Regorafenib (mesylate)

Regorafenib (BAY 73-4506) mesylate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib mesylate shows very robust antitumor and antiangiogenic activity[1].

Product Specifications

CAS Number

[835621-08-4]

Product Name Alternative

BAY 73-4506 (mesylate)

UNSPSC

12352005

Target

Autophagy; c-Kit; FGFR; PDGFR; Raf; RET; Tie; VEGFR

Type

Reference compound

Related Pathways

Autophagy; MAPK/ERK Pathway; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/regorafenib-mesylate.html

Solubility

10 mM in DMSO

Smiles

O=C(NC1=CC=C(C(C(F)(F)F)=C1)Cl)NC2=CC=C(OC3=CC(C(NC)=O)=NC=C3)C=C2F.CS(O)(=O)=O

Molecular Formula

C22H19ClF4N4O6S

Molecular Weight

578.92

References & Citations

[1]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.|[2]Carr BI, et al. Fluoro-Bay 43-9006 (Regorafenib) effects on hepatoma cells: growth inhibition, quiescence, and recovery. J Cell Physiol, 2013, 228 (2), 292-297.