Shelf life (days): 1460.0
Formulation: A solid
Formal Name: 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-(methyl-13C-d3)-2-pyridinecarboxamide
Purity: ≥99% deuterated forms (d1-d3)
Formula Markup: C20[13C]H12D3ClF4N4O3
Formula Weight: 486.8
CAS Number: 2126178-55-8
Notes: Regorafenib-13C-d3 is intended for use as an internal standard for the quantification of regorafenib (Item No. 18498) by GC- or LC-MS. Regorafenib is an orally bioavailable multi-kinase inhibitor with anticancer activity.{29730} 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.{29730,27528,29728} In vivo, regorafenib (10 mg/kg) reduces tumor size in the MDA-MB-231 breast and 786-O renal cancer mouse xenograft models.{29730} 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.
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