Regorafenib | Multi-kinase inhibitor

CAS:
 755037-03-7
Catalog Number:
 10-4752

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Regorafenib (755037-03-7) is a multi-kinase inhibitor related to sorafenib1. Inhibits c-Raf, B-Raf, VEGFR1, VEGFR2, VEGFR3, Tie2, PDGFRb, FGFR1, c-Kit, and RET with IC50s=2.5, 28, 13, 4.2, 46, 311, 22, 202, 7 and 1.5 nM respectively.1,2 Enhances SHP-1 activity.3 Also inhibits soluble epoxide hydrolase (IC50=0.5 nM).4 Clinically useful anticancer agent.

References/Citations:

  1. Wilhelm et al. (2011), Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity; Int. J. Med. Cancer 129 245
  2. Uitdehaag et al. (2014), Comparison of the cancer gene targeting and biochemical selectivities of all targeted kinase inhibitors approved for clinical use; PLoS One 9 e92146
  3. Fan et al. (2014), SHP-1 is a target of regorafenib in colorectal cancer; Oncotarget 5 6243
  4. Hwang et al. (2013), Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors; Bioorg. Med. Chem. Lett. 23 3732
755037-03-7, BAY 73-4506, BAY 73-4506 supplier, Regorafenib, Regorafenib supplier
CAS:
755037-03-7
Catalog Number:
10-4752
Activity:
Multi-kinase inhibitor
Chemical Names:
4-[4-[[[[4-Chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide;
Alternate Name:
BAY 73-4506
Molecular Weight:
482.82
Molecular Formula:

C21H15ClF4N4O3

Solubility:
Soluble in DMSO (50 mg/ml)
Physical Properties:
Off-white solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

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Product Data Sheet:

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Regorafenib (755037-03-7) is a multi-kinase inhibitor related to sorafenib1. Inhibits c-Raf, B-Raf, VEGFR1, VEGFR2, VEGFR3, Tie2, PDGFRb, FGFR1, c-Kit, and RET with IC50s=2.5, 28, 13, 4.2, 46, 311, 22, 202, 7 and 1.5 nM respectively.1,2 Enhances SHP-1 activity.3 Also inhibits soluble epoxide hydrolase (IC50=0.5 nM).4 Clinically useful anticancer agent.

References/Citations:

  1. Wilhelm et al. (2011), Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity; Int. J. Med. Cancer 129 245
  2. Uitdehaag et al. (2014), Comparison of the cancer gene targeting and biochemical selectivities of all targeted kinase inhibitors approved for clinical use; PLoS One 9 e92146
  3. Fan et al. (2014), SHP-1 is a target of regorafenib in colorectal cancer; Oncotarget 5 6243
  4. Hwang et al. (2013), Synthesis and biological evaluation of sorafenib- and regorafenib-like sEH inhibitors; Bioorg. Med. Chem. Lett. 23 3732

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