1616493-44-7

1616493-44-7 structure

Name: Tucidinostat (Chidamide)
Chemical Name: tucidinostat
CAS Number: 1616493-44-7
Molecular Formula: C₂₂H₁₉FN₄O₂
Molecular Weight: 390.410
Catalog: Research Areas Cancer
Create Date: 2018-10-17 09:08:45
Modify Date: 2024-01-01 17:38:30
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.

Name	tucidinostat
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]-

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	Research Areas >> Cancer
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.

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℃

Hazard Codes	N