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Alofanib

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Chemical Structure| 1612888-66-0 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：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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
动物实验配方：
生物活性
靶点

  • FGFR2
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
1mg 5mg 10mg

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

[1]Tyulyandina A, Harrison D, et al. Alofanib, an allosteric FGFR2 inhibitor, has potent effects on ovarian cancer growth in preclinical studies. Invest New Drugs. 2017 Apr;35(2):127-133