Regorafenib - CAS 755037-03-7
Catalog number: B0084-151007
Category: Inhibitor
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Regorafenib, also known as BAY 73-4506, is an orally bioavailable small molecule with potential antiangiogenic and antineoplastic activities. Regorafenib binds to and inhibits vascular endothelial growth factor receptors (VEGFRs) 2 and 3, and Ret, Kit, PDGFR and Raf kinases, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation. VEGFRs are receptor tyrosine kinases that play important roles in tumor angiogenesis; the receptor tyrosine kinases RET, KIT, and PDGFR, and the serine/threonine-specific Raf kinase are involved in tumor cell signaling. Regorafenib is demonstrated to increase the overall survival of patients with metastatic colorectal cancer and has been approved by the US FDA on September 27, 2012.
Brife Description:
inhibitor of VEGFRs, antineoplastic agent
Off-white to light pink solid powder
Regorafenibum; Stivarga; 4-(4-(3-(4-Chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide; BAY 73-4506; BAY 734506; BAY734506; BAY-734506
antineoplastic agent
Shelf Life:
2 years
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1.Quantitative determination of regorafenib and its two major metabolites in human plasma with high-performance liquid chromatography and ultraviolet detection.
Fujita K1, Miura M1, Shibata H2. Biomed Chromatogr. 2016 Apr 2. doi: 10.1002/bmc.3730. [Epub ahead of print]
A simple, highly sensitive and specific high-performance liquid chromatography (HPLC) method was developed for the simultaneous quantitation of regorafenib, N-oxide metabolite (M-2) and the desmethyl N-oxide metabolite (M-5) in human plasma. Regorafenib, M-2 and M-5 and the internal standard sorafenib were separated using a mobile phase of 0.5% KH2 PO4 (pH 3.5)-acetonitrile (30:70, v/v), on a CAPCELL PAK MG II column at a flow rate of 0.5 mL/min and measurement at UV 260 nm. The lower limits of quantification for regorafenib, M-2 and M-5 were 10 ng/mL for each analyte. A procedure using solid-phase extraction required only a small amount of plasma (100 μL) for one analysis while providing high extraction recovery (>81% for all compounds) and good selectivity. Coefficients of variation for intra- and inter-day assays were less than 12.2% for regorafenib, less than 12.3% for M-2 and less than 15.1% for M-5. Accuracies for intra- and inter-day assays were within 9.
2.Toxicity and early outcomes of regorafenib in multiply pre-treated metastatic colorectal adenocarcinoma-experience from a tertiary cancer centre in India.
Zanwar S1, Ostwal V1, Gupta S1, Sirohi B1, Toshniwal A1, Shetty N1, Banavali S1. Ann Transl Med. 2016 Feb;4(4):74. doi: 10.3978/j.issn.2305-5839.2016.02.05.
BACKGROUND: Regorafenib is a multikinase inhibitor (MKI) approved for use in multiply pre-treated metastatic colorectal cancers (mCRC). To the best of our knowledge, this is the first report of regorafenib from India.
3.Pazopanib plus best supportive care versus best supportive care alone in advanced gastrointestinal stromal tumours resistant to imatinib and sunitinib (PAZOGIST): a randomised, multicentre, open-label phase 2 trial.
Mir O1, Cropet C2, Toulmonde M3, Cesne AL1, Molimard M4, Bompas E5, Cassier P6, Ray-Coquard I6, Rios M7, Adenis A8, Italiano A3, Bouché O9, Chauzit E4, Duffaud F10, Bertucci F11, Isambert N12, Gautier J2, Blay JY13, Pérol D2; PAZOGIST study group of the F Lancet Oncol. 2016 Apr 5. pii: S1470-2045(16)00075-9. doi: 10.1016/S1470-2045(16)00075-9. [Epub ahead of print]
BACKGROUND: Gastrointestinal stromal tumours (GIST) are the most common mesenchymal neoplasms of the gastrointestinal tract. Imatinib followed by sunitinib and regorafenib is the standard sequence of treatment for advanced disease. Pazopanib is effective in soft tissue sarcomas but has never been assessed in advanced GIST in a randomised trial. We aimed to assess the efficacy and safety of pazopanib in patients with previously treated advanced GIST.
4.Efficacy and Safety of TAS-102 in Clinical Practice of Salvage Chemotherapy for Metastatic Colorectal Cancer.
Arita S1, Shirakawa T2, Matsushita Y3, Shimokawa HK4, Hirano G5, Makiyama A5, Shibata Y6, Tamura S7, Esaki T2, Mitsugi K3, Ariyama H4, Kusaba H4, Akashi K4, Baba E8. Anticancer Res. 2016 Apr;36(4):1959-66.
BACKGROUND: TAS-102 is an anti-metabolite which demonstrated activity against multidrug-resistant advanced colorectal cancer. Its major toxicities are hematological disorders.
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CAS 755037-03-7 Regorafenib

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