Tinostamustine
产品说明书
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同义名 : | EDO-s101; NL-101 |
| CAS号 : | 1236199-60-2 | |
| 货号 : | A256760 | |
| 分子式 : | C19H28Cl2N4O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 415.36 | |
| MDL号 : | MFCD28400036 | |
| 存储条件： |
Pure form Keep in dark place, inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Histone deacetylases (HDACs) are epigenetic regulators that regulate the histone tail, chromatin conformation, protein-DNA interaction, and even transcription. HDACs are also post-transcriptional modifiers that regulate the protein acetylation implicated in several pathophysiologic states[1]. EDO-S101, a pan HDAC inhibitor, inhibits HDAC6, HDAC1, HDAC2 and HDAC3 with IC50 values of 6 nM, 9 nM, 9 nM and 25 nM, respectively. EDO-S101 (10 mg/kg i.v.; 1 h) inhibited HDAC activity in rat PBMCs in a cellular assay by approximately 90%. in HL60 and MM1S Cells, EDO-S101 demonstrated significant acetylation of lysine residues, further confirming the HDAC-inhibition function of the vorinostat moiety in the EDO-S101 molecule. Alkylation was evaluated in vitro in myeloid (HL60 AML cell line) and lymphoid cell lines. EDO-S101 caused DNA cross links in the Comet assay at low concentrations demonstrating the alkylating function of the molecule. Exposure to EDO-S101 in vivo caused a strong DNA repair response evidenced by activation of pH2AX and p53 in tumors taken from mice bearing subcutaneous human Burkitt’s lymphoma. Moreover, 4 μM EDO-S101 triggered apoptosis in vitro and in vivo, resulting in strong antitumor activity in HL60 and Daudi cells and in the Daudi xenograft model[2]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.41mL 0.48mL 0.24mL |
12.04mL 2.41mL 1.20mL |
24.08mL 4.82mL 2.41mL |
| 参考文献 |
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