Tucidinostat (Chidamide)

Modify Date: 2024-01-01 17:38:30

Tucidinostat (Chidamide) Structure
Tucidinostat (Chidamide) structure
Common Name Tucidinostat (Chidamide)
CAS Number 1616493-44-7 Molecular Weight 390.410
Density 1.3±0.1 g/cm3 Boiling Point 602.1±55.0 °C at 760 mmHg
Molecular Formula C22H19FN4O2 Melting Point N/A
MSDS N/A Flash Point 317.9±31.5 °C

 Use of Tucidinostat (Chidamide)


Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9.

 Names

Name tucidinostat
Synonym More Synonyms

 Tucidinostat (Chidamide) Biological Activity

Description Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9.
Related Catalog
Target

HDAC3:67 nM (IC50)

HDAC10:78 nM (IC50)

HDAC1:95 nM (IC50)

HDAC2:160 nM (IC50)

HDAC11:432 nM (IC50)

HDAC8:733 nM (IC50)

In Vitro Tucidinostat (Chidamide/CS055/HBI-8000) is a potent and orally bioavailable HDAC enzymes class I (HDAC1, 2, 3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, less active on HDAC8 and HDAC11 (IC50s, 733 nM, 432 nM, respectively), and shows no effect on HDAC4/5/6/7/9 (IC50s, >30 μM). Tucidinostat shows potent antitumor activity, and inhibits several human derived tumor cell lines, such as HL-60, U2OS, LNCaP with GI50s of 0.4 ± 0.1, 2.0 ± 0.6, and 4.0 ± 1.2 μM, respectively. In addition, Tucidinostat shows less toxic to normal cells from human fetal kidney (CCC-HEK) and liver (CCCHEL)[1].
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].
References

[1]. Ning ZQ, et al. 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. Cancer Chemother Pharmacol. 2012 Apr;69(4):901-9.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 602.1±55.0 °C at 760 mmHg
Molecular Formula C22H19FN4O2
Molecular Weight 390.410
Flash Point 317.9±31.5 °C
Exact Mass 390.149200
LogP 2.40
Vapour Pressure 0.0±1.7 mmHg at 25°C
Index of Refraction 1.691
Storage condition -20℃

 Safety Information

Hazard Codes N

 Synonyms

Epidaza
10318
87CIC980Y0
N-(2-Amino-4-fluorophenyl)-4-({[(2E)-3-(3-pyridinyl)-2-propenoyl]amino}methyl)benzamide
tucidinostat
Benzamide, N-(2-amino-4-fluorophenyl)-4-[[[(2E)-1-oxo-3-(3-pyridinyl)-2-propen-1-yl]amino]methyl]-
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Price: ¥770/10 mM * 1 mL in DMSO

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