Alofanib
产品说明书
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同义名 : | 阿洛法尼（RPT835） ;RPT835 |
| CAS号 : | 1612888-66-0 | |
| 货号 : | A500409 | |
| 分子式 : | C19H15N3O6S | |
| 纯度 : | 99%+ | |
| 分子量 : | 413.404 | |
| MDL号 : | MFCD30747921 | |
| 存储条件： |
Pure form Inert atmosphere,Room Temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 30 mg/mL(72.57 mM)，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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| 靶点 |
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| 描述 | Fibroblast growth factor receptor 2 (FGFR2) is receptor with tyrosine-kinase activity. FGFR2 amplification and high-level polysomy may be a promising molecular target for serous ovarian cancer. Alofanib is a predominantly FGFR2-selective allosteric small-molecular inhibitor that shows promising antiangiogenic and antitumor activities in preclinical studies. In the human ovarian cancer FGFR-expressing cell line, alofanib (ranging from 0 to 1 μM) significantly inhibited FGF-triggered cell proliferation in a dose-dependent manner. In FGFR2-overexpressing SKOV3 cell xenograft model, the combination of oral alofanib and paclitaxel/carboplatin produced a greater inhibitory effect on xenograft growth compared with vehicle group with inhibition rate over 63 %. Moreover, alofanib significantly decreased number of vessels in tumor (−49 %) and number of Ki-67-positive SKOV3 cells. Daily intravenous regimen of alofanib (total maximum dose per week was 350 mg/kg) dramaticly inhibited tumor growth by 80%[1]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.42mL 0.48mL 0.24mL |
12.09mL 2.42mL 1.21mL |
24.19mL 4.84mL 2.42mL |
| 参考文献 |
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