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Regorafenib-13C-d3 is intended for use as an internal standard for the quantification of regorafenib by GC- or LC-MS. Regorafenib is an orally bioavailable multi-kinase inhibitor with anticancer activity.1 It inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ with IC50 values of 1.5, 2.5, 4.2, 7, 13, and 22 nM, respectively. Regorafenib also inhibits B-RAF, VEGFR3, FGFR, and Tie2 (IC50s = 28, 46, 202, and 311 nM, respectively) as well as other kinases.1,2,3 In vivo, regorafenib (10 mg/kg) reduces tumor size in the MDA-MB-231 breast and 786-O renal cancer mouse xenograft models.1 It also reduces tumor microvessel area and inhibits tumor growth in a panel of mouse xenograft models. Formulations containing regorafenib have been used in the treatment of advanced gastrointestinal stromal tumors and metastatic colorectal cancer. | [References]
1. Wilhelm, S.M., Dumas, J., Adnane, L., et al. Regorafenib (BAY 73-4506): A new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity Int. J. Cancer 129(1),245-255(2011).
2. Uitdehaag, J.C.M., de Roos, J.A.D.M., van Doornmalen, A.M., et al. Comparison of the cancer gene targeting and biochemical selectivities of all targeted kinase inhibitors approved for clinical use PLoS One 9(3),1-13(2014).
3. Ravi, S., and Singal, A.K. Regorafenib: An evidence-based review of its potential in patients with advanced liver cancer Core Evid. 9,81-87(2014). |
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Boao Pike
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010-57798038 15652371397 |
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www.biopike.cn |
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