An active metabolite of sorafenib; inhibits FLT3-ITD (Kd = 70 nM); inhibits proliferation of MV4-11 AML cells expressing FLT3-ITD (IC50 = 25.8 nM); selective for AML cell lines containing FLT3-ITD over lines containing wild-type FLT3 (IC50s = 3.9-13.3 µM); a linear-mixed inhibitor of CYP3A4 (Ki = 15 µM)

Sorafenib N-oxide – 5 mg

Brand:
Cayman
CAS:
583840-03-3
Storage:
-20
UN-No:
Non-Hazardous - /

Sorafenib N-oxide is an active metabolite of sorafenib (BAY 43-9006; Item No. 10009644), an inhibitor of Raf-1, B-RAF, and receptor tyrosine kinases.{48271} Sorafenib N-oxide inhibits FLT3 that contains the internal tandem duplication mutation (FLT3-ITD; Kd = 70 nM) and inhibits proliferation of MV4-11 acute myeloid leukemia (AML) cells expressing FLT3-ITD (IC50 = 25.8 nM). It is selective for AML cell lines containing FLT3-ITD over lines containing wild-type FLT3 (IC50s = 3.9-13.3 µM). Sorafenib N-oxide is also a linear-mixed inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 (Ki = 15 µM in human liver microsomes).{48272}  

 

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SKU: 27830 - 5 mg Category:

Description

An active metabolite of sorafenib; inhibits FLT3-ITD (Kd = 70 nM); inhibits proliferation of MV4-11 AML cells expressing FLT3-ITD (IC50 = 25.8 nM); selective for AML cell lines containing FLT3-ITD over lines containing wild-type FLT3 (IC50s = 3.9-13.3 µM); a linear-mixed inhibitor of CYP3A4 (Ki = 15 µM)

Formal name: 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]phenoxy]-N-methyl-2-pyridinecarboxamide, 1-oxide

Synonyms:  BAY 67-3472

Molecular weight: 480.8

CAS: 583840-03-3

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Kinase Inhibitors|VEGFR Family||Product Type|Biochemicals|Ox Stress Reagents||Product Type|Biochemicals|Small Molecule Inhibitors|Cytochrome P450||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Product Type|Biochemicals|Transporter & Exchanger Modulators||Product Type|Biochemicals|Xenobiotic Metabolites||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling||Research Area|Toxicology|Drug Metabolism|Cytochrome P450

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