Regorafenib

  • Chemical Properties
CAS No. 755037-03-7 Cat. No. BCP02105
Name Regorafenib
Synonyms BAY 734506; BAY734506; BAY-734506;BAY 73-4506;BAY73-4506;
Formula C21H15ClF4N4O3 M. Wt 482.82
  • Biological Activity
Description Regorafenib strongly prevents VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs, regorafenib suppress PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. Regorafenib also inhibits FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10. Regorafenib very potently inhibited the mutant receptors KITK642E and RETC634W, with IC50 of approximately 20 nM and 10 nM, respectively. Regorafenib inhibits the proliferation of VEGF165-stimulated HUVECs, with an IC50 of approximately 3 nM. Regorafenib prevents the proliferation of FGF2-stimulated HUVECs and of PDGF-BB-stimulated HAoSMCs with IC50 of 127 nM and 146 nM, respectively.
Related Products 1019206-88-2(Regorafenib monohydrate) 835621-07-3(Regorafenib hydrochloride)
Pathways Angiogenesis/Protein Tyrosine Kinase MAPK Pathway 
Targets PDGFR VEGFR c Kit RET Raf 

Structure

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