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受注：045-509-1970 |
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化学情報
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Synonyms | SNDX-275 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
| 化学式 | C21H20N4O3 |
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| 分子量 | 376.41 | CAS No. | 209783-80-2 | |
| Solubility (25°C)* | 体外 | DMSO | 75 mg/mL (199.25 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 | Entinostat (MS-275, SNDX-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM in cell-free assays, compared with HDACs 4, 6, 8, and 10. Entinostat induces autophagy and apoptosis. Phase 3. |
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| in vitro | MS-275 shows inhibitory to HDACs by 2'-amino group. MS-275 induces accumulation of p21WAF1/CIP1 and gelsolin in K562 cell. MS-275 could reduce S-phase cells and induce G1-phase cells in A2780 cell. MS-275 inhibits the proliferation of human tumor cell lines including A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 with IC50 from 41.5 nM to 4.71 μM, which due to HAD-inhibition. [1] MS-275 is not sensitive to other HDACs (4, 6, 8 and 10) with IC50 about/above 100 μM. [2] MS-275 shows great inhibition to human leukemia and lymphoma cells, including U937, HL-60, K562, and Jurkat. MS-275 also decreases expression of cyclin D1 and the antiapoptotic proteins Mcl-1 and XIAP. [3] |
| in vivo | MS-275 exhibits great antitumor activity against human tumor xenografts except HCT-15 at 49 mg/kg. [1] MS-275 demonstrates promising therapeutic potential in both solid and hematologic malignancies, as well as regulation of physiologic and aberrant gene expression. [4] MS-275, combination with IL-2, has great antitumor activity to renal cell carcinoma xenograft model, which due to decreased T regulatory cells and increased splenocytes. [5] |
プロトコル(参考用のみ)
| キナーゼアッセイ | Standard HDAC Assays | |
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| Rat liver enzyme is diluted 1:6 with HDAC buffer. Recombinant human HDACs are diluted 1:4 in HDAC buffer. For standard HDAC assays, 60 μL of HDAC buffer is mixed with 10 μL of diluted enzyme solution at 30 °C. The HDAC reaction is started by adding 30 μL substrate solution in HDAC buffer followed by 30 min of incubation at 30 °C. The reaction is stopped by adding 100 μL trypsin solutions (10 mg/ml trypsin in 50 mM Tris-HCl [pH 8.0], 100 mM NaCl, 2 μM TSA). After a 20 min incubation period at 30 °C, the release of AMC is monitored by measuring the fluorescence at 460 nm (λex = 390 nm). Fluorescence intensity is calibrated using free AMC. For standard time course experiments, 20 pmol of substrate is used in the initial 100 μL HDAC reaction. Km and Vmax values are determined by measuring the fluorescence AMC generated by enzymatic cleavage of 2–50 pmol of substrate. The experimental data are analyzed using a Hanes plot. The AMC signals are recorded against a blank with buffer and substrate but without the enzyme. | ||
| 細胞アッセイ | 細胞株 | A2780, Calu-3, HL-60, K562, St-4, HT-29, KB-3-1, Capan-1, 4-1St and HCT-15 cells |
| 濃度 | ~ 10 μM | |
| 反応時間 | 3 days | |
| 実験の流れ | Cancer cells (5 × 103) are seeded into each well of 96-well plates and cultured with graded concentrations of MS-275 for 3 days. The cells are stained with 0.1 mg/mL neutral red for 1 hour in a CO2-incubator, and, after aspiration of the medium, OD540 of the neutral red solubilized with 50 μL of ethanol and 150 μL of 0.1 M Na2HPO4 is measured. The IC50 value is determined by plotting growth inhibition of the cells against the logarithm of the drug concentration. |
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| 動物実験 | 動物モデル | A2780, HT-29, HTC-15, KB-3-1, 4-1St, St-4, Capan-1 and Calu-3 cells are injected subcutaneously into the flank of nude mice. |
| 投薬量 | 12.3, 24.5 and 49 mg/kg | |
| 投与方法 | Administered orally once daily 5 days per week for 4 weeks | |
参考
カスタマーフィードバック
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Data from [Data independently produced by PLoS Biol, 2014, 12, e1001758]
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Data from [Biochem Biophys Res Commun, 2014, 10.1016/j.bbrc.2014.01.184]
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Data from [Biochem Biophys Res Commun, 2014, 10.1016/j.bbrc.2014.01.184]
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：
| A functional personalised oncology approach against metastatic colorectal cancer in matched patient derived organoids [ NPJ Precis Oncol, 2024, 8(1):52] | PubMed: 38413740 |
| Romidepsin and afatinib abrogate JAK-STAT signaling and elicit synergistic antitumor effects in cutaneous T-cell lymphoma [ J Invest Dermatol, 2024, S0022-202X(23)03210-4] | PubMed: 38219917 |
| HDAC Inhibition Induces CD26 Expression on Multiple Myeloma Cells via the c-Myc/Sp1-mediated Promoter Activation [ Cancer Res Commun, 2024, 4(2):349-364] | PubMed: 38284882 |
| Single-cell RNA sequencing identifies critical transcription factors of tumor cell invasion induced by hypoxia microenvironment in glioblastoma [ Theranostics, 2023, 13(11):3744-3760] | PubMed: 37441593 |
| Novel hydroxamic acid derivative induces apoptosis and constrains autophagy in leukemic cells [ Journal of Advanced Research, 2023, 10.1016/j.jare.2023.07.005] | PubMed: None |
| HDAC3 Inhibition Promotes Antitumor Immunity by Enhancing CXCL10-Mediated Chemotaxis and Recruiting of Immune Cells [ Cancer Immunol Res, 2023, 11(5):657-673] | PubMed: 36898011 |
| Differential regulation of H3K9/H3K14 acetylation by small molecules drives neuron-fate-induction of glioma cell [ Cell Death Dis, 2023, 14(2):142] | PubMed: 36805688 |
| Elucidating the direct effects of the novel HDAC inhibitor bocodepsin (OKI-179) on T cells to rationally design regimens for combining with immunotherapy [ Front Immunol, 2023, 14:1260545] | PubMed: 37744352 |
| Elucidating the direct effects of the novel HDAC inhibitor bocodepsin (OKI-179) on T cells to rationally design regimens for combining with immunotherapy [ Front Immunol, 2023, 14:1260545] | PubMed: 37744352 |
| Porcine Epidemic Diarrhea Virus Antagonizes Host IFN-λ-Mediated Responses by Tilting Transcription Factor STAT1 toward Acetylation over Phosphorylation To Block Its Activation [ mBio, 2023, e0340822.] | PubMed: 37052505 |
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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