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Tucidinostat (Chidamide)

Tucidinostat (Chidamide) structure

CAS No:
1616493-44-7
Formula:
C22H19FN4O2
Chemical Name:
Tucidinostat (Chidamide)
Synonyms:
N-(2-Amino-4-fluorophenyl)-4-[[[(2E)-1-oxo-3-(3-pyridinyl)-2-propen-1-yl]amino]methyl]benzamide;Tucidinostat - Chidamide | HBI-8000 | CS 055 | Epidaza;CS055;CS055; HBI-8000;Benzamide, N-(2-amino-4-fluorophenyl)-4-[[[(2E)-1-oxo-3-(3-pyridinyl)-2-propen-1-yl]amino]methyl]-;HBI-8000， CS-055;Chidamide (Tucidinostat, HBI8000, CS 055);HDAC,HBI8000,CS055,Tucidinostat,Histone deacetylases,CS-055,Inhibitor,HBI 8000,inhibit
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

Chidamide is a member of benzamides.|Tucidinostat is an orally bioavailable benzamide-type inhibitor of histone deacetylase (HDAC) isoenzymes 1, 2, 3 and 10, with potential antineoplastic activity. Upon administration, tucidinostat binds to and inhibits HDACs, leading to an increase of acetylation levels of histone proteins. This agent also inhibits the expression of kinases in the PI3K/Akt and MAPK/Ras signaling pathways and may result in cell cycle arrest and the induction of tumor cell apoptosis. This may inhibit tumor cell proliferation in susceptible tumor cells. HDACs, a class of enzymes that deacetylate chromatin histone proteins, are upregulated in many tumor types and play key roles in gene expression. Compared to some other benzamide-type HDAC inhibitors, chidamide is more stable, more resistant to degradation and has a longer half-life.

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.

ChEBI: Chidamide is a member of benzamides.

Tucidinostat (Chidamide) Basic Attributes

Molecular Weight：

390.41

Exact Mass：

390.41

UNII：

87CIC980Y0

NCI Thesaurus Code：

C97263

Color/Form：

White to off-white

Characteristics

PSA：

97.11

XLogP3：

4.4299

Density：

1.336±0.06 g/cm3(Predicted)

Boiling Point：

602.1±55.0 °C(Predicted)

PKA：

12.05±0.70(Predicted)

Critical Temperature & Pressure：

Store at -20°C

Drug Information

Drug Indication：

Investigated for use/treatment in cancer/tumors (unspecified).

Mechanism of Action：

Chidamide is an orally bioavailable histone deacetylase (HDAC) inhibitor derived from the benzamide class. Histone deacetylase inhibitors are a class of cancer drugs that induce selective regulation of gene expression in cancer cells. [HUYA Biosciences Press Release]

MeSH Entry Terms：

(E)-N-(2-amino-4-fluorophenyl)-4-((3-(pyridin-3-yl)acrylamido)methyl)benzamide

Tucidinostat (Chidamide) Use and Manufacturing

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.

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