产品说明书
STAT3-IN-1
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同义名 : | - |
| CAS号 : | 2059952-75-7 | |
| 货号 : | A1176397 | |
| 分子式 : | C28H29NO6 | |
| 纯度 : | 98% | |
| 分子量 : | 475.533 | |
| MDL号 : | MFCD32174234 | |
| 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(252.35 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 | |||
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| 描述 | Signal transducer and activator of transcription 3 (STAT3) is a cytoplasmic protein that plays important roles in oncogenic signaling pathways. STAT3-IN-1 (compound 7d) is a potent, selective and orally active STAT3 inhibitor with IC50 values of 1.82 μM and 2.14 μM in HT29 and MDA-MB 231 cells, respectively. Exposing MDA-MB-231 cells to STAT3-IN-1 (1-5 μM) for 48 h led to dose-dependent inhibition of STAT3 acetylation at Lys685 residue. STAT3-IN-1 increased the expressions of the tumor-suppressor genes which were related to STAT3 acetylation at Lys685, thereby further demonstrated that STAT3-IN-1 inhibited STAT3 acetylation. In MDA-MB-231 cancer cells, STAT3-IN-1 (1-5 μM for 48 hr) markedly decreased the phospho-Tyr705 STAT3 in a dose-dependent manner without affecting the total STAT3, indicating that STAT3-IN-1 selectively decreased the level of p-STAT3. STAT3-IN-1 (1-10 μM for 48 hr) dose-dependently inhibited the proliferation of STAT3 dependent MDA-MB-231 cells. STAT3-IN-1 (10 mg/kg, 20 mg/kg) significantly inhibited tumor growth as reflected in decreased tumor weight. And the level of p-STAT3 (Y705) was also inhibited in tumor tissues from mice treated with STAT3-IN-1[2]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.10mL 0.42mL 0.21mL |
10.51mL 2.10mL 1.05mL |
21.03mL 4.21mL 2.10mL |
| 参考文献 |
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