Catalog No.S8567 Synonyms: HBI-8000, CS-055
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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|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.|
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.|
|In vitro||DMSO||78 mg/mL (199.78 mM)|
|Ethanol||2 mg/mL (5.12 mM)|
|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.
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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|
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.
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