产品属性:
产品名称 | 规格 | CAS号 | 型号 |
Alofanib (RPT835) | 5mg 10mg 25mg 50mg 100mg | 1612888-66-0 | EY-Y0165151 |
Cas No.1612888-66-0
别名 N/A
化学名 N/A
分子式 C19H15N3O6S
![Alofanib (RPT835).png Alofanib (RPT835).png](/SupplyImg/2022-11-28/6380524945152962954913418.jpg)
分子量 413.4
溶解度 DMSO : ≥ 30.1 mg/mL (72.81 mM)
储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述:
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.
关键字: 1612888-66-0;C19H15N3O6S;Alofanib (RPT835);
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要从事免疫学、分子生物学和常规生化试剂等为一体的科研产品销售企业,公司自成立以来,秉承""全心全意服务于科研工作者""的企业理念,立足生物科技领域,运用生物技术和科研试剂,发展现代生物科技,为各类大中小医院及其它医疗机构、高等院校、科研院所、企事业单位提供优质的产品,服务生物科技领域的科学研究人员。
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