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SML4257

Chidamide

Name: Chidamide
Brand: SIGMA

≥98% (HPLC), powder, histone deacetylase (HDAC) inhibitor

Synonym(s):

CS 055, CS-055, CS055, HBI 8000, HBI-8000, HBI8000, Tucidinostat, N-(2-Amino-4-fluorophenyl)-4-[[[(2E)-1-oxo-3-(3-pyridinyl)-2-propen-1-yl]amino]methyl]benzamide

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About This Item

Empirical Formula (Hill Notation):

C₂₂H₁₉FN₄O₂

CAS Number:

1616493-44-7

Molecular Weight:

390.41

MDL number:

MFCD28100259

NACRES:

NA.21

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

-10 to -25°C

Application

Chidamide may be used as an enhancer of zeste homolog 2 (EZH2) inhibitor and study the antileukemia effects in vivo in leukemia-bearing nude mouse models

Biochem/physiol Actions

Chidamide (CS055, HBI-8000, Tucidinostat) is an orally available benzamide that inhibits against class I histone deaceylases HDAC1/2/3/8 (IC50 of 95/160/67/733 nM), class II2b HDAC10 (IC50 = 78 nM), and class IV HDAC11 (IC50 = 432 nM), but not class IIa HDAC4/5/7/9 or IIb HDAC10 (IC50 >30 μM). Chidamide effectively upregulates cellular acetylation levels of histone H3 and H4 (3 μM for 24 h in SKM-1 and HEL cultures) and exhibits anti-cancer efficacy both in cultures and in vivo.

pictograms

GHS07

signalword

Warning

hcodes

H302

pcodes

P264 - P270 - P301 + P312 - P501

Hazard Classifications

Acute Tox. 4 Oral

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Induction of apoptosis by HBI-8000 in adult T-cell leukemia/lymphoma is associated with activation of Bim and NLRP3.

Hiroo Hasegawa et al.

Cancer science, 107(8), 1124-1133 (2016-05-20)

Adult T-cell leukemia/lymphoma (ATL) is an aggressive T-cell malignancy caused by human T-cell lymphotropic virus 1. Treatment options for acute ATL patients include chemotherapy, stem cell transplantation, and recently the anti-chemokine (C-C motif) receptor 4 antibody, although most patients still

CS055 (Chidamide/HBI-8000), a novel histone deacetylase inhibitor, induces G1 arrest, ROS-dependent apoptosis and differentiation in human leukaemia cells.

Ke Gong et al.

The Biochemical journal, 443(3), 735-746 (2012-02-22)

CS055 (Chidamide/HBI-8000) is a novel benzamide-type HDACi (histone deacetylase inhibitor), which has entered Phase I clinical trials in the U.S. and Phase II/III in China. In the present study, we investigated the effects of CS055 on proliferation, differentiation and apoptosis

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.

Zhi-Qiang Ning et al.

Cancer chemotherapy and pharmacology, 69(4), 901-909 (2011-11-15)

Chidamide (CS055/HBI-8000) is a new histone deacetylase (HDAC) inhibitor of the benzamide class currently under clinical development in cancer indications. This study reports the in vitro and in vivo antitumor characteristics of the compound. Selectivity and potency of chidamide in

Global Trade Item Number

SKU	GTIN
SML4257-10MG	04065273262568
SML4257-50MG	04065273262575

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