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Cat. No. Name Size Price Add Cart
KI1326Regorafenib5 mg$192
Regorafenib10 mg$336
Regorafenib25 mg$752
Regorafenib100 mg$2032

Chemical Characteristic

Product NameRegorafenib
SynonymsBAY 73-4506, Stivarga
CAS No.755037-03-7
Molecular Weight 482.82
FormulaC21H15ClF4N4O3
Chemical Name1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea
Smilesc1(cc(ccn1)Oc1cc(c(cc1)NC(=O)Nc1cc(c(cc1)Cl)C(F)(F)F)F)C(=O)NC
Chemical Structure

Biological activities

Regorafenib is an oral multi-kinase inhibitor. Regorafenib shows anti-angiogenic activity due to its dual targeted VEGFR2-TIE2 tyrosine kinase inhibition. Regorafenib inhibis the receptor tyrosine kinases (RTKs) VEGFR2, PDGFR-β and FGFR in biochemical and cellular assays within the nanomolar range (3 - 200 nM).[1] Regorafenib inhibits Kit??Ret??Raf-1 and VEGFR1 with IC50 of 7, 1.5 and 2.5 nM, respectively. In contrast??egorafenib inhibits murine VEGFR2 and murine VEGFR3 with IC50 of 4.2 and 46 nM, respectively. The IC50 of regorafenib is 311 and 22 nM against Tie2 and PDGFR-β, respectively. Regorafenib potently inhibits VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with an IC50 of 3 nM. Regorafenib prevents PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM, in HAoSMCs cells. Regorafenib also suppresses FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10. Regorafenib very potently inhibits the mutant receptors KITK642E and RETC634W, with IC50 values of 20 and 10 nM, respectively.[2] Regorafenib concentration- and time-dependently inhibits growth of human Hep3B, PLC/PRF/5, and HepG2 cells.[3] Regorafenib inhibits tumor vasculature and tumor growth in a rat GS9L glioblastoma model. Regorafenib effectively inhibits the RAF/MEK/ERK signaling cascade. Regorafenib significantly inhibits tumor growth in a wide range of additional xenografts derived from lung, melanoma, pancreatic and ovarian tumor cell lines at doses of 10 and 30 mg/kg, [2]

Protocols

In vitro: Regorafenib is dissolved in 0.1% BSA/DMEM/0.1% dimethylsulfoxide (DMSO).[2]

References

[1] Strumberg D, et al. Regorafenib for cancer. Expert Opin Investig Drugs. 2012, 21(6): 879-889.
[2] Wilhelm SM, et al. Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer. 2011, 129(1): 245-255.
[3] Carr BI, et al. Fluoro-Sorafenib (Regorafenib) effects on hepatoma cells: Growth inhibition, quiescence, and recovery. J Cell Physiol. 2013, 228(2): 292-297.

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