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Chidamide

Cat. No. M6178
Chidamide Structure
Synonym:

HBI-8000, CS-055

Size Price Availability Quantity
10mg USD 180 In stock
25mg USD 280 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 390.41
Formula C22H19FN4O2
CAS Number 743420-02-2
Purity >99%
Solubility 78 mg/mL in DMSO
Storage at -20°C
References

Results from a multicenter, open-label, pivotal phase II study of chidamide in relapsed or refractory peripheral T-cell lymphoma.
Shi Y, et al. Ann Oncol. 2015 Aug;26(8):1766-71. PMID: 26105599.

Non-toxic dose chidamide synergistically enhances platinum-induced DNA damage responses and apoptosis in Non-Small-Cell lung cancer cells.
Zhou Y, et al. Biomed Pharmacother. 2014 May;68(4):483-91. PMID: 24721323.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Chidamide, HBI-8000, CS-055 supplier, HDAC, inhibitors

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