1612888-66-0

1612888-66-0 structure

Name: Alofanib
Chemical Name: Alofanib
CAS Number: 1612888-66-0
Molecular Formula: C₁₉H₁₅N₃O₆S
Molecular Weight: 413.40
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK FGFR
Create Date: 2018-03-29 08:00:00
Modify Date: 2024-01-24 15:57:46
Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer activities[1]. Antiangiogenic Activity[2].

Name	Alofanib
Synonyms	3-{[4-Methyl-2-nitro-5-(3-pyridinyl)phenyl]sulfamoyl}benzoic acid Benzoic acid, 3-[[[4-methyl-2-nitro-5-(3-pyridinyl)phenyl]amino]sulfonyl]- Alofanib (RPT835)

Description	Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer activities[1]. Antiangiogenic Activity[2].
Related Catalog	Research Areas >> Cancer Research Areas >> Cardiovascular Disease Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FGFR
Target	FGFR2
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].
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].
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.