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化学情報
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Synonyms | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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| 化学式 | C23H21N5O3S |
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| 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 | |||
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* <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. |
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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. |
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| in vitro | In HeLa cells, 4SC-202 induces hyperacetylation of histone H3 with EC50 of 1.1 μM. 4SC-202 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, 4SC-202 shows a broad anti-proliferative activity towards human cancer cell lines with a mean IC50 of 0.7 μM. [1] |
| in vivo | In vivo, 4SC-202 has a high oral bioavailability, and shows high metabolic stability and a low plasma clearance. 4SC-202 (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) |
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| 濃度 | 0.1, 1, 5, 10 μM | |
| 反応時間 | 72 hours | |
| 実験の流れ | CRC cell lines (HT-29, HCT-116, HCT-15, and DLD1), the primary human colon cancer cells, or primary human colon epithelial cells were treated with applied concentrations of 4SC-202, cells were further cultured for indicated time, and 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. |
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| 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
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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 |
| 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 |
| 4sc-202 and Ink-128 cooperate to reverse the epithelial to mesenchymal transition in OSCC [ Oral Dis, 2021, 10.1111/odi.13860] | PubMed: 33772986 |
| Analysis of Dual Class I Histone Deacetylase and Lysine Demethylase Inhibitor Domatinostat (4SC-202) on Growth and Cellular and Genomic Landscape of Atypical Teratoid/Rhabdoid. [ Cancers (Basel), 2020, 23;12(3) pii: E756] | PubMed: 32210076 |
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。