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Tucidinostat (Chidamide)
Catalog No.S8567 Synonyms: HBI-8000, CS-055
For research use only.
Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.
CAS No. 1616493-44-7
Selleck's Tucidinostat (Chidamide) has been cited by 9 Publications
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Biological Activity
| Description | Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| Targets |
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| In vitro |
Chidamide inhibits class I HDACs 1-3, as well as class IIb HDAC10, at low nanomolar concentrations. Chidamide significantly induces histone H3 acetylation in both HeLa human cervical adenocarcinoma cells and human PBMC. Cell growth inhibition studies performed with 18 human-derived tumor cell lines demonstrate that chidamide and MS-275 similarly inhibit the in vitro growth of most, but not all, tumor cells in the low micromolar concentration range. However, chidamide, and to a lesser extent MS-275, is significantly less toxic to normal cells from human fetal kidney (CCC-HEK) and liver (CCC-HEL), indicating a differential cytotoxic response of normal cells versus cancerous cells to chidamide[1]. |
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| Cell Data |
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| Assay |
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| In vivo | In HCT-8 colorectal carcinoma mice xenografts, Chidamide shows in vivo antitumor activity. Chidamide in the dose range of 12.5-50 mg/kg dose-dependently reduces tumor size and tumor weight, and the dose of 50 mg/kg produces similar or greater efficacy compared with the control drugs 5-fluorouracil(5-FU, 20 mg/kg) and MS-275 (25 mg/kg, which was reported as the maximum tolerated dose in xenograft models). However, chidamide is well-tolerated at the above doses in the tumor-bearing animals, whereas the control drugs cause significant weight loss[1]. |
Protocol (from reference)
| Cell Research: |
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|---|---|
| Animal Research: |
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Solubility (25°C)
|
In vitro |
DMSO |
78 mg/mL
(199.78 mM) |
| Ethanol |
2 mg/mL
(5.12 mM) |
|
| Water |
Insoluble
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|
|
In vivo |
Add solvents to the product individually and in order |
30mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 390.41 | ||
|---|---|---|---|
| Formula | C22H19FN4O2 |
||
| CAS No. | 1616493-44-7 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | C1=CC(=CN=C1)C=CC(=O)NCC2=CC=C(C=C2)C(=O)NC3=C(C=C(C=C3)F)N | ||
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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g
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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.
Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT05141357 | Not yet recruiting | Drug: HBI-8000 in combination with pembrolizumab | Non Small Cell Lung Cancer | HUYABIO International LLC. | December 2021 | Phase 2 |
| NCT04994210 | Not yet recruiting | Drug: Sintilimab|Drug: Chidamide | Safety and Efficacy | Sun Yat-sen University | September 1 2021 | Phase 2 |
| NCT05140616 | Recruiting | Drug: Chidamide | Safety and Efficacy | The First Affiliated Hospital of Soochow University | May 31 2021 | Phase 1|Phase 2 |
| NCT04651127 | Recruiting | Drug: Toripalimab + Chidamide | Cervical Cancer|Cervix Cancer|Cervix Neoplasm | Sun Yat-sen University | November 9 2020 | Phase 1|Phase 2 |
| NCT03820596 | Recruiting | Drug: Sintilimab|Drug: Chidamide | Safety and Efficacy | Huiqiang Huang|Sun Yat-sen University | March 29 2019 | Phase 1|Phase 2 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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