Alofanib

• CAS: 1612888-66-0
• Catalog Number: ACM1612888660
• Category: Inhibitors
• Molecular Weight: 413.40
• Molecular Formula: C19H15N3O6S
• Description: Alofanib, 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.
• Synonyms: RPT835; RPT-835; RPT 835; Alofanib
• IUPAC Name: 3-(N-(4-methyl-2-nitro-5-(pyridin-3-yl)phenyl)sulfamoyl)benzoic acid
• Canonical SMILES: O=[N+](C1=CC(C)=C(C2=CC=CN=C2)C=C1NS(=O)(C3=CC(C(O)=O)=CC=C3)=O)[O-]
• 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)
• InChI Key: QUQGQIASFYWKAB-UHFFFAOYSA-N
• Solubility: Soluble in DMSO, not in water
• Appearance: Solid powder
• Shelf Life: >2 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Biological Target: Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2).
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 55.20; H, 3.66; N, 10.16; O, 23.22; S, 7.76
• Exact Mass: 413.06816
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: Alofanib was evaluated for antiproliferative activity against the human ovarian cancer FGFR-expressing cell line in FGF-mediated signaling model. FGF2 significantly increased proliferation of the ovarian cancer cells in untreated control group (P = 0.001). Cells were treated with increasing concentrations of alofanib ranging from 0 to 1 μmol/L. Compound significantly inhibited FGF-triggered cell proliferation in dose-dependent manner (P < 0.001). To find out whether alofanib could demonstrate cytotoxic activity in vitro, this study examined the effect of compound on SKOV3 cell line by MTT assay. Alofanib displayed low cytotoxic effect on ovarian cancer cells. Compound inhibited growth of SKOV3 cells with GI50 value of 0.37 μmol/L (Fig. 2a).; Reference: Invest New Drugs. 2017 Apr;35(2):127-133. https://pubmed.ncbi.nlm.nih.gov/27812884/
• In Vivo Activity: Ability of alofanib to block tumor angiogenesis in vivo in tumors was evaluated on the model of human serous ovarian cancer SKOV-3 inoculated to mice with immune deficiency. Peroral administration of alofanib (50 mg/kg) reduced the number of CD31+ microvessels in tumor tissue by 48.9% in comparison with the control (p<0.001, Table 2). Histological analysis revealed significant dilatation and plethora of tumor microvessels and extensive hemorrhages.; Reference: Bull Exp Biol Med. 2015 Nov;160(1):84-7. https://pubmed.ncbi.nlm.nih.gov/26597690/
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).