WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206428
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.
MedKoo Cat#: 206428
Chemical Formula: C19H15N3O6S
Exact Mass: 413.06816
Molecular Weight: 413.4
Elemental Analysis: C, 55.20; H, 3.66; N, 10.16; O, 23.22; S, 7.76
Alofanib, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.
Synonym: RPT835; RPT-835; RPT 835; Alofanib
IUPAC/Chemical Name: 3-(N-(4-methyl-2-nitro-5-(pyridin-3-yl)phenyl)sulfamoyl)benzoic acid
InChi Key: QUQGQIASFYWKAB-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: O=[N+](C1=CC(C)=C(C2=CC=CN=C2)C=C1NS(=O)(C3=CC(C(O)=O)=CC=C3)=O)[O-]
The following data is based on the product molecular weight 413.4 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
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.