[CAS NO. 1616493-44-7] Tucidinostat (Chidamide)

Name: Tucidinostat (Chidamide)
Brand: Arctom Scientific
SKU: SLK-S8567

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PRODUCTS SPECIFICATIONS [1616493-44-7]

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Catalog

SLK-S8567

Brand

Selleck

CAS

1616493-44-7

DESCRIPTION [1616493-44-7]

Overview

MDL	-
Molecular Weight	390.41
Molecular Formula	C22H19FN4O2
SMILES	C(NC1=C(N)C=C(F)C=C1)(=O)C2=CC=C(CNC(/C=C/C=3C=CC=NC3)=O)C=C2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume 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
10 mM	0.2561 mL	1.2807 mL	2.5614 mL
50 mM	0.0512 mL	0.2561 mL	0.5123 mL

Description

Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of , 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.

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.

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.

References

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

Synonyms

Benzamide, N-(2-amino-4-fluorophenyl)-4-[[[(2E)-1-oxo-3-(3-pyridinyl)-2-propen-1-yl]amino]methyl]-

N-(2-Amino-4-fluorophenyl)-4-[[[(2E)-1-oxo-3-(3-pyridinyl)-2-propen-1-yl]amino]methyl]benzamide

Tucidinostat

HBI 8000

Epidaza

Chidamide

CS 055

(4-(2-Amino-4-fluorophenyl)carbamoylphenyl)methyl (E)-3-(3-pyridyl)acrylamide