Tucidinostat (Chidamide)

製品コードS8567 バッチS856703

印刷

化学情報

Synonyms

HBI-8000, CS-055

Storage
(From the date of receipt)

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

化学式

C₂₂H₁₉FN₄O₂

分子量

390.41

CAS No.

1616493-44-7

Solubility (25°C)*

体外

DMSO

78 mg/mL (199.78 mM)

Ethanol

1 mg/mL (2.56 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* 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.

溶剤液（一定の濃度）を調合する

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.
in vitro	Tucidinostat (Chidamide) inhibits class I HDACs 1-3, as well as class IIb HDAC10, at low nanomolar concentrations. It 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 this compound and MS-275 similarly inhibit the in vitro growth of most, but not all, tumor cells in the low micromolar concentration range. However, it, 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].
in vivo	In HCT-8 colorectal carcinoma mice xenografts, Tucidinostat (Chidamide) shows in vivo antitumor activity. However, it is well-tolerated at the above doses in the tumor-bearing animals, whereas the control drugs cause significant weight loss^[1].

プロトコル(参考用のみ)

細胞アッセイ	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 Tucidinostat (Chidamide) at different concentrations (0-400 nM) for different times (24-72 h).
動物実験	動物モデル	Athymic nude mice (BALB/c-nu)
	投薬量	12.5-50 mg/kg
	投与方法	oral

参考

https://pubmed.ncbi.nlm.nih.gov/22080169/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

CPSF6-RARγ interacts with histone deacetylase 3 to promote myeloid transformation in RARG-fusion acute myeloid leukemia [ Nat Commun, 2025, 16(1):616]	PubMed: 39805830
A patient-derived T cell lymphoma biorepository uncovers pathogenetic mechanisms and host-related therapeutic vulnerabilities [ Cell Rep Med, 2025, S2666-3791(25)00102-8]	PubMed: 40147445
Targeting fucosyltransferase FUT8 as a prospective therapeutic approach for DLBCL [ Oncogenesis, 2025, 14(1):1]	PubMed: 39881135
BDA-366 inhibits extra-nodal natural killer/T-cell lymphoma by inducing mitochondria damage through NF-κB pathway [ Biochem Pharmacol, 2025, S0006-2952(25)00712-9]	PubMed: 41135664
Comprehensive characterization of fatty acid oxidation in triple-negative breast cancer: Focus on biological roles and drug modulation [ Eur J Pharmacol, 2025, 991:177343]	PubMed: 39900330
Chidamide impedes glycolysis but increases ferroptosis and cisplatin sensitivity of lung cancer cells through downregulating USP35 [ BMC Cancer, 2025, 25(1):1504]	PubMed: 41044693
Targeting the akt/mtor signaling pathway by maprotiline leads to tumor suppression in T-cell lymphoma [ Ann Hematol, 2025, 10.1007/s00277-025-06571-z]	PubMed: 40892074
CYLD induces high oxidative stress and DNA damage through class I HDACs to promote radiosensitivity in nasopharyngeal carcinoma [ Cell Death Dis, 2024, 15(1):95]	PubMed: 38287022
IKAROS expression drives the aberrant metabolic phenotype of macrophages in chronic HIV infection [ Clin Immunol, 2024, 260:109915]	PubMed: 38286172
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862]	PubMed: 39319271

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。