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product name Regorafenib (BAY 73-4506)


ReferencesInt J Cancer, 2011, 129(1), 245-255.



Molecular Weight (MW)

482.82
Formula

C21H15ClF4N4O3
CAS No.

755037-03-7
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 97 mg/mL (200.9 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol:
Solubility (In vivo)

 30% PEG400+0.5% Tween80+5% Propylene glycol: 30mg/mL
Chemical Name

1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19403294

Regorafenib targets both tumor cell proliferation and tumor vasculature through inhibition of receptors of tyrosine kinases (VEGFR, KIT, RET, FGFR, and PDGFR) and serine/threonine kinases (Raf and p38MAPK).
In Vivo Regorafenib reveals potent dose-dependent TGI in various preclinical human xenograft models in mice, with tumor shrinkages in breast MDA-MB-231 and renal 786-O carcinoma models. Regorafenib prevents not only the growth of syngeneic primary 4T1 breast tumors growing orthotopically in the fat pad, but also suppresses the formation of tumor metastasis in the lung.
Animal model Female athymic NCr nu/nu mice with Colo-205, MDA-MB-231 or 786-O
Formulation & Dosage PEG400/125 mM aqueous methanesulfonic acid (80/20) or polypropylene glycol/PEG400/Pluronic F68 (42.5/42.5/15 + 20% Aqua); 3, 10, 30, 200 mg/kg; oral
References [1] Wilhelm SM, et al. Int J Cancer, 2011, 129(1), 245-255.

Gadodiamide (hydrate)