Tucidinostat (Chidamide)

Name: Tucidinostat (Chidamide)
Brand: Selleck Chemicals
SKU: S8567
Rating: 5 (2 reviews)

For research use only.

Catalog No.S8567 Synonyms: HBI-8000, CS-055

2 publications

Tucidinostat (Chidamide) Chemical Structure

CAS No. 1616493-44-7

Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively.

Selleck's Tucidinostat (Chidamide) has been cited by 2 publications

Purity & Quality Control

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Biological Activity

Description

Targets

HDAC3 ^[1] (Cell-free)	HDAC10 ^[1] (Cell-free)	HDAC1 ^[1] (Cell-free)	HDAC2 ^[1] (Cell-free)
67 nM	78 nM	95 nM	160 nM

In vitro

Chidamide inhibits class I HDACs 1-3, as well as class IIb HDAC10, at low nanomolar concentrations. Chidamide significantly induces histone H3 acetylation in both HeLa human cervical adenocarcinoma cells and human PBMC. Cell growth inhibition studies performed with 18 human-derived tumor cell lines demonstrate that chidamide and MS-275 similarly inhibit the in vitro growth of most, but not all, tumor cells in the low micromolar concentration range. However, chidamide, and to a lesser extent MS-275, is significantly less toxic to normal cells from human fetal kidney (CCC-HEK) and liver (CCC-HEL), indicating a differential cytotoxic response of normal cells versus cancerous cells to chidamide^[1].

Assay

Methods	Test Index	PMID
Western blot	PARP / Cleaved PARP / Caspase-3 / Cleaved caspase-3 ; PubMed: 30854137 J Cancer Expression and activation level of Caspase-3 and PARP after treatment of serial dilutions of chidamide in HCC827 cells (48h). p-EGFR / EGFR / p-STAT3 / STAT3 / p-AKT / AKT / p-AMPK / MAPK ; PubMed: 30854137 J Cancer Chidamide inhibition of PTK signaling molecules in A549 cells (48h). Ace-H3K18 / Ace-H3K9 / Ac-H4K8 ; PubMed: 29773595 Haematologica Western blot analysis of H3 acetylation at Lys18 and Lys9 and H4 acetylation at Lys8. H3 and H4 expression levels were used as loading controls. Mcl-1 / Myc / Bcl-xl / p21 / p27 / CDK6 / CDK4 / Cyclin D2 ; PubMed: 29773595 Haematologica Western blot analysis of Mcl-1, Myc, Bcl-xL, Bcl-2, p21, p27, CDK4, CDK6, and Cyclin-D2 levels; α-tubulin was used as the loading control. HDAC1 / HDAC2 / HDAC3 / acetyl-H3 / acetyl-H4 ; PubMed: 31289512 Oncol Lett (A) RPMI8226 cells were treated with 0, 0.5, 1 or 2 µmol/l chidamide for 48 h and (B) U266 cells were treated with 0, 2, 4 or 8 µmol/l chidamide for 48 h, and HDACs expression was assessed using western blot analysis.	30854137 29773595 31289512
Growth inhibition assay	Cell viability; PubMed: 29100410 Oncotarget (a) Proliferation rates at 24, 48, 72 hour of Hs445 cells after treated with 0.1μM, 0.3μM, 1μM, 3μM, 10μM, 30μM Chidamides; (b) proliferation rates at 24, 48, 72 hours of L428 cells after treated with 0.1μM, 0.3μM, 1μM, 3μM, 10μM, 30μM Chidamide;	29100410

In vivo

In HCT-8 colorectal carcinoma mice xenografts, Chidamide shows in vivo antitumor activity. Chidamide in the dose range of 12.5-50 mg/kg dose-dependently reduces tumor size and tumor weight, and the dose of 50 mg/kg produces similar or greater efficacy compared with the control drugs 5-fluorouracil(5-FU, 20 mg/kg) and MS-275 (25 mg/kg, which was reported as the maximum tolerated dose in xenograft models). However, chidamide is well-tolerated at the above doses in the tumor-bearing animals, whereas the control drugs cause significant weight loss^[1].

Protocol

Cell Research: ^[1]	- Collapse Cell lines: PBMC effector cells Concentrations: 0-400 nM Incubation Time: 0-400 nM Method: Isolated PBMC effector cells are seeded into 6-well plates (6 x 10⁶ cells/well) and treated with chidamide at different concentrations (0-400 nM) for different times (24-72 h). (Only for Reference)
Animal Research: ^[1]	- Collapse Animal Models: Athymic nude mice (BALB/c-nu) Dosages: 12.5-50 mg/kg Administration: oral (Only for Reference)

References

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

Solubility (25°C)

In vitro	DMSO	78 mg/mL (199.78 mM)
	Water	Insoluble
	Ethanol	'2 mg/mL
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 1% CMC Na For best results, use promptly after mixing.	30mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Tucidinostat (Chidamide) SDF

Molecular Weight	390.41
Formula	C₂₂H₁₉FN₄O₂
CAS No.	1616493-44-7
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	HBI-8000, CS-055
Smiles	C1=CC(=CN=C1)C=CC(=O)NCC2=CC=C(C=C2)C(=O)NC3=C(C=C(C=C3)F)N

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Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
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Bio Calculators

Molarity Calculator

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The Serial Dilution Calculator Equation

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-09-01)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03820596	Recruiting	Drug: Sintilimab\|Drug: Chidamide	Safety and Efficacy	Huiqiang Huang\|Sun Yat-sen University	March 29 2019	Phase 1\|Phase 2
NCT02944812	Unknown status	Drug: Chidamide	Peripheral T Cell Lymphoma	Guangdong Provincial People''s Hospital	March 2016	Phase 2
NCT02569489	Withdrawn	Drug: HBI-8000\|Drug: Trastuzumab\|Drug: Paclitaxel	Breast Cancer	HUYA Bioscience International	December 2015	Phase 1
NCT02513901	Completed	Drug: Chidamide	Chronic HIV Infections	Tang-Du Hospital\|Chipscreen Biosciences Ltd.	August 2015	Phase 1\|Phase 2
NCT02482753	Active not recruiting	Drug: Chidamide\|Drug: exemestane\|Drug: placebo	Breast Cancer	Chipscreen Biosciences Ltd.	July 2015	Phase 3

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Tucidinostat (Chidamide)