Regorafenib – 5 mg

Brand:
Cayman
CAS:
755037-03-7
Storage:
-20
UN-No:
Non-Hazardous - /

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, respectivey) 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.  

 

Available on backorder

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Description

A multi-kinase inhibitor; inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ (IC50s = 1.5, 2.5, 4.2, 7, 13, and 22 nM, respectively); inhibits B-RAF, VEGFR3, FGFR, and Tie2 (IC50s = 28, 46, 202, and 311 nM, respectively); reduces tumor size in the MDA-MB-231 breast and 786-O renal cancer mouse xenograft models at 10 mg/kg; reduces tumor microvessel area and inhibits tumor growth in a panel of mouse xenograft models


Formal name: 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-2-pyridinecarboxamide

Synonyms:  BAY 73-4506

Molecular weight: 482.8

CAS: 755037-03-7

Purity: ≥98%

Formulation: A crystalline solid


Product Type|Biochemicals|Kinase Inhibitors|FGFR Family||Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||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|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Signaling|ERK/MAPK Signaling||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling