An active metabolite of regorafenib
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Regorafenib N-oxide

Item No. 35101

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide 1-oxide
CAS Number
835621-11-9
Molecular Formula
C21H15ClF4N4O4
Formula Weight
498.8
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
264 nm
SMILES
O=C(NC1=C(F)C=C(OC2=CC=[N+](C(C(NC)=O)=C2)[O-])C=C1)NC3=CC(C(F)(F)F)=C(Cl)C=C3
InChi Code
InChI=1S/C21H15ClF4N4O4/c1-27-19(31)18-10-13(6-7-30(18)33)34-12-3-5-17(16(23)9-12)29-20(32)28-11-2-4-15(22)14(8-11)21(24,25)26/h2-10H,1H3,(H,27,31)(H2,28,29,32)
InChi Key
NUCXNEKIESREQY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    Regorafenib N-oxide is an active metabolite of the multi-kinase inhibitor regorafenib (Item No. 18498).1 It is formed from regorafenib by the cytochrome P450 (CYP) isoform CYP3A4. Regorafenib N-oxide inhibits VEGFR2, Tie2, c-Kit, and B-RAF in vitro, as well as inhibits tumor growth in HT-29 and MDA-MB-231 mouse xenograft models when administered at a dose of 1 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Li, Y.-H., Lin, Q.-M., Pang, N.-H., et al. Functional characterization of 27 CYP3A4 protein variants to metabolize regorafenib in vitro. Basic Clin. Pharmacol. Toxicol. 125(4), 337-344 (2019).

    2. Zopf, D., Heinig, R., Thierauch, K.-H., et al. Abstract 1666: Regorafenib (BAY 73-4506): Preclinical pharmacology and clinical identification and quantification of its major metabolites. Cancer. Res. 70(8 Suppl.), (2010).