Tucidinostat (Chidamide)

Catalog No.S8567 Batch:S856704

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Technical Data

Formula

C22H19FN4O2
Molecular Weight 390.41 CAS No. 1616493-44-7
Solubility (25°C)* In vitro DMSO 78 mg/mL (199.78 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5% DMSO 95% corn oil
0.5mg/ml 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. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.0mg/ml 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. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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.
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 (from reference)

Cell Assay:

[1]
  • 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).
Animal Study:

[1]
  • Animal Models

    Athymic nude mice (BALB/c-nu)

  • Dosages

    12.5-50 mg/kg

  • Administration

    oral

Selleck's Tucidinostat (Chidamide) has been cited by 20 publications

CYLD induces high oxidative stress and DNA damage through class I HDACs to promote radiosensitivity in nasopharyngeal carcinoma [ Cell Death Dis, 2024, 15(1):95] PubMed: 38287022
IKAROS expression drives the aberrant metabolic phenotype of macrophages in chronic HIV infection [ Clin Immunol, 2024, 260:109915] PubMed: 38286172
Synergistic effect of HDAC inhibitor Chidamide with Cladribine on cell cycle arrest and apoptosis by targeting HDAC2/c-Myc/RCC1 axis in acute myeloid leukemia [ Exp Hematol Oncol, 2023, 12(1):23] PubMed: 36849955
Preclinical development and evaluation of nanobody-based CD70-specific CAR T cells for the treatment of acute myeloid leukemia [ Cancer Immunol Immunother, 2023, 10.1007/s00262-023-03422-6] PubMed: 36932256
Low-Dose Chidamide Treatment Displays Sex-Specific Differences in the 3xTg-AD Mouse [ Biomolecules, 2023, 10.3390/biom13091324] PubMed: 37759724
Low-Dose Chidamide Treatment Displays Sex-Specific Differences in the 3xTg-AD Mouse [ Biomolecules, 2023, 13(9)1324] PubMed: 37759724
Single-cell profiling-guided combination therapy of c-Fos and histone deacetylase inhibitors in diffuse large B-cell lymphoma [ Clin Transl Med, 2022, 12(5):e798] PubMed: 35522945
HDAC1/3-dependent moderate liquid-liquid phase separation of YY1 promotes METTL3 expression and AML cell proliferation [ Cell Death Dis, 2022, 13(11):992] PubMed: 36424383
Targeting Class I Histone Deacetylases in Human Uterine Leiomyosarcoma [ Cells, 2022, 11(23)3801] PubMed: 36497061
A dual SHOX2:GFP; MYH6:mCherry knockin hESC reporter line for derivation of human SAN-like cells [ iScience, 2022, 25(4):104153] PubMed: 35434558

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.