS-055
Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay
Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay
[PMID: 28835797]
HCT-116 IC50
> 20 μM
Compound: 1; CS055, HBI-8000
Antiproliferative activity against human HCT116 cells NAMPT deficient assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human HCT116 cells NAMPT deficient assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31938461]
HCT-116 IC50
0.34 μM
Compound: 1; CS055, HBI-8000
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31938461]
HCT-116 IC50
1.09 μM
Compound: HBI-8000; CS055
Antiproliferative activity against human HCT116 assessed as reduction in cell viability measured after 72 hrs using alamar blue based fluorescence method
Antiproliferative activity against human HCT116 assessed as reduction in cell viability measured after 72 hrs using alamar blue based fluorescence method
[PMID: 30802729]
HCT-116 IC50
2.08 μM
Compound: Chidamide
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by luminescence based analysis
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by luminescence based analysis
[PMID: 35649291]
HCT-116 IC50
2.08 μM
Compound: chidamide
Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
HCT-116 IC50
2.082 μM
Compound: Chidamide
Antiproliferative activity against human HCT-116 cells assessed as cell viability at 1 uM incubated for 72 hrs by luminescence assay
Antiproliferative activity against human HCT-116 cells assessed as cell viability at 1 uM incubated for 72 hrs by luminescence assay
[PMID: 34995925]
HCT-116 IC50
7.8 μM
Compound: CS-055
Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay
Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay
[PMID: 28835797]
HEL IC50
0.013 μM
Compound: 1; CS055, HBI-8000
Antiproliferative activity against human HEL cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human HEL cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31938461]
HEL IC50
1.8 μM
Compound: 1; CS055, HBI-8000
Antiproliferative activity against human HEL cells NAMPT deficient assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human HEL cells NAMPT deficient assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31938461]
HeLa IC50
7.16 μM
Compound: CS055, Epidaza
Inhibition of HDAC in human HeLa cell extract incubated for 1 hr by colorimetric activity assay
Inhibition of HDAC in human HeLa cell extract incubated for 1 hr by colorimetric activity assay
10.1039/C4MD00350K
HepG2 IC50
2 μM
Compound: Chidamide
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by luminescence based analysis
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by luminescence based analysis
[PMID: 35649291]
HepG2 IC50
4.89 μM
Compound: 2
Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay
[PMID: 31053508]
HL-60 IC50
0.0022 μM
Compound: 1; CS055, HBI-8000
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31938461]
HL-60 IC50
1.97 μM
Compound: HBI-8000; CS055
Antiproliferative activity against human HL60 assessed as reduction in cell viability measured after 72 hrs using alamar blue based fluorescence method
Antiproliferative activity against human HL60 assessed as reduction in cell viability measured after 72 hrs using alamar blue based fluorescence method
[PMID: 30802729]
HL-60 IC50
3.2 μM
Compound: 1; CS055, HBI-8000
Antiproliferative activity against human HL60 cells NAMPT deficient assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human HL60 cells NAMPT deficient assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31938461]
HT-29 IC50
6.04 μM
Compound: chidamide
Antiproliferative activity against human HT-29 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human HT-29 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
HuT78 IC50
2.42 μM
Compound: chidamide
Antiproliferative activity against human HuT78 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human HuT78 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
K562 IC50
0.32 μM
Compound: 1; CS055, HBI-8000
Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31938461]
K562 IC50
0.747 μM
Compound: HBI-8000; CS055
Antiproliferative activity against human K562 assessed as reduction in cell viability measured after 72 hrs using alamar blue based fluorescence method
Antiproliferative activity against human K562 assessed as reduction in cell viability measured after 72 hrs using alamar blue based fluorescence method
[PMID: 30802729]
K562 IC50
0.87 μM
Compound: 2
Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay
[PMID: 31053508]
K562 IC50
1.34 μM
Compound: Chidamide
Cytotoxicity against human K562 cells by MTT assay
Cytotoxicity against human K562 cells by MTT assay
[PMID: 31078410]
K562 IC50
2.4 μM
Compound: 1; CS055, HBI-8000
Antiproliferative activity against human K562 cells NAMPT deficient assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human K562 cells NAMPT deficient assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31938461]
K562 IC50
8.3 μM
Compound: Chidamide
Cytotoxicity against human K562 cells measured after 72 hrs by MTT assay
Cytotoxicity against human K562 cells measured after 72 hrs by MTT assay
[PMID: 34986303]
MCF7 IC50
29.07 μM
Compound: HBI-8000; CS055
Antiproliferative activity against human MCF7 assessed as reduction in cell viability measured after 72 hrs using alamar blue based fluorescence method
Antiproliferative activity against human MCF7 assessed as reduction in cell viability measured after 72 hrs using alamar blue based fluorescence method
[PMID: 30802729]
MDA-MB-231 IC50
9.52 μM
Compound: chidamide
Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
MDA-MB-468 IC50
2.65 μM
Compound: 2
Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs by MTT assay
[PMID: 31053508]
MOLT-4 IC50
0.75 μM
Compound: chidamide
Antiproliferative activity against human MOLT-4 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human MOLT-4 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
MV4-11 IC50
0.783 μM
Compound: Chidamide
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by luminescence based analysis
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by luminescence based analysis
[PMID: 35649291]
MV4-11 IC50
3.73 μM
Compound: 2
Antiproliferative activity against human MV4-11 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human MV4-11 cells measured after 48 hrs by MTT assay
[PMID: 31053508]
NCI-H441 IC50
2.62 μM
Compound: chidamide
Antiproliferative activity against human NCI-H441 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human NCI-H441 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
NCI-H460 IC50
2.34 μM
Compound: chidamide
Antiproliferative activity against human NCI-H460 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human NCI-H460 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
Rec1 IC50
1.01 μM
Compound: chidamide
Antiproliferative activity against human REC1 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human REC1 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
RS4-11 IC50
0.6 μM
Compound: chidamide
Antiproliferative activity against human RS4-11 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human RS4-11 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
Sf9 IC50
0.167 μM
Compound: 2
Inhibition of recombinant full-length human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using Fluor-de-Lys as substrate measured after 10 mins by fluorescence assay
Inhibition of recombinant full-length human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using Fluor-de-Lys as substrate measured after 10 mins by fluorescence assay
[PMID: 31053508]
SK-OV-3 IC50
8.46 μM
Compound: chidamide
Antiproliferative activity against human SK-OV-3 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human SK-OV-3 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
SU-DHL-2 IC50
0.56 μM
Compound: chidamide
Antiproliferative activity against human SUDHL2 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human SUDHL2 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
TMD8 IC50
0.48 μM
Compound: chidamide
Antiproliferative activity against human TMD8 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human TMD8 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
U-937 IC50
3.3 μM
Compound: Chidamide
Cytotoxicity against human U-937 cells measured after 72 hrs by MTT assay
Cytotoxicity against human U-937 cells measured after 72 hrs by MTT assay
[PMID: 34986303]
体外研究
(In Vitro)

