产品说明书
OTX008
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同义名 : | Calixarene 0118;PTX008;N(2dimethylamino)ethyl)acetamidyl calix4arene. |
| CAS号 : | 286936-40-1 | |
| 货号 : | A1177354 | |
| 分子式 : | C52H72N8O8 | |
| 纯度 : | 99%+ | |
| 分子量 : | 937.177 | |
| MDL号 : | MFCD28396412 | |
| 存储条件： |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 4 mg/mL(4.27 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO 无水乙醇: 30 mg/mL(32.01 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Galectin-1 is a member of a family of evolutionarily conserved glycan-binding proteins, displays broad anti-inflammatory and pro-resolving activities by targeting multiple immune cell types[1]. Galectin-1 is also a carbohydrate-binding protein is implicated in cancer cell proliferation, invasion and tumor angiogenesis. OTX008 is a calixarene-based compound and selective galectin-1 (Gal-1) inhibitor with potential anti-angiogenic and antineoplastic activities. OTX008 inhibited tumor cell proliferation, though inhibition was very variable, with IC50 ranging from 1.7 to 192.3 μM. In vivo, the human ovarian carcinoma A2780-1A9 and human glioblastoma U87MG showed a different degree of sensitivity to OTX008 (IC50 of 2.1 and 35.8 μM, respectively). OTX008 achieved a Cmax of 14.39 μg/mL (15.35 μM) and then the drug was rapidly distributed through the body with half-life (HL) of 20 min and cleared from plasma with a long elimination HL of 31.4 h. In vitro, OTX008 inhibited endothelial cell proliferation in a concentration-dependent manner with a mean IC50 values of 9.9 ± 4.2, 8.7 ± 1.7, and 12.9 ± 3.3 μM respectively[2]. |
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| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.07mL 0.21mL 0.11mL |
5.34mL 1.07mL 0.53mL |
10.67mL 2.13mL 1.07mL |
| 参考文献 |
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