Tucidinostat (Chidamide)
别名: HBI-8000, CS-055 中文名称：
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
CAS: 1616493-44-7
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
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 |
|
| 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]。 |
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|---|---|---|---|---|
| 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 |
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 (2.56 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 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
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
只
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，注：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：取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：取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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