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BAY-73-4506 (Regorafenib) | Tyrosine kinase inhibitor

  • BAY-73-4506 (Regorafenib) (.png)
  • BAY-73-4506 (Regorafenib) (.jpg)
Price:
$129.00
Catalog #:
C2734-5
Quantity:


Product Description

BAY-73-4506 (Regorafenib) is an orally active and highly potent inhibitor against multiple tyrosine kinases, including VEGFR1/2/3, PDGFR?, Kit, RET and Raf-1. Regorafenib inhibits the proliferation of HUVEC cells stimulated with VEGF, and inhibits FGFR signaling in breast cancer MCF-7 cells stimulated with FGF. Regorafenib is anti-angiogenic due to its inhibitions against VEGFR2-TIE2 tyrosine kinase. [1]
Co-administration of Regorafenib and a PI3K/Akt inhibitor (MK-2206) clearly demonstrated synergistic effect in a HCT116 xenocraft mouse model [2]. Regorafenib is currently being studied as a potential treatment option in multiple tumor types, and has recently be approved in treating patients with Metastatic Colorectal cancer. [3]


Technical information:

Chemical Formula:   C21H15ClF4N4O3
CAS #:   755037-03-7
Molecular Weight:   482.82
Purity:   > 98%
Appearance:   White
Chemical Name:   1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea
Solubility:   Up to 100 mM in DMSO
Synonyms:   BAY-73-4506, BAY73-4506, Regorafenib, Fluoro-Sorafenib

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.


Reference:

1. Wilhelm SM et al, Regorafenib (BAY 73-4506): a new oral multi-kinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer. 2011; 129:245-55 Pubmed ID: 21170960
2. Sajithlal GB et al. Sorafenib/regorafenib and phosphatidyl inositol 3 kinase/thymoma viral proto-oncogene inhibition interact to kill tumor cells. Mol Pharmacol. 2013; 84(4):562-71. Pubmed ID: 23877009
3. Carter NJ. Regorafenib: a review of its use in previously treated patients with progressive metastatic colorectal cancer. Drugs Aging. 2014; 31(1):67-78. Pubmed ID: 24276917

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.




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