Tucidinostat (Chidamide)

别名: HBI-8000, CS-055

Tucidinostat (Chidamide, HBI-8000, CS-055) 是HDAC1, 2, 3, 10的低摩尔浓度抑制剂,IC50分别为95、160、67、78 nM。

Tucidinostat (Chidamide) Chemical Structure

Tucidinostat (Chidamide) Chemical Structure

CAS: 1616493-44-7

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 794.43 现货
5mg RMB 795.33 现货
25mg RMB 2023.28 现货
100mg RMB 5299.86 现货
1g RMB 7944.3 现货
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产品质控

批次: 纯度: 99.99%
99.99

Tucidinostat (Chidamide)相关产品

相关信号通路图

HDAC抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
U2OS Function assay 1 uM 24 hrs Activation of PPARG (unknown origin) expressed in human U2OS cells at 1 uM in presence of 10 uM rosiglitazone incubated for 24 hrs by luciferase reporter gene assay ChEMBL
U2OS Function assay 1 uM 24 hrs Activation of ERbeta (unknown origin) expressed in human U2OS cells at 1 uM in presence of 0.01 uM E2 incubated for 24 hrs by luciferase reporter gene assay ChEMBL
U2OS Function assay 1 uM 24 hrs Activation of glulcocorticoid receptor (unknown origin) expressed in human U2OS cells at 1 uM in presence of 0.1 uM dexamethasone incubated for 24 hrs by luciferase reporter gene assay ChEMBL
U2OS Function assay 1 uM 24 hrs Activation of ERalpha (unknown origin) expressed in human U2OS cells at 1 uM in presence of 0.01 uM E2 incubated for 24 hrs by luciferase reporter gene assay ChEMBL
U2OS Function assay 1 uM 24 hrs Activation of glulcocorticoid receptor (unknown origin) expressed in human U2OS cells at 1 uM incubated for 24 hrs by luciferase reporter gene assay ChEMBL
U2OS Function assay 1 uM 24 hrs Activation of PPARG (unknown origin) expressed in human U2OS cells at 1 uM incubated for 24 hrs by luciferase reporter gene assay ChEMBL
U2OS Function assay 1 uM 24 hrs Activation of ERalpha (unknown origin) expressed in human U2OS cells at 1 uM incubated for 24 hrs by luciferase reporter gene assay ChEMBL
U2OS Function assay 1 uM 24 hrs Activation of ERbeta (unknown origin) expressed in human U2OS cells at 1 uM incubated for 24 hrs by luciferase reporter gene assay ChEMBL
Sf9 Function assay 5 mins Inhibition of recombinant human full length HDAC1 expressed in baculovirus infected Sf9 insect cells using biotinylated lysine 9 acetylated histone H3 (1 to 21 residues) as substrate incubated for 5 mins followed by substrate addition measured after 60 mi, IC50 = 0.112 μM. 28835797
EBC1 Antiproliferative assay 72 hrs Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay, IC50 = 2.9 μM. 28835797
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay, IC50 = 7.8 μM. 28835797
HL60 Growth inhibition assay 48 hrs Growth inhibition of human HL60 cells incubated for 48 hrs by MTS method, GI50 = 0.4 μM. ChEMBL
Jurkat Growth inhibition assay 48 hrs Growth inhibition of human Jurkat cells incubated for 48 hrs by MTS method, GI50 = 1.5 μM. ChEMBL
U2OS Growth inhibition assay 48 hrs Growth inhibition of human U2OS cells incubated for 48 hrs by MTS method, GI50 = 2 μM. ChEMBL
HepG2 Growth inhibition assay 48 hrs Growth inhibition of human HepG2 cells incubated for 48 hrs by MTS method, GI50 = 4 μM. ChEMBL
LNCAP Growth inhibition assay 48 hrs Growth inhibition of human LNCAP cells incubated for 48 hrs by MTS method, GI50 = 4 μM. ChEMBL
Raji Growth inhibition assay 48 hrs Growth inhibition of human Raji cells incubated for 48 hrs by MTS method, GI50 = 4 μM. ChEMBL
MCF7 Growth inhibition assay 48 hrs Growth inhibition of human MCF7 cells incubated for 48 hrs by MTS method, GI50 = 5 μM. ChEMBL
28SC Growth inhibition assay 48 hrs Growth inhibition of human 28SC cells incubated for 48 hrs by MTS method, GI50 = 5.8 μM. ChEMBL
PANC1 Growth inhibition assay 48 hrs Growth inhibition of human PANC1 cells incubated for 48 hrs by MTS method, GI50 = 6.3 μM. ChEMBL
HeLa Function assay 10 mins Inhibition of HDAC enzymatic activity in human HeLa cells incubated for 10 mins in presence of substrate by colorimetric activity assay, IC50 = 7.2 μM. ChEMBL
MDA-MB-231 Growth inhibition assay 48 hrs Growth inhibition of human MDA-MB-231 cells incubated for 48 hrs by MTS method, GI50 = 7.9 μM. ChEMBL
SMMC7721 Growth inhibition assay 48 hrs Growth inhibition of human SMMC7721 cells incubated for 48 hrs by MTS method, GI50 = 16 μM. ChEMBL
DU145 Growth inhibition assay 48 hrs Growth inhibition of human DU145 cells incubated for 48 hrs by MTS method, GI50 = 25 μM. ChEMBL
HeLa Growth inhibition assay 48 hrs Growth inhibition of human HeLa cells incubated for 48 hrs by MTS method, GI50 = 40 μM. ChEMBL
hematopoietic malignant cells Cytotoxicity assay Cytotoxicity against human hematopoietic malignant cells assessed as growth inhibition, GI50 = 1.86 μM. ChEMBL
human solid tumor cells Cytotoxicity assay Cytotoxicity against human solid tumor cells assessed as growth inhibition, GI50 = 6.65 μM. ChEMBL
点击查看更多细胞系数据

