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Alofanib

  Cat. No.:  DC11931   Featured
Chemical Structure
1612888-66-0
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More than 5000 active chemicals with high quality for research!
Field of application
Alofanib ((RPT-835) is a potent, selective, allosteric FGFR2 inhibitor that significantly inhibits bFGF-induced proliferation of HUVEC cells with IC50 of 11 nM
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1612888-66-0
Chemical Name: Alofanib
Synonyms: 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
SMILES: O=[N+](C1=CC(C)=C(C2=CC=CN=C2)C=C1NS(=O)(C3=CC(C(O)=O)=CC=C3)=O)[O-]
Formula: C19H15N3O6S
M.Wt: 413.4039
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer activities[1]. Antiangiogenic Activity[2].
In Vivo: In a FGFR-driven human tumour xenograft model, oral administration of alofanib (30 mg/kg) is well tolerated and resulted in potent antitumour activity[1]. Treatment with alofanib ablated experimental FGF-induced angiogenesis in vivo[1].
In Vitro: Alofanib inhibits phosphorylation of FRS2α with IC50s of 7 and 9 nM in cancer cells expressing different FGFR2 isoforms[1]. Alofanib (10-1000 nM) 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].
References: [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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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