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Regorafenib monohydrate(BAY73-4506)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Regorafenib monohydrate(BAY73-4506)图片
CAS NO:1019206-88-2
规格:≥98%
包装与价格:
包装价格(元)
10mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)500.83
FormulaC21H17ClF4N4O4
CAS No.1019206-88-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO:>100 mg/mL (200.9 mM)
Water: N/A
Ethanol: N/A
Solubility (In vivo)30% PEG400+0.5% Tween80+5% Propylene glycol: 30mg/mL
Chemical Name1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea monohydrate
SynonymBAY-734506 monohydratel; BAