Regorafenib (monohydrate)
Regorafenib (BAY 73-4506) monohydrate 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 monohydrate shows very robust antitumor and antiangiogenic activity[1].
Product Specifications
CAS Number
1019206-88-2
Product Name Alternative
BAY 73-4506 (monohydrate)
UNSPSC
12352005
Hazard Statement
H361, H373, H410
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-monohydrate.html
Concentration
10mM
Purity
99.94
Solubility
DMSO : 50 mg/mL (ultrasonic)
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.O
Molecular Formula
C21H17ClF4N4O4
Molecular Weight
500.83
Precautions
H361, H373, H410
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]Heng DY, et al. Targeted therapy for metastatic renal cell carcinoma: current treatment and future directions. Ther Adv Med Oncol, 2010, 2 (1), 39-49.|[3]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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
B-Raf; C-Raf; PDGFRβ; Tie2; VEGFR1/Flt-1; VEGFR2/KDR/Flk-1; VEGFR3/Flt-4
Citation 01
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