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
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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 | |
| 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 |
| 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 |
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