Regorafenib

For research use only. Not for therapeutic Use.

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Regorafenib(Cat No.:A000931)is a multi-targeted tyrosine kinase inhibitor that blocks various receptors involved in tumor growth, angiogenesis, and metastasis, including VEGFR, PDGFR, and RAF kinases. It is approved for the treatment of metastatic colorectal cancer, advanced gastrointestinal stromal tumors (GIST), and hepatocellular carcinoma. By inhibiting these signaling pathways, regorafenib disrupts cancer cell proliferation and reduces blood vessel formation, ultimately slowing tumor progression. Its broad activity across multiple targets makes it an effective option for patients with advanced cancers, especially those resistant to other therapies.


Catalog Number A000931
CAS Number 755037-03-7
Synonyms

Fluoro-Sorafenib

Molecular Formula C₂₁H₁₅ClF₄N₄O₃
Purity ≥95%
Target c-RET
Solubility >25mg/mL in DMSO
Storage 3 years -20C powder
IUPAC Name 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
InChI InChI=1S/C21H15ClF4N4O3/c1-27-19(31)18-10-13(6-7-28-18)33-12-3-5-17(16(23)9-12)30-20(32)29-11-2-4-15(22)14(8-11)21(24,25)26/h2-10H,1H3,(H,27,31)(H2,29,30,32)
InChIKey FNHKPVJBJVTLMP-UHFFFAOYSA-N
SMILES CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F
Reference

</br>1: Ravi S, Singal AK. Regorafenib: an evidence-based review of its potential in patients with advanced liver cancer. Core Evid. 2014 Jul 17;9:81-7. doi: 10.2147/CE.S48626. eCollection 2014. Review. PubMed PMID: 25114628; PubMed Central PMCID: PMC4109634.</br>2: Abdel-Rahman O, Fouad M. Risk of cardiovascular toxicities in patients with solid tumors treated with sunitinib, axitinib, cediranib or regorafenib: An updated systematic review and comparative meta-analysis. Crit Rev Oncol Hematol. 2014 Jul 1. pii: S1040-8428(14)00114-0. doi: 10.1016/j.critrevonc.2014.06.003. [Epub ahead of print] Review. PubMed PMID: 25028151.</br>3: Khan G, Moss RA, Braiteh F, Saltzman M. Proactive strategies for regorafenib in metastatic colorectal cancer: implications for optimal patient management. Cancer Manag Res. 2014 Mar 4;6:93-103. doi: 10.2147/CMAR.S52217. eCollection 2014. Review. PubMed PMID: 24623990; PubMed Central PMCID: PMC3949557.</br>4: De Wit M, Boers-Doets CB, Saettini A, Vermeersch K, de Juan CR, Ouwerkerk J, Raynard SS, Bazin A, Cremolini C. Prevention and management of adverse events related to regorafenib. Support Care Cancer. 2014 Mar;22(3):837-46. doi: 10.1007/s00520-013-2085-z. Epub 2013 Dec 14. Review. PubMed PMID: 24337717; PubMed Central PMCID: PMC3913844.</br>5: Lyseng-Williamson KA. Regorafenib: a guide to its use in advanced gastrointestinal stromal tumor (GIST) after failure of imatinib and sunitinib. BioDrugs. 2013 Oct;27(5):525-31. doi: 10.1007/s40259-013-0061-2. Review. PubMed PMID: 23975637.</br>6: Regorafenib (Stivarga) for metastatic colorectal cancer and GIST. Med Lett Drugs Ther. 2013 Apr 29;55(1415):e36. Review. PubMed PMID: 23836345.</br>7: Sirohi B, Philip DS, Shrikhande SV. Regorafenib: carving a niche in the crowded therapeutic landscape. Expert Rev Anticancer Ther. 2013 Apr;13(4):385-93. doi: 10.1586/era.13.12. Review. PubMed PMID: 23560833.</br>8: Davis SL, Eckhardt SG, Messersmith WA, Jimeno A. The development of regorafenib and its current and potential future role in cancer therapy. Drugs Today (Barc). 2013 Feb;49(2):105-15. doi: 10.1358/dot.2013.49.2.1930525. Review. PubMed PMID: 23462625.</br>9: Roman D, Whiteside R. Regorafenib: Adding to the Armamentarium for Refractory Colorectal Cancer and GIST. J Adv Pract Oncol. 2013 Mar;4(2):118-22. Review. PubMed PMID: 25031991; PubMed Central PMCID: PMC4093419.</br>10: Aprile G, Macerelli M, Giuliani F. Regorafenib for gastrointestinal malignancies : from preclinical data to clinical results of a novel multi-target inhibitor. BioDrugs. 2013 Jun;27(3):213-24. doi: 10.1007/s40259-013-0014-9. Review. PubMed PMID: 23435872.</br>11: Strumberg D, Schultheis B. Regorafenib for cancer. Expert Opin Investig Drugs. 2012 Jun;21(6):879-89. doi: 10.1517/13543784.2012.684752. Review. PubMed PMID: 22577890.</br>

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