产品说明书
BAY-8002
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同义名 : | - |
| CAS号 : | 724440-27-1 | |
| 货号 : | A1142862 | |
| 分子式 : | C20H14ClNO5S | |
| 纯度 : | 98% | |
| 分子量 : | 415.847 | |
| MDL号 : | MFCD05157149 | |
| 存储条件： |
粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 120 mg/mL(288.57 mM)，配合低频超声助溶，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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | MCT1 (monocarboxylate transporter 1/ SLC16A1) plays a central role in tumor cell energy homeostasis. BAY-8002 is a novel class of MCT1 inhibitor which can potently suppress bidirectional lactate transport with IC50 value of 8nM and EC50 value of 7nM for L-lactate uptake and lactate export in DLD-1 cells. Also, BAY-8002 inhibited lactate uptake in MCT2-expressing oocytes, with approximately 5-fold lower potency compared with the MCT1 isoform. For the accumulation of lactate in the cell supernatant was inhibited by BAY8002, the change of intracellular pH and decrease of extracellular acidification rate could be observed. This inhibition of lactate transport resulted an efficient proliferation inhibition of Raji and Daudi Burkitt lymphoma cells expressed MCT1. Oral administration of BAY8002 at dose of 80 and 160mg/kg twice daily led a significant inhibition of tumor growth and modulation of intratumor lactate in Raji tumor–bearing mice but not WSU-DLCL2. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.40mL 0.48mL 0.24mL |
12.02mL 2.40mL 1.20mL |
24.05mL 4.81mL 2.40mL |
