Name: Tucidinostat (Chidamide)
Brand: Selleck Chemicals
SKU: S8567
Availability: InStock
Rating: 5 (31 reviews)

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	JAK BET Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other HDAC Products	Entinostat (MS-275) Trichostatin A (TSA) RGFP966 Tubastatin A Quisinostat (JNJ-26481585) Dihydrochloride Tubastatin A HCl Fimepinostat (CUDC-907) Givinostat (ITF-2357) Hydrochloride Monohydrate Mocetinostat (MGCD0103) Ricolinostat (ACY-1215)

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
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
hematopoietic malignant cells	Cytotoxicity assay			Cytotoxicity against human hematopoietic malignant cells assessed as growth inhibition, GI50 = 1.86 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
human solid tumor cells	Cytotoxicity assay			Cytotoxicity against human solid tumor cells assessed as growth inhibition, GI50 = 6.65 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
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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (199.78 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.000mg/ml (5.12mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (1.28mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	390.41	Formula	C₂₂H₁₉FN₄O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1616493-44-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	HBI-8000, CS-055			Smiles	C1=CC(=CN=C1)C=CC(=O)NCC2=CC=C(C=C2)C(=O)NC3=C(C=C(C=C3)F)N

Mechanism of Action

Targets/IC₅₀/Ki	HDAC3 (Cell-free) 67 nM HDAC10 (Cell-free) 78 nM HDAC1 (Cell-free) 95 nM HDAC2 (Cell-free) 160 nM
In vitro	Tucidinostat (Chidamide) inhibits class I HDACs 1-3, as well as class IIb HDAC10, at low nanomolar concentrations. It 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 this compound and MS-275 similarly inhibit the in vitro growth of most, but not all, tumor cells in the low micromolar concentration range. However, it, 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.
In vivo	In HCT-8 colorectal carcinoma mice xenografts, Tucidinostat (Chidamide) shows in vivo antitumor activity. However, it is well-tolerated at the above doses in the tumor-bearing animals, whereas the control drugs cause significant weight loss.
References	[1] https://pubmed.ncbi.nlm.nih.gov/22080169/

Applications

Methods	Biomarkers	Images	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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

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Tucidinostat (Chidamide) HDAC inhibitor

Chemical Structure

Molecular Weight: 390.41