1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. Tucidinostat

Tucidinostat  (Synonyms: Chidamide; HBI-8000; CS 055)

Cat. No.: HY-109015 Purity: 98.60%
SDS COA Handling Instructions

Tucidinostat (Chidamide) 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.

For research use only. We do not sell to patients.

Tucidinostat Chemical Structure

Tucidinostat Chemical Structure

CAS No. : 1616493-44-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 85 In-stock
Solution
10 mM * 1 mL in DMSO USD 85 In-stock
Solid
5 mg USD 77 In-stock
10 mg USD 121 In-stock
25 mg USD 242 In-stock
50 mg USD 385 In-stock
100 mg USD 616 In-stock
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Customer Review

Based on 22 publication(s) in Google Scholar

Other Forms of Tucidinostat:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Tucidinostat (Chidamide) 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[1].

IC50 & Target[1]

HDAC3

67 nM (IC50)

HDAC10

78 nM (IC50)

HDAC1

95 nM (IC50)

HDAC2

160 nM (IC50)

HDAC11

432 nM (IC50)

HDAC8

733 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
786-0 IC50
0.63 μM
Compound: chidamide
Antiproliferative activity against human 786-O cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human 786-O cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
A549 IC50
2.79 μM
Compound: chidamide
Antiproliferative activity against human A549 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human A549 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
CCRF-CEM IC50
0.63 μM
Compound: Chidamide
Cytotoxicity against human CCRF-CEM cells by MTT assay
Cytotoxicity against human CCRF-CEM cells by MTT assay
[PMID: 31078410]
CCRF-CEM IC50
0.83 μM
Compound: chidamide
Antiproliferative activity against human CCRF-CEM cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human CCRF-CEM cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
CCRF-CEM IC50
1 μM
Compound: Chidamide
Cytotoxicity against human CCRF-CEM cells measured after 72 hrs by MTT assay
Cytotoxicity against human CCRF-CEM cells measured after 72 hrs by MTT assay
[PMID: 34986303]
COLO-678 IC50
> 10 μM
Compound: chidamide
Antiproliferative activity against human COLO-678 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human COLO-678 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
CWR22R IC50
1.08 μM
Compound: chidamide
Antiproliferative activity against human 22Rv1 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human 22Rv1 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
DOHH-2 IC50
0.53 μM
Compound: chidamide
Antiproliferative activity against human DOHH-2 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human DOHH-2 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
EBC-1 IC50
2.9 μM
Compound: CS-055
Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay
Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay
[PMID: 28835797]
HCT-116 IC50
> 20 μM
Compound: 1; CS055, HBI-8000
Antiproliferative activity against human HCT116 cells NAMPT deficient assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human HCT116 cells NAMPT deficient assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31938461]
HCT-116 IC50
0.34 μM
Compound: 1; CS055, HBI-8000
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31938461]
HCT-116 IC50
1.09 μM
Compound: HBI-8000; CS055
Antiproliferative activity against human HCT116 assessed as reduction in cell viability measured after 72 hrs using alamar blue based fluorescence method
Antiproliferative activity against human HCT116 assessed as reduction in cell viability measured after 72 hrs using alamar blue based fluorescence method
[PMID: 30802729]
HCT-116 IC50
2.08 μM
Compound: Chidamide
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by luminescence based analysis
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by luminescence based analysis
[PMID: 35649291]
HCT-116 IC50
2.08 μM
Compound: chidamide
Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human HCT-116 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
HCT-116 IC50
2.082 μM
Compound: Chidamide
Antiproliferative activity against human HCT-116 cells assessed as cell viability at 1 uM incubated for 72 hrs by luminescence assay
Antiproliferative activity against human HCT-116 cells assessed as cell viability at 1 uM incubated for 72 hrs by luminescence assay
[PMID: 34995925]
HCT-116 IC50
7.8 μM
Compound: CS-055
Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay
Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay
[PMID: 28835797]
HEL IC50
0.013 μM
Compound: 1; CS055, HBI-8000
Antiproliferative activity against human HEL cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human HEL cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31938461]
HEL IC50
1.8 μM
Compound: 1; CS055, HBI-8000
Antiproliferative activity against human HEL cells NAMPT deficient assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human HEL cells NAMPT deficient assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31938461]
HeLa IC50
7.16 μM
Compound: CS055, Epidaza
Inhibition of HDAC in human HeLa cell extract incubated for 1 hr by colorimetric activity assay
Inhibition of HDAC in human HeLa cell extract incubated for 1 hr by colorimetric activity assay
10.1039/C4MD00350K
HepG2 IC50
2 μM
Compound: Chidamide
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by luminescence based analysis
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by luminescence based analysis
[PMID: 35649291]
HepG2 IC50
4.89 μM
Compound: 2
Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human HepG2 cells measured after 48 hrs by MTT assay
[PMID: 31053508]
HL-60 IC50
0.0022 μM
Compound: 1; CS055, HBI-8000
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31938461]
HL-60 IC50
1.97 μM
Compound: HBI-8000; CS055
Antiproliferative activity against human HL60 assessed as reduction in cell viability measured after 72 hrs using alamar blue based fluorescence method
Antiproliferative activity against human HL60 assessed as reduction in cell viability measured after 72 hrs using alamar blue based fluorescence method
[PMID: 30802729]
HL-60 IC50
3.2 μM
Compound: 1; CS055, HBI-8000
Antiproliferative activity against human HL60 cells NAMPT deficient assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human HL60 cells NAMPT deficient assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31938461]
HT-29 IC50
6.04 μM
Compound: chidamide
Antiproliferative activity against human HT-29 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human HT-29 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
HuT78 IC50
2.42 μM
Compound: chidamide
Antiproliferative activity against human HuT78 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human HuT78 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
K562 IC50
0.32 μM
Compound: 1; CS055, HBI-8000
Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human K562 cells assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31938461]
K562 IC50
0.747 μM
Compound: HBI-8000; CS055
Antiproliferative activity against human K562 assessed as reduction in cell viability measured after 72 hrs using alamar blue based fluorescence method
Antiproliferative activity against human K562 assessed as reduction in cell viability measured after 72 hrs using alamar blue based fluorescence method
[PMID: 30802729]
K562 IC50
0.87 μM
Compound: 2
Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human K562 cells measured after 48 hrs by MTT assay
[PMID: 31053508]
K562 IC50
1.34 μM
Compound: Chidamide
Cytotoxicity against human K562 cells by MTT assay
Cytotoxicity against human K562 cells by MTT assay
[PMID: 31078410]
K562 IC50
2.4 μM
Compound: 1; CS055, HBI-8000
Antiproliferative activity against human K562 cells NAMPT deficient assessed as reduction in cell viability after 72 hrs by CCK8 assay
Antiproliferative activity against human K562 cells NAMPT deficient assessed as reduction in cell viability after 72 hrs by CCK8 assay
[PMID: 31938461]
K562 IC50
8.3 μM
Compound: Chidamide
Cytotoxicity against human K562 cells measured after 72 hrs by MTT assay
Cytotoxicity against human K562 cells measured after 72 hrs by MTT assay
[PMID: 34986303]
MCF7 IC50
29.07 μM
Compound: HBI-8000; CS055
Antiproliferative activity against human MCF7 assessed as reduction in cell viability measured after 72 hrs using alamar blue based fluorescence method
Antiproliferative activity against human MCF7 assessed as reduction in cell viability measured after 72 hrs using alamar blue based fluorescence method
[PMID: 30802729]
MDA-MB-231 IC50
9.52 μM
Compound: chidamide
Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
MDA-MB-468 IC50
2.65 μM
Compound: 2
Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells measured after 48 hrs by MTT assay
[PMID: 31053508]
MOLT-4 IC50
0.75 μM
Compound: chidamide
Antiproliferative activity against human MOLT-4 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human MOLT-4 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
MV4-11 IC50
0.783 μM
Compound: Chidamide
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by luminescence based analysis
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 72 hrs by luminescence based analysis
[PMID: 35649291]
MV4-11 IC50
3.73 μM
Compound: 2
Antiproliferative activity against human MV4-11 cells measured after 48 hrs by MTT assay
Antiproliferative activity against human MV4-11 cells measured after 48 hrs by MTT assay
[PMID: 31053508]
NCI-H441 IC50
2.62 μM
Compound: chidamide
Antiproliferative activity against human NCI-H441 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human NCI-H441 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
NCI-H460 IC50
2.34 μM
Compound: chidamide
Antiproliferative activity against human NCI-H460 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human NCI-H460 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
Rec1 IC50
1.01 μM
Compound: chidamide
Antiproliferative activity against human REC1 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human REC1 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
RS4-11 IC50
0.6 μM
Compound: chidamide
Antiproliferative activity against human RS4-11 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human RS4-11 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
Sf9 IC50
0.167 μM
Compound: 2
Inhibition of recombinant full-length human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using Fluor-de-Lys as substrate measured after 10 mins by fluorescence assay
Inhibition of recombinant full-length human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected Sf9 insect cells using Fluor-de-Lys as substrate measured after 10 mins by fluorescence assay
[PMID: 31053508]
SK-OV-3 IC50
8.46 μM
Compound: chidamide
Antiproliferative activity against human SK-OV-3 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human SK-OV-3 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
SU-DHL-2 IC50
0.56 μM
Compound: chidamide
Antiproliferative activity against human SUDHL2 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human SUDHL2 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
TMD8 IC50
0.48 μM
Compound: chidamide
Antiproliferative activity against human TMD8 cells incubated for 72 hrs by luminescence assay
Antiproliferative activity against human TMD8 cells incubated for 72 hrs by luminescence assay
[PMID: 34954594]
U-937 IC50
3.3 μM
Compound: Chidamide
Cytotoxicity against human U-937 cells measured after 72 hrs by MTT assay
Cytotoxicity against human U-937 cells measured after 72 hrs by MTT assay
[PMID: 34986303]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

