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Regorafenib monohydrate

Cat No.
CEI-1495
Product Overview
Regorafenib monohydrate is a multitargeted inhibitor of tyrosine kinase with IC50 values of 13nM, 4.2nM, 46nM, 2.5nM, 28nM, 19nM, 202nM, 22nM, 7nM, 1.5nM and 311nM, respectively for VEGFR-1, mVEGFR-2, mVEGFR-3, Raf-1, BRAF WT, BRAFV600E, FGFR-1, PDGFR-β, c-KIT, RETand TIE2. Regorafenib is a multikinase inhibitor of both intracellular and membrane-bound RTKs. It shows potent inhibition of angiogenic and stromal RTKs like VEGF receptors-1-3, PDGFR-β and FGF receptor-1 with IC50 values ranging from4.2 to 311nM in biochemical assays. It also inhibits oncogenic RTKs, such as RET and c-KIT, with IC50 values ranging from 1.5 to 28nM in cellular assays. Regorafenib is reported to have anti-tumor efficacy to various tumors including breast, pancreas, thyroid, melanoma, GIST, and CRC with a mean IC50 value less than 1μM. These inhibition effects of tumor growth are also found in mouse xenograft models after the treatment of regorafenib at dose ranging from 10 to 100 mg/kg.
CAS No.
1019206-88-2
Molecular Weight
500.83
Purity
0.9928
Storage
Store at -20°C
Synonyms
BAY 73-4506 monohydrate
Targets
Tyrosine kinase
Molecular Formula
C21H17ClF4N4O4
Chemical Name
4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide; hydrate
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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