| Identification | Back Directory | [Name]
Tucidinostat (Chidamide) | [CAS]
1616493-44-7 | [Synonyms]
CS055
TUCIDINOSTAT
CS055; HBI-8000
Tucidinostat - Chidamide | HBI-8000 | CS 055 | Epidaza
N-(2-Amino-4-fluorophenyl)-4-[[[(2E)-1-oxo-3-(3-pyridinyl)-2-propen-1-yl]amino]methyl]benzamide
Benzamide, N-(2-amino-4-fluorophenyl)-4-[[[(2E)-1-oxo-3-(3-pyridinyl)-2-propen-1-yl]amino]methyl]- | [Molecular Formula]
C22H19FN4O2 | [MOL File]
1616493-44-7.mol | [Molecular Weight]
390.41 |
| Chemical Properties | Back Directory | [Boiling point ]
602.1±55.0 °C(Predicted) | [density ]
1.336±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 20 mg/ml; DMSO: 20 mg/ml; DMSO:PBS(pH7.2) (1:1): 0.5 mg/ml | [form ]
A crystalline solid | [pka]
12.05±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
Chidamide is an inhibitor of histone deacetylases (HDACs; IC50s = 0.095, 0.160, 0.067, 0.733, 0.078, and 0.432 μM for HDAC1-3, 8, 10, and 11, respectively). It is selective for these HDACs over HDAC4-7 and 9 (IC50s = >30 μM for all). Chidamide also inhibits nicotinamide phosphoribosyltransferase (Nampt; IC50 = 2.1 μM). It inhibits cell growth in a panel of 18 cancer cell lines (GI50s = 0.4-40 μM) but has no effect on the growth of non-cancerous CCC-HEK human fetal kidney or CCC-HEL human liver cells (GI50s = >100 μM). In vivo, tucidinostat (12.5, 25, and 50 mg/kg) reduces tumor growth in HCT-8, A549, BEL-7402, and MCF-7 mouse xenograft models. | [Uses]
Chidamide is a newly designed histone deacetylase inhibitor that induces an antitumor effect in various cancer by increasing the acetylation levels of histone H3 and decrease histone deacetylase (HDAC) activity, induces apoptosis. Also, it is a potential utility of Chidamide for the treatment of Myelodysplastic syndromes. | [Definition]
ChEBI: Chidamide is a member of benzamides. | [in vivo]
Tucidinostat (12.5-50 mg/kg, p.o.) dose-dependently reduces tumor size and tumor weight in mice bearing HCT-8 colorectal carcinoma, A549 lung carcinoma, BEL-7402 liver carcinoma, and MCF-7 breast carcinoma, and with no obvious body loss[1]. | [IC 50]
HDAC3: 67 nM (IC50); HDAC10: 78 nM (IC50); HDAC1: 95 nM (IC50); HDAC2: 160 nM (IC50); HDAC11: 432 nM (IC50); HDAC8: 733 nM (IC50) | [storage]
Store at -20°C | [References]
[1] ZHI-QIANG NING. Chidamide (CS055/HBI-8000): a new histone deacetylase inhibitor of the benzamide class with antitumor activity and the ability to enhance immune cell-mediated tumor cell cytotoxicity.[J]. Cancer Chemotherapy and Pharmacology, 2012, 69 4: 901-909. DOI: 10.1007/s00280-011-1766-x
[2] YING WU. Nicotinamide Phosphoribosyltransferase (NAMPT) Is a New Target of Antitumor Agent Chidamide[J]. ACS Medicinal Chemistry Letters, 2019, 11 1: 40-44. DOI: 10.1021/acsmedchemlett.9b00407 |
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