Alofanib (RPT835)

Alofanib is a novel selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2) tyrosine kinase. It inhibits phosphorylation of FGF receptor substrate 2alpha (FRS2alpha) with IC50 values of 7nM and 9nM in cancer cells expressing different FGFR2 isoforms. It inhibits FGF-mediated proliferation in a panel of four cell lines representing tumor types such as triple-negative breast cancer, melanoma, and ovarian cancer with 50% growth inhibition (GI50) values of 16nM-370nM. It inhibits the proliferation and migration of human and mouse endothelial cells. It ablates experimental FGF-induced angiogenesis in vivo. Oral administration of alofanib shows potent antitumor activity in a FGFR-driven human tumor xenograft model.

https://pubchem.ncbi.nlm.nih.gov/compound/86280646

Small volumes of Alofanib biochemical vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS8400450 is a biochemical targeting Alofanib.