Tucidinostat (Chidamide)

製品コードS8567 バッチS856702

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)
		Water	Insoluble
		Ethanol	Insoluble
* <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	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].
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].

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 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

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

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：

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
Synergistic effect of HDAC inhibitor Chidamide with Cladribine on cell cycle arrest and apoptosis by targeting HDAC2/c-Myc/RCC1 axis in acute myeloid leukemia [ Exp Hematol Oncol, 2023, 12(1):23]	PubMed: 36849955
Preclinical development and evaluation of nanobody-based CD70-specific CAR T cells for the treatment of acute myeloid leukemia [ Cancer Immunol Immunother, 2023, 10.1007/s00262-023-03422-6]	PubMed: 36932256
Low-Dose Chidamide Treatment Displays Sex-Specific Differences in the 3xTg-AD Mouse [ Biomolecules, 2023, 10.3390/biom13091324]	PubMed: 37759724
Low-Dose Chidamide Treatment Displays Sex-Specific Differences in the 3xTg-AD Mouse [ Biomolecules, 2023, 13(9)1324]	PubMed: 37759724
Single-cell profiling-guided combination therapy of c-Fos and histone deacetylase inhibitors in diffuse large B-cell lymphoma [ Clin Transl Med, 2022, 12(5):e798]	PubMed: 35522945
HDAC1/3-dependent moderate liquid-liquid phase separation of YY1 promotes METTL3 expression and AML cell proliferation [ Cell Death Dis, 2022, 13(11):992]	PubMed: 36424383
Targeting Class I Histone Deacetylases in Human Uterine Leiomyosarcoma [ Cells, 2022, 11(23)3801]	PubMed: 36497061
A dual SHOX2:GFP; MYH6:mCherry knockin hESC reporter line for derivation of human SAN-like cells [ iScience, 2022, 25(4):104153]	PubMed: 35434558

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。

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