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.

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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].

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 10<sup>6</sup> 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 individually and in order:
1% CMC Na
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. 743420-02-2
Storage powder
in solvent
Synonyms HBI-8000, CS-055

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID