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Tucidinostat (Chidamide)
別名: HBI-8000, CS-055 中文名稱：西達本胺
Tucidinostat (Chidamide, HBI-8000, CS-055) 是HDAC1, 2, 3, 10的低摩爾濃度抑制劑，IC50分別為95、160、67、78 nM。
Tucidinostat (Chidamide) Chemical Structure
CAS: 1616493-44-7
產(chǎn)品質(zhì)控
批次：
純度：
99.99%
99.99
Tucidinostat (Chidamide)相關(guān)產(chǎn)品
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Tucidinostat (Chidamide, HBI-8000, CS-055) 是HDAC1, 2, 3, 10的低摩爾濃度抑制劑，IC50分別為95、160、67、78 nM。 | ||||||||
|---|---|---|---|---|---|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | Chidamide抑制I型HDACs 1-3，以及IIb型HDAC10。在人類宮頸腺癌Hela細胞和人源PBMC細胞中，Chidamide顯著地誘導(dǎo)組蛋白H3乙酰化。在人胚腎（CCC-HEK）和人胚肝（CCC-HEL）中，Chidamide對正常細胞的毒性作用比MS-275大大減少，說明Chidamide對正常細胞和癌細胞的細胞毒性作用的差異[1]。 |
|||
|---|---|---|---|---|
| 細胞實驗 | 細胞系 | PBMC效應(yīng)細胞 | ||
| 濃度 | 0-400 nM | |||
| 孵育時間 | 24-72 h | |||
| 方法 | 將分離的PBMC效應(yīng)細胞接種于6孔板（細胞密度為6 x 106 cells/孔），用不同濃度的chidamide(0-400 nM)處理細胞一定時間（24-72 h）。 |
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| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | PMID |
| Western blot | HDAC1 / HDAC2 / HDAC3 / acetyl-H3 / acetyl-H4 Mcl-1 / Myc / Bcl-xl / p21 / p27 / CDK6 / CDK4 / Cyclin D2 Ace-H3K18 / Ace-H3K9 / Ac-H4K8 p-EGFR / EGFR / p-STAT3 / STAT3 / p-AKT / AKT / p-AMPK / MAPK PARP / Cleaved PARP / Caspase-3 / Cleaved caspase-3 |
|
31289512 | |
| Growth inhibition assay | Cell viability |
|
29100410 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 在小鼠結(jié)腸癌HCT-8移植瘤模型中，Chidamide具有體內(nèi)抗腫瘤活性。給藥濃度范圍為12.5-50 mg/kg的Chidamide可濃度依賴性地減少腫瘤大小和重量。Chidamide的給藥濃度為50 mg/kg時，相較于對照藥物組5-FU（20 mg/kg）和MS-275組（25 mg/kg）具有相似甚至更大的功效。在攜瘤動物模型中，Chidamide耐受良好[1]。 |
|
|---|---|---|
| 動物實驗 | 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 |
化學(xué)信息&溶解度
| 分子量 | 390.41 | 分子式 | C22H19FN4O2 |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 78 mg/mL ( (199.78 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 1 mg/mL (2.56 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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