Domatinostat (4SC-202)

製品コードS7555 バッチS755503

印刷

化学情報

Synonyms

Storage
(From the date of receipt)

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

化学式

C₂₃H₂₁N₅O₃S

分子量

447.51

CAS No.

910462-43-0

Solubility (25°C)*

体外

DMSO

89 mg/mL (198.87 mM)

Water

Insoluble

Ethanol

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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	4.450mg/ml (9.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 89 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.450mg/ml (1.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 9 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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	Domatinostat (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1). Phase 1.
in vitro	In HeLa cells, Domatinostat (4SC-202) induces hyperacetylation of histone H3 with EC50 of 1.1 μM. It induces a G2/M cell cycle arrest by interfering with the normal development of the mitotic spindle and causing collapsed spindle apparatus and multiple nucleation centres. In addition, this compound shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC50 of 0.7 μM. ^[1]
in vivo	Domatinostat (4SC-202) has a high oral bioavailability in vivo, and shows high metabolic stability and a low plasma clearance. It (120 mg/kg p.o.) shows pronounced and robust anti-tumor activity in both A549 NSCLC xenograft and RKO27 colon carcinoma model. ^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	CRC lines (HT-29, HCT-116, HT-15, and DLD-1)
	濃度	0.1, 1, 5, 10 μM
	反応時間	72 hours
	実験の流れ	Domatinostat (4SC-202) was applied to CRC cell lines (HT-29, HCT-116, HCT-15, and DLD1), primary human colon cancer cells, or primary human colon epithelial cells at specified concentrations. After further culture for the indicated time, cell survival was tested by MTT assay or trypan blue staining assay; cell proliferation was tested by clonogenicity assay. Expression of listed proteins was tested by Western blots.
動物実験	動物モデル	A549 NSCLC xenograft model and RKO27 colon carcinoma model
	投薬量	120 mg/kg
	投与方法	p.o.

参考

http://www.4sc.de/wp-content/uploads/4SC-202-Poster-EORTC-Berlin-2010.pdf
https://pubmed.ncbi.nlm.nih.gov/26831668/

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：

Epigenetic and molecular coordination between HDAC2 and SMAD3-SKI regulates essential brain tumour stem cell characteristics [ Nat Commun, 2023, 14(1):5051]	PubMed: 37598220
Epigenetic and molecular coordination between HDAC2 and SMAD3-SKI regulates essential brain tumour stem cell characteristics [ Nat Commun, 2023, 14(1):5051]	PubMed: 37598220
Single-cell dissection of Merkel cell carcinoma heterogeneity unveils transcriptomic plasticity and therapeutic vulnerabilities [ Cell Rep Med, 2023, 4(7):101101]	PubMed: 37421947
Domatinostat Targets the FOXM1-Survivin Axis to Reduce the Viability of Ovarian Cancer Cells Alone and in Combination with Chemotherapeutic Agents [ Int J Mol Sci, 2023, 24(13)10817]	PubMed: 37445993
Domatinostat Targets the FOXM1-Survivin Axis to Reduce the Viability of Ovarian Cancer Cells Alone and in Combination with Chemotherapeutic Agents [ Int J Mol Sci, 2023, 24(13)10817]	PubMed: 37445993
HDAC Inhibition Restores Response to HER2-Targeted Therapy in Breast Cancer via PHLDA1 Induction [ Int J Mol Sci, 2023, 24(7)6228]	PubMed: 37047202
Targeting the USP7/RRM2 axis drives senescence and sensitizes melanoma cells to HDAC/LSD1 inhibitors [ Cell Rep, 2022, 40(12):111396]	PubMed: 36130505
HDAC Class I Inhibitor Domatinostat Preferentially Targets Glioma Stem Cells over Their Differentiated Progeny [ Int J Mol Sci, 2022, 23(15)8084]	PubMed: 35897656
Reduction of Metastasis via Epigenetic Modulation in a Murine Model of Metastatic Triple Negative Breast Cancer (TNBC) [ Cancers (Basel), 2022, 14(7)1753]	PubMed: 35406526
Complexities in the role of acetylation dynamics in modifying inducible gene activation parameters [ Nucleic Acids Res, 2021, 49(22):12744-12756]	PubMed: 34850951

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。