产品说明书
BAY-3827
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同义名 : | - |
| CAS号 : | 2377576-35-5 | |
| 货号 : | A1721515 | |
| 分子式 : | C27H25FN6O | |
| 纯度 : | 98% | |
| 分子量 : | 468.525 | |
| MDL号 : | MFCD34662962 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 25 mg/mL(53.36 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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | BAY-3827 is a potent and selective AMPK inhibitor with an IC50 of 1.4 nM at low concentrations of ATP (10 µM) and 15 nM at high concentrations of ATP (2 mM). BAY-3827 (0-200 µM) inhibits Aurora A, Flt3, c-Met and Rsk4 with an IC50 of 10 µM ATP. BAY-3827 prevented the phosphorylation of acetyl-CoA carboxylase 1 and showed the strongest antiproliferative activity in androgen-dependent prostate cancer cell lines. BAY-3827 (overnight) strongly reduced the phosphorylation of ACC1 Ser79 in LNCaP and VCaP cells. BAY-3827 (0-200 μM) inhibited Aurora A, Flt3, c-Met and Rsk4, with an IC50 at 10 µM ATP concentration of 1324, 124, 788, and 36 nM, respectively. Phosphorylation of ACC1 Ser79 was reduced to a lesser extent in IMR-32 cells, especially in Colo320 cells. At concentrations less than 10 nM, acting for 6 days, BAY-3827 had a strong inhibitory effect on LNCaP and VCaP cells. At 1 and 5 μM concentrations for 24 and 48 hours, BAY-3827 inhibited the expression of the LIPE gene, reduced AKT3, and blocked the expression of several genes in the CPT family involved in acylcarnitine formation in VCaP cells . At a concentration of 5 μM for 2-4 days, BAY-3827 significantly increased lipid droplet formation, whereas androgen-only treatment did not[1]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.13mL 0.43mL 0.21mL |
10.67mL 2.13mL 1.07mL |
21.34mL 4.27mL 2.13mL |
| 参考文献 |
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