390.41

Formula

C22H19FN4O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(CNC(/C=C/C2=CN=CC=C2)=O)C=C1)NC(C=CC(F)=C3)=C3N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (128.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 1 mg/mL (2.56 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5614 mL 12.8070 mL 25.6141 mL
5 mM 0.5123 mL 2.5614 mL 5.1228 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.60%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.5614 mL 12.8070 mL 25.6141 mL 64.0352 mL
DMSO 5 mM 0.5123 mL 2.5614 mL 5.1228 mL 12.8070 mL
10 mM 0.2561 mL 1.2807 mL 2.5614 mL 6.4035 mL
15 mM 0.1708 mL 0.8538 mL 1.7076 mL 4.2690 mL
20 mM 0.1281 mL 0.6404 mL 1.2807 mL 3.2018 mL
25 mM 0.1025 mL 0.5123 mL 1.0246 mL 2.5614 mL
30 mM 0.0854 mL 0.4269 mL 0.8538 mL 2.1345 mL
40 mM 0.0640 mL 0.3202 mL 0.6404 mL 1.6009 mL
50 mM 0.0512 mL 0.2561 mL 0.5123 mL 1.2807 mL
60 mM 0.0427 mL 0.2135 mL 0.4269 mL 1.0673 mL
80 mM 0.0320 mL 0.1601 mL 0.3202 mL 0.8004 mL
100 mM 0.0256 mL 0.1281 mL 0.2561 mL 0.6404 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Tucidinostat
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