生物活性

产品描述 Tucidinostat (Chidamide, HBI-8000, CS-055) 是HDAC1, 2, 3, 10的低摩尔浓度抑制剂,IC50分别为95、160、67、78 nM。
靶点
HDAC3 [1]
(Cell-free)
HDAC10 [1]
(Cell-free)
HDAC1 [1]
(Cell-free)
HDAC2 [1]
(Cell-free)
67 nM 78 nM 95 nM 160 nM
体外研究(In Vitro)
体外研究活性 Chidamide抑制I型HDACs 1-3,以及IIb型HDAC10。在人类宫颈腺癌Hela细胞和人源PBMC细胞中,Chidamide显著地诱导组蛋白H3乙酰化。在微摩尔浓度范围内,Chidamide和MS-275可抑制大多数人源肿瘤细胞系的细胞生长,但并不是所有所检测的肿瘤细胞(共检测18种)。在人胚肾(CCC-HEK)和人胚肝(CCC-HEL)中,Chidamide对正常细胞的毒性作用比MS-275大大减少,说明Chidamide对正常细胞和癌细胞的细胞毒性作用的差异[1]
细胞实验 细胞系 PBMC效应细胞
浓度 0-400 nM
孵育时间 24-72 h
方法

将分离的PBMC效应细胞接种于6孔板(细胞密度为6 x 106 cells/孔),用不同浓度的chidamide(0-400 nM)处理细胞一定时间(24-72 h)。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot PARP / Cleaved PARP / Caspase-3 / Cleaved caspase-3 p-EGFR / EGFR / p-STAT3 / STAT3 / p-AKT / AKT / p-AMPK / MAPK Ace-H3K18 / Ace-H3K9 / Ac-H4K8 Mcl-1 / Myc / Bcl-xl / p21 / p27 / CDK6 / CDK4 / Cyclin D2 HDAC1 / HDAC2 / HDAC3 / acetyl-H3 / acetyl-H4 30854137
Growth inhibition assay Cell viability 29100410
体内研究(In Vivo)
体内研究活性 在小鼠结肠癌HCT-8移植瘤模型中,Chidamide具有体内抗肿瘤活性。给药浓度范围为12.5-50 mg/kg的Chidamide可浓度依赖性地减少肿瘤大小和重量。Chidamide的给药浓度为50 mg/kg时,相较于对照药物组5-FU(20 mg/kg)和MS-275组(25 mg/kg)具有相似甚至更大的功效。在携瘤动物模型中,Chidamide耐受良好[1]
动物实验 Animal Models Athymic nude mice (BALB/c-nu)
Dosages 12.5-50 mg/kg
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05586841 Not yet recruiting
HR+/HER2- Advanced Breast Cancer
Beijing 302 Hospital
November 1 2022 Phase 1
NCT05141357 Terminated
Non Small Cell Lung Cancer
HUYABIO International LLC.
March 14 2022 Phase 2
NCT04994210 Recruiting
Safety and Efficacy
Sun Yat-sen University
October 4 2021 Phase 2
NCT05140616 Recruiting
Safety and Efficacy
The First Affiliated Hospital of Soochow University
May 31 2021 Phase 1|Phase 2
NCT04651127 Unknown status
Cervical Cancer|Cervix Cancer|Cervix Neoplasm
Sun Yat-sen University
November 9 2020 Phase 1|Phase 2

化学信息&溶解度

分子量 390.41 分子式

C22H19FN4O2

CAS号 1616493-44-7 SDF Download Tucidinostat (Chidamide) SDF
Smiles C1=CC(=CN=C1)C=CC(=O)NCC2=CC=C(C=C2)C(=O)NC3=C(C=C(C=C3)F)N
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 78 mg/mL ( (199.78 mM); DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 1 mg/mL

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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