受注:045-509-1970 |
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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 | |||
* <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. |
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] |
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. |
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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。
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