Alofanib (RPT835)

• CAT Number: I000625
• CAS Number: 1612888-66-0
• Molecular Formula: C19H15N3O6S
• Molecular Weight: 413.4
• Purity: ≥95%
• Target: FGFR2 inhibitor
• Solubility: Soluble in DMSO, not in water
• Storage: Store at 4°C
• 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: CC1=CC(=C(C=C1C2=CN=CC=C2)NS(=O)(=O)C3=CC=CC(=C3)C(=O)O)[N+](=O)[O-]

Alofanib (Cat.No:I000625), also known as RPT835, is a potent and selective allosteric inhibitor of FGFR2 with potential anticancer activity. Alofanib blocks the extracellular part of the receptor and prevents its binding with the ligand. Alofanib suppressed proliferation of endothelial cells, their migration activity, and ability to form vessellike structures in vitro and significantly decreased the number of microvessels in Matrigel implant and in ovarian cancer (SKOV-3) xenograft in vivo. RPT835 potently inhibited growth of KATO III gastric cancer cells expressing FGFR2, with GI50 value of 10 nmol/L.

Reference

1: Tyulyandina A, Harrison D, Yin W, Stepanova E, Kochenkov D, Solomko E, Peretolchina N, Daeyaert F, Joos JB, Van Aken K, Byakhov M, Gavrilova E, Tjulandin S, Tsimafeyeu I. Alofanib, an allosteric FGFR2 inhibitor, has potent effects on ovarian cancer growth in preclinical studies. Invest New Drugs. 2016 Nov 3. [Epub ahead of print] PubMed PMID: 27812884. 2: Tsimafeyeu I, Ludes-Meyers J, Stepanova E, Daeyaert F, Kochenkov D, Joose JB, Solomko E, Van Akene K, Peretolchina N, Yin W, Ryabaya O, Byakhov M, Tjulandin S. 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. PubMed PMID: 27136102. 3: Tsimafeyeu I, Daeyaert F, Joos JB, Aken KV, Ludes-Meyers J, Byakhov M, Tjulandin S. Molecular Modeling, de novo Design and Synthesis of a Novel, Extracellular Binding Fibroblast Growth Factor Receptor 2 Inhibitor Alofanib (RPT835). Med Chem. 2016;12(4):303-17. PubMed PMID: 26732115. 4: Khochenkov DA, Solomko ES, Peretolchina NM, Ryabaya OO, Stepanova EV. 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. PubMed PMID: 26597690..