Alofanib

Names

[ Name ]:
Alofanib

[Synonym ]:
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)

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
659.6±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₉H₁₅N₃O₆S

[ Molecular Weight ]:
413.40

[ Flash Point ]:
352.7±34.3 °C

[ Exact Mass ]:
413.068146

[ LogP ]:
4.00

[ Vapour Pressure ]:
0.0±2.1 mmHg at 25°C

[ Index of Refraction ]:
1.667

[ Storage condition ]:
-20℃