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Regorafenib

CAT: 0013-GTR19161571-01Size: 500 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19161571-01Size:500 mg
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Description
A potent multikinase inhibitor that potently inhibits these endothelial cell kinases in biochemical and cellular kinase phosphorylation assays with nanomolar range (IC50=3-200 nM) ; inhibits VEGFR1/2/3, PDGFRβ, FGFR1, KIT, RET and B-RAF etc.; exhibits potent dose-dependent TGI in various preclinical human xenograft models in mice; orally active.Colon Cancer Approved (In Vitro) :Regorafenib (0-10 μM, 96 h) shows anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells.Regorafenib (0-3000 nM, 30 min) inhibits the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, and inhibits FGFR and pERK1/2.Regorafenib causes a concentration-dependent decrease in Hep3B cell growth, with an IC50 of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells. (In Vivo) :Regorafenib (10 mg/kg, Orally, single dose or daily for 4 days) inhibits tumor vasculature and tumor growth in a rat GS9L glioblastoma model.Regorafenib (0-100 mg/kg, Orally, qd x 9) exhibits antitumorigenic and antiangiogenic effects in the Colo-205, MDA-MB-231 and 786-O model.
CAS Number
755037-03-7
Product Name Alternative
BAY 73-4506 | BAY73-4506
Field of Research
Pharmacology & Drug Discovery
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 260 mg/mL
Smiles
C12=NC (NC3=CC=C (N4CCOCC4) C=C3) =NC (NC5CCCCC5) =C1NC=N2
Molecular Formula
C21H15ClF4N4O3
Molecular Weight
482.8154
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
2-Pyridinecarboxamide, 4-[4-[[[[4-chloro-3- (trifluoromethyl) phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-

Alternative Products

CatalogName
A8236-50Regorafenib

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