性能参数 |
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产品名称 |
Alofanib |
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规格 |
5mg 10mg 25mg 50mg 100mg |
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货号 |
GOY-Y1896 |
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含量 |
>98.00% |
||
CAS |
1612888-66-0 |
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别名 |
N/A |
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化学名 |
N/A |
分子式 |
C19H15N3O6S |
分子量 |
分子 413.4 |
溶解度 |
DMSO : ≥ 30.1 mg/mL (72.81 mM) |
储存条件 |
Store at -20°C |
General tips |
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用途 |
仅供科研 |
价格 |
电询 |
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详细内容 |
Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer and antiangiogenic activity[1][2]. Alofanib inhibits phosphorylation of FRS2α with IC50s of 7 and 9 nM in cancer cells expressing different FGFR2 isoforms[1]. Alofanib (0.2, 0.4, 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[1].|| Cell Proliferation Assay[1]||Cell Line:|SKOV3, HS478T, Mel Kor cells|Concentration:|0.2, 0.4, 0.8 μM|Incubation Time:|6 hours after dosing, FGF2 is added at a concentration of 25 ng/ml|Result:|Alofanib inhibits growth of SKOV3 and HS578T cells with GI50s of 0.37 and 0.21 μM. Alofanib does not potently inhibit growth of Mel Kor cells that do not contain FGFR2 (GI50>10 μM)[1]. 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[1].Treatment with alofanib (10 mg/kg/d, 0, 3 and 6 d, intraperitoneally) ablates experimental FGF-induced angiogenesis in vivo[1].|| Animal Model:|C57Bl/6 × DBA/2 F1 mice of 22-30 g[1]|Dosage:|10 mg/kg/d|Administration:|Intraperitoneally, 0, 3 and 6 d|Result:|Alofanib inhibits angiogenesis in mouse models[1]. [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. |
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产品均为实验试剂,仅供科研实验使用,非药品、非食品、不可用于动物及人体!