RPT-835(alofanib)
RPT-835(alofanib) Basic information
- Product Name:
- RPT-835(alofanib)
- Synonyms:
-
- RPT835
- RPT-835(alofanib)
- 3-(N-(4-methyl-2-nitro-5-(pyridin-3-yl)phenyl)sulfamoyl)benzoic acid
- Alofanib (RPT835)
- Alofanib
- CS-2880
- ES 000835
- RPT-835;RPT835;RPT 835;ES 000835
- CAS:
- 1612888-66-0
- MF:
- C19H15N3O6S
- MW:
- 413.4
- Mol File:
- 1612888-66-0.mol
RPT-835(alofanib) Chemical Properties
- Boiling point:
- 659.6±65.0 °C(Predicted)
- Density
- 1.488±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:47.7(Max Conc. mg/mL);115.38(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:6):0.14(Max Conc. mg/mL);0.34(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);72.57(Max Conc. mM) - form
- A crystalline solid
- pka
- 3.59±0.10(Predicted)
- color
- Light yellow to yellow
- InChI
- InChI=1S/C19H15N3O6S/c1-12-8-18(22(25)26)17(10-16(12)14-5-3-7-20-11-14)21-29(27,28)15-6-2-4-13(9-15)19(23)24/h2-11,21H,1H3,(H,23,24)
- InChIKey
- QUQGQIASFYWKAB-UHFFFAOYSA-N
- SMILES
- C(O)(=O)C1=CC=CC(S(NC2=CC(C3=CC=CN=C3)=C(C)C=C2[N+]([O-])=O)(=O)=O)=C1
RPT-835(alofanib) Usage And Synthesis
Uses
Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer and antiangiogenic activity[1][2].
in vivo
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]. |
IC 50
FGFR2
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. DOI:10.1016/j.ejca.2016.03.068
[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. DOI:10.1007/s10517-015-3104-5
RPT-835(alofanib)Supplier
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