Tucidinostat (Chidamide)

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.

CAS No. 1616493-44-7

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 37000	国内在庫あり
100mg	JPY 86500	国内在庫なし(納期7~10日)
1g	JPY 145500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（19）

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

Tucidinostat (Chidamide)関連製品

関連ターゲット	HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2	もっと見る
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関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Bioactive Compound Library-Ⅱ	もっと見る

シグナル伝達経路

HDACシグナル伝達経路

HDAC阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
U2OS	Function assay	1 uM	24 hrs	Activation of PPARG (unknown origin) expressed in human U2OS cells at 1 uM in presence of 10 uM rosiglitazone incubated for 24 hrs by luciferase reporter gene assay	ChEMBL
U2OS	Function assay	1 uM	24 hrs	Activation of ERbeta (unknown origin) expressed in human U2OS cells at 1 uM in presence of 0.01 uM E2 incubated for 24 hrs by luciferase reporter gene assay	ChEMBL
U2OS	Function assay	1 uM	24 hrs	Activation of glulcocorticoid receptor (unknown origin) expressed in human U2OS cells at 1 uM in presence of 0.1 uM dexamethasone incubated for 24 hrs by luciferase reporter gene assay	ChEMBL
U2OS	Function assay	1 uM	24 hrs	Activation of ERalpha (unknown origin) expressed in human U2OS cells at 1 uM in presence of 0.01 uM E2 incubated for 24 hrs by luciferase reporter gene assay	ChEMBL
U2OS	Function assay	1 uM	24 hrs	Activation of glulcocorticoid receptor (unknown origin) expressed in human U2OS cells at 1 uM incubated for 24 hrs by luciferase reporter gene assay	ChEMBL
U2OS	Function assay	1 uM	24 hrs	Activation of PPARG (unknown origin) expressed in human U2OS cells at 1 uM incubated for 24 hrs by luciferase reporter gene assay	ChEMBL
U2OS	Function assay	1 uM	24 hrs	Activation of ERalpha (unknown origin) expressed in human U2OS cells at 1 uM incubated for 24 hrs by luciferase reporter gene assay	ChEMBL
U2OS	Function assay	1 uM	24 hrs	Activation of ERbeta (unknown origin) expressed in human U2OS cells at 1 uM incubated for 24 hrs by luciferase reporter gene assay	ChEMBL
Sf9	Function assay		5 mins	Inhibition of recombinant human full length HDAC1 expressed in baculovirus infected Sf9 insect cells using biotinylated lysine 9 acetylated histone H3 (1 to 21 residues) as substrate incubated for 5 mins followed by substrate addition measured after 60 mi, IC50 = 0.112 μM.	28835797
EBC1	Antiproliferative assay		72 hrs	Antiproliferative activity against human EBC1 cells after 72 hrs by SRB assay, IC50 = 2.9 μM.	28835797
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay, IC50 = 7.8 μM.	28835797
HL60	Growth inhibition assay		48 hrs	Growth inhibition of human HL60 cells incubated for 48 hrs by MTS method, GI50 = 0.4 μM.	ChEMBL
Jurkat	Growth inhibition assay		48 hrs	Growth inhibition of human Jurkat cells incubated for 48 hrs by MTS method, GI50 = 1.5 μM.	ChEMBL
U2OS	Growth inhibition assay		48 hrs	Growth inhibition of human U2OS cells incubated for 48 hrs by MTS method, GI50 = 2 μM.	ChEMBL
HepG2	Growth inhibition assay		48 hrs	Growth inhibition of human HepG2 cells incubated for 48 hrs by MTS method, GI50 = 4 μM.	ChEMBL
LNCAP	Growth inhibition assay		48 hrs	Growth inhibition of human LNCAP cells incubated for 48 hrs by MTS method, GI50 = 4 μM.	ChEMBL
Raji	Growth inhibition assay		48 hrs	Growth inhibition of human Raji cells incubated for 48 hrs by MTS method, GI50 = 4 μM.	ChEMBL
MCF7	Growth inhibition assay		48 hrs	Growth inhibition of human MCF7 cells incubated for 48 hrs by MTS method, GI50 = 5 μM.	ChEMBL
28SC	Growth inhibition assay		48 hrs	Growth inhibition of human 28SC cells incubated for 48 hrs by MTS method, GI50 = 5.8 μM.	ChEMBL
PANC1	Growth inhibition assay		48 hrs	Growth inhibition of human PANC1 cells incubated for 48 hrs by MTS method, GI50 = 6.3 μM.	ChEMBL
HeLa	Function assay		10 mins	Inhibition of HDAC enzymatic activity in human HeLa cells incubated for 10 mins in presence of substrate by colorimetric activity assay, IC50 = 7.2 μM.	ChEMBL
MDA-MB-231	Growth inhibition assay		48 hrs	Growth inhibition of human MDA-MB-231 cells incubated for 48 hrs by MTS method, GI50 = 7.9 μM.	ChEMBL
SMMC7721	Growth inhibition assay		48 hrs	Growth inhibition of human SMMC7721 cells incubated for 48 hrs by MTS method, GI50 = 16 μM.	ChEMBL
DU145	Growth inhibition assay		48 hrs	Growth inhibition of human DU145 cells incubated for 48 hrs by MTS method, GI50 = 25 μM.	ChEMBL
HeLa	Growth inhibition assay		48 hrs	Growth inhibition of human HeLa cells incubated for 48 hrs by MTS method, GI50 = 40 μM.	ChEMBL
hematopoietic malignant cells	Cytotoxicity assay			Cytotoxicity against human hematopoietic malignant cells assessed as growth inhibition, GI50 = 1.86 μM.	ChEMBL
human solid tumor cells	Cytotoxicity assay			Cytotoxicity against human solid tumor cells assessed as growth inhibition, GI50 = 6.65 μM.	ChEMBL
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

