Tucidinostat (Chidamide)

Catalog No.S8567 Synonyms: HBI-8000, CS-055

Tucidinostat (Chidamide) Chemical Structure

Molecular Weight(MW): 390.41

Chidamide 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.

Size Price Stock Quantity  
USD 97 In stock
USD 247 In stock
USD 647 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

Description Chidamide 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.
Targets
HDAC3 [1]
(Cell-free)
HDAC10 [1]
(Cell-free)
HDAC1 [1]
(Cell-free)
HDAC2 [1]
(Cell-free)
67 nM 78 nM 95 nM 160 nM
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].

Assay
Methods Test Index PMID
Western blot
PARP / Cleaved PARP / Caspase-3 / Cleaved caspase-3 ; 

PubMed: 30854137     


Expression and activation level of Caspase-3 and PARP after treatment of serial dilutions of chidamide in HCC827 cells (48h).

p-EGFR / EGFR / p-STAT3 / STAT3 / p-AKT / AKT / p-AMPK / MAPK ; 

PubMed: 30854137     


Chidamide inhibition of PTK signaling molecules in A549 cells (48h).

Ace-H3K18 / Ace-H3K9 / Ac-H4K8 ; 

PubMed: 29773595     


Western blot analysis of H3 acetylation at Lys18 and Lys9 and H4 acetylation at Lys8. H3 and H4 expression levels were used as loading controls. 

Mcl-1 / Myc / Bcl-xl / p21 / p27 / CDK6 / CDK4 / Cyclin D2 ; 

PubMed: 29773595     


Western blot analysis of Mcl-1, Myc, Bcl-xL, Bcl-2, p21, p27, CDK4, CDK6, and Cyclin-D2 levels; α-tubulin was used as the loading control. 

HDAC1 / HDAC2 / HDAC3 / acetyl-H3 / acetyl-H4 ; 

PubMed: 31289512     


(A) RPMI8226 cells were treated with 0, 0.5, 1 or 2 µmol/l chidamide for 48 h and (B) U266 cells were treated with 0, 2, 4 or 8 µmol/l chidamide for 48 h, and HDACs expression was assessed using western blot analysis.

30854137 29773595 31289512
Growth inhibition assay
Cell viability; 

PubMed: 29100410     


(a) Proliferation rates at 24, 48, 72 hour of Hs445 cells after treated with 0.1μM, 0.3μM, 1μM, 3μM, 10μM, 30μM Chidamides; (b) proliferation rates at 24, 48, 72 hours of L428 cells after treated with 0.1μM, 0.3μM, 1μM, 3μM, 10μM, 30μM Chidamide;

29100410
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

Cell Research:

[1]

+ Expand
  • Cell lines: PBMC effector cells
  • Concentrations: 0-400 nM
  • Incubation Time: 0-400 nM
  • Method:

    Isolated PBMC effector cells are seeded into 6-well plates (6 x 106 cells/well) and treated with chidamide at different concentrations (0-400 nM) for different times (24-72 h).


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Athymic nude mice (BALB/c-nu)
  • Formulation: 0.2% carboxymethyl cellulose (CMC) and 0.1% Tween 80
  • Dosages: 12.5-50 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (199.78 mM)
Ethanol 2 mg/mL (5.12 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% CMC Na
For best results, use promptly after mixing.
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 powder
in solvent
Synonyms HBI-8000, CS-055

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03820596 Recruiting Drug: Sintilimab|Drug: Chidamide Safety and Efficacy Huiqiang Huang|Sun Yat-sen University February 12 2019 Phase 1|Phase 2
NCT02944812 Unknown status Drug: Chidamide Peripheral T Cell Lymphoma Guangdong General Hospital March 2016 Phase 2
NCT02569489 Withdrawn Drug: HBI-8000|Drug: Trastuzumab|Drug: Paclitaxel Breast Cancer HUYA Bioscience International December 2015 Phase 1
NCT02513901 Completed Drug: Chidamide Chronic HIV Infections Tang-Du Hospital|Chipscreen Biosciences Ltd. August 2015 Phase 1|Phase 2
NCT02482753 Active not recruiting Drug: Chidamide|Drug: exemestane|Drug: placebo Breast Cancer Chipscreen Biosciences Ltd. July 2015 Phase 3
NCT02697552 Completed Drug: HBI-8000 Non-Hodgkin''s Lymphoma HUYA Bioscience International March 2014 Phase 1

Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

HDAC Signaling Pathway Map

Related HDAC Products

Tags: buy Tucidinostat (Chidamide) | Tucidinostat (Chidamide) supplier | purchase Tucidinostat (Chidamide) | Tucidinostat (Chidamide) cost | Tucidinostat (Chidamide) manufacturer | order Tucidinostat (Chidamide) | Tucidinostat (Chidamide) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID