Alofanib (Synonyms: RPT835)
目录号: PL04752 纯度: ≥98%
CAS No. :1612888-66-0
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中文名称
Alofanib
中文别名
RPT835
英文名称
Alofanib
英文别名
RPT835;Alofanib;3-(N-(4-methyl-2-nitro-5-(pyridin-3-yl)phenyl)sulfamoyl)benzoic acid;LQX7RFK8MZ;Alofanib [INN];Alofanib(RPT835);Benzoic acid, 3-(((4-methyl-2-nitro-5-(3-pyridinyl)phenyl)amino)sulfonyl)-;SB19665;AK668992;ES000835
Cas No.
1612888-66-0
分子式
C19H15N3O6S
分子量
413.40
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Alofanib (RPT835)是高效和选择性的成纤维细胞生长因子受体2 (FGFR2) 的变构抑制剂。抗癌活性。抗血管生成活性。
生物活性
Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer and antiangiogenic activity.
性状
Solid
IC50 & Target[1][2]
FGFR2
体外研究(In Vitro)
Alofanib inhibits phosphorylation of FRS2α with IC50s of 7 and 9 nM in hFOB and SUM 52PE cells expressing different FGFR2 isoforms. Alofanib (0.2-0.8 μM, 6 hours) inhibits FGF-mediated proliferation in a panel of four cell lines representing several tumour types (triple-negative breast cancer, melanoma, and ovarian cancer) with GI50s of 16-370 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
In a FGFR-driven human tumour xenograft model, oral administration of alofanib (30 mg/kg, gavage, daily, 40 days, N=10) is well tolerated and results in potent antitumour activity. Treatment with alofanib (10 mg/kg/d, 0, 3 and 6 d, intraperitoneally) ablates experimental FGF-induced angiogenesis in vivo. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Tsimafeyeu I, et al. Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models. Eur J Cancer. 2016 Jul;61:20-8.
[2]. Khochenkov DA, et al. Antiangiogenic Activity of Alofanib, an Allosteric Inhibitor of Fibroblast Growth Factor Receptor 2. Bull Exp Biol Med. 2015 Nov;160(1):84-7.
溶解度数据
In Vitro: DMSO : ≥ 30.1 mg/mL (72.81 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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