R-8024 Regorafenib, Free Base, >99%

Synonyms : [Bay 73-4506] [Fluoro-Sorafenib]

Related Terms : [Stivarga]

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  • 25 mg
  • 48
  • 44
  • 38
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  • 50 mg
  • 69
  • 63
  • 54
  • 7,600
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  • 100 mg
  • 107
  • 98
  • 85
  • 11,800
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  • 200 mg
  • 178
  • 163
  • 141
  • 19,700
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  • 250 mg
  • 213
  • 196
  • 169
  • 23,600
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  • 500 mg
  • 398
  • 366
  • 316
  • 44,000
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  • 1 g
  • 685
  • 630
  • 544
  • 75,800
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  • 2 g
  • 1,190
  • 1,095
  • 946
  • 131,700
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  • M.W. 482.82
  • C21H15ClF4N4O3
  • [755037-03-7]

  • Regorafenib demonstrated tolerability and antitumour activity in patients with metastatic colorectal cancer (CRC) in a phase 1 clinical trail. Strumberg D., et al. "Regorafenib (BAY 73-4506) in advanced colorectal cancer: a phase I study." Br. J. Cancer 106: 1722-1727 (2012).
  • In combination chemotherapy, regorafenib showed acceptable tolerability with SN-38 and irinotecan but showed no significant effect on oxaliplatin or 5-fluorouracil pharmacokinetics. Schultheis B., et al. "Regorafenib in combination with FOLFOX or FOLFIRI as first- or second-line treatment of colorectal cancer: results of a multicenter, phase Ib study." Ann. Oncol. 24: 1560-1567 (2013).
  • Regorafenib showed significant activity in patients with advanced and metastatic GI stromal tumor (GIST) after failure of both imatinib and sunitinib in a phase 2 clinical trial. George S., et al. "Efficacy and safety of regorafenib in patients with metastatic and/or unresectable GI stromal tumor after failure of imatinib and sunitinib: a multicenter phase II trial." J. Clin. Oncol. 30: 2401-2407 (2012).
  • In a phase 2 clinical trial, regorafenib demonstrated acceptable tolerability and antitumour activity in patients with intermediate or advanced hepatocellular carcinoma (HCC) after failure of first-line sorafenib. Bruix J., et al. "Regorafenib as second-line therapy for intermediate or advanced hepatocellular carcinoma: Multicentre, open-label, phase II safety study." Eur. J. Cancer 49: 3412-3419 (2013).
  • In a phase 3 study, regorafenib demonstrated prolonged survival of patients with metastatic colorectal cancer after standard therapies failed. Grothey A., et al. "Regorafenib monotherapy for previously treated metastatic colorectal cancer (CORRECT): an international, multicentre, randomised, placebo-controlled, phase 3 trial." Lancet 381: 303-312 (2013).
  • Regorafenib demonstrated antitumour activity as a first-line treatment for metastatic or unresectable renal-cell carcinoma in a phase 2 clinical trial. However, the drug's safety profile required close monitoring. Eisen T., et al. "Regorafenib for patients with previously untreated metastatic or unresectable renal-cell carcinoma: a single-group phase 2 trial." Lancet Oncol. 13: 1055-1062 (2012).
  • Oral regorafenib significantly improved progression-free survival when compared with placebo in patients with metastatic gastrointestinal stromal tumours (GIST) after failure of standard treatments in a phase 3 clinical trial. Demetri G.D., et al. "Efficacy and safety of regorafenib for advanced gastrointestinal stromal tumours after failure of imatinib and sunitinib (GRID): an international, multicentre, randomised, placebo-controlled, phase 3 trial." Lancet 381: 295-302 (2013).
  • Regorafenib is the active ingredient in the drug product sold under the trade name Stivarga®. This drug is currently approved in at least one country for use in patients with metastatic colorectal cancer and patients with advanced gastrointestinal stromal tumors which cannot be removed surgically and no longer respond to other FDA-approved treatments for this disease. NOTE: THE REGORAFENIB, FREE BASE RESEARCH COMPOUND SOLD BY LC LABORATORIES IS NOT STIVARGA®, AND IS NOT FOR HUMAN USE.
  • Related CAS numbers: 835621-07-3 for the hydrochloride salt.
  • Other CAS numbers previously assigned to Regorafenib, Free Base, namely 1219951-07-1 and 1370461-45-2, have been deleted by CAS and are no longer in use.
  • Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
  • Not available in some countries; not available to some institutions; not available for some uses.
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