產(chǎn)品屬性：
產(chǎn)品名稱 | 規(guī)格 | CAS號 | 型號 |
Alofanib (RPT835) | 5mg 10mg 25mg 50mg 100mg | 1612888-66-0 | EY-Y0165151 |
Cas No.1612888-66-0
別名 N/A
化學(xué)名 N/A
分子式 C19H15N3O6S
分子量 413.4
溶解度 DMSO : ≥ 30.1 mg/mL (72.81 mM)
儲存條件 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
產(chǎn)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.
關(guān)鍵字： 1612888-66-0;C19H15N3O6S;Alofanib (RPT835);
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學(xué)、分子生物學(xué)和常規(guī)生化試劑等為一體的科研產(chǎn)品銷售企業(yè)，公司自成立以來，秉承""全心全意服務(wù)于科研工作者""的企業(yè)理念，立足生物科技領(lǐng)域，運用生物技術(shù)和科研試劑，發(fā)展現(xiàn)代生物科技，為各類大中小醫(yī)院及其它醫(yī)療機構(gòu)、高等院校、科研院所、企事業(yè)單位提供優(yōu)質(zhì)的產(chǎn)品，服務(wù)生物科技領(lǐng)域的科學(xué)研究人員。
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