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In vitro: Tucidinostat (Chidamide) inhibits class I HDACs 1-3, as well as class IIb HDAC10, at low nanomolar concentrations. Tucidinostat (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.
In vivo: In HCT-8 colorectal carcinoma mice xenografts, Tucidinostat (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.
| Cell Experiment | |
|---|---|
| Cell lines | PBMC effector cells |
| Preparation 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). |
| Concentrations | 0-400 nM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| 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 |
| Molecular Weight | 390.41 |
| Formula | C22H19FN4O2 |
| CAS Number | 1616493-44-7 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related HDAC Products |
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CM-444 is an inhibitor for HDAC and DNA methyltransferases (DNMT) with IC50 values of 6 nM-0.6 μM and 1.8-2.3 μM, respectively. CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models. |
| CM-1758
CM-1758 is a histone deacetylase (HDAC) inhibitor. CM-1758 inhibits tumor growth in vivo. CM-1758 induces acetylation of non-histone proteins in acute myeloid leukemia cells. |
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BRD9757 is a potent, capless and selective HDAC6 inhibitor with an IC50 of 30 nM. |
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