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.

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
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].
細胞実験	細胞株	PBMC effector cells
	濃度	0-400 nM
	反応時間	0-400 nM
	実験の流れ	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).
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	PARP / Cleaved PARP / Caspase-3 / Cleaved caspase-3 p-EGFR / EGFR / p-STAT3 / STAT3 / p-AKT / AKT / p-AMPK / MAPK Ace-H3K18 / Ace-H3K9 / Ac-H4K8 Mcl-1 / Myc / Bcl-xl / p21 / p27 / CDK6 / CDK4 / Cyclin D2 HDAC1 / HDAC2 / HDAC3 / acetyl-H3 / acetyl-H4		30854137
	Growth inhibition assay	Cell viability		29100410

In Vivo
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].
動物実験	動物モデル	Athymic nude mice (BALB/c-nu)
	投与量	12.5-50 mg/kg
	投与経路	oral

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05586841	Not yet recruiting	HR+/HER2- Advanced Breast Cancer	Beijing 302 Hospital	November 1 2022	Phase 1
NCT05141357	Terminated	Non Small Cell Lung Cancer	HUYABIO International LLC.	March 14 2022	Phase 2
NCT04994210	Recruiting	Safety and Efficacy	Sun Yat-sen University	October 4 2021	Phase 2
NCT05140616	Recruiting	Safety and Efficacy	The First Affiliated Hospital of Soochow University	May 31 2021	Phase 1\|Phase 2
NCT04651127	Unknown status	Cervical Cancer\|Cervix Cancer\|Cervix Neoplasm	Sun Yat-sen University	November 9 2020	Phase 1\|Phase 2

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

参考

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

化学情報

分子量	390.41	化学式	C₂₂H₁₉FN₄O₂
CAS No.	1616493-44-7	SDF	Download Tucidinostat (Chidamide) SDFをダウンロードする
Smiles	C1=CC(=CN=C1)C=CC(=O)NCC2=CC=C(C=C2)C(=O)NC3=C(C=C(C=C3)F)N
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 78 mg/mL ( (199.78 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 1 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):