Tucidinostat (Chidamide/CS055/HBI -8000) 是一种有效的口服生物可利用的 HDAC 酶 I 类 (HDAC1,2,3) 和 IIb 类 (HDAC10) 抑制剂,IC50 为 95,160,67 和 78 nM,对 HDAC8HDAC11 的活性较低 (IC50,分别为 733 nM,432 nM),对 HDAC4/5/6/7/9 没有影响 (IC50,>30 μM)。Tucidinostat 具有强大的抗肿瘤活性,可抑制多种人源性肿瘤细胞系,例如 HL-60、U2OS、LNCaP,GI50s 分别为 0.4 ± 0.1、2.0 ± 0.6 和 4.0 ± 1.2 μM。此外,Tucidinostat 对人胎肾 (CCC-HEK) 和肝 (CCCHEL) 的正常细胞显示出较低的毒性[1]

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

体内研究
(In Vivo)

Tucidinostat (12.5-50 mg/kg,po) 在荷有 HCT-8 结直肠癌、A549 肺癌、BEL-7402 肝癌和 MCF-7 乳腺癌的小鼠中剂量依赖性地减小肿瘤大小和肿瘤重量,并且没有明显的身体损失[1]

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

Clinical Trial
分子量

390.41

Formula

C22H19FN4O2

CAS 号
性状

固体

颜色

White to off-white

中文名称

西达本胺

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (128.07 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

Ethanol 中的溶解度 : 1 mg/mL (2.56 mM; 超声助溶 (<60°C))

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5614 mL 12.8070 mL 25.6141 mL
5 mM 0.5123 mL 2.5614 mL 5.1228 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用
以下溶剂前显示的百分比是指该溶剂在您配制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

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.40 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

    生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.40 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
请输入您的动物体内配方组成:
%
DMSO +
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
连续给药周期超过半月以上,请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 98.60%

参考文献

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.5614 mL 12.8070 mL 25.6141 mL 64.0352 mL
DMSO 5 mM 0.5123 mL 2.5614 mL 5.1228 mL 12.8070 mL
10 mM 0.2561 mL 1.2807 mL 2.5614 mL 6.4035 mL
15 mM 0.1708 mL 0.8538 mL 1.7076 mL 4.2690 mL
20 mM 0.1281 mL 0.6404 mL 1.2807 mL 3.2018 mL
25 mM 0.1025 mL 0.5123 mL 1.0246 mL 2.5614 mL
30 mM 0.0854 mL 0.4269 mL 0.8538 mL 2.1345 mL
40 mM 0.0640 mL 0.3202 mL 0.6404 mL 1.6009 mL
50 mM 0.0512 mL 0.2561 mL 0.5123 mL 1.2807 mL
60 mM 0.0427 mL 0.2135 mL 0.4269 mL 1.0673 mL
80 mM 0.0320 mL 0.1601 mL 0.3202 mL 0.8004 mL
100 mM 0.0256 mL 0.1281 mL 0.2561 mL 0.6404 mL
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  • 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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产品名称:
Tucidinostat
目录号:
HY-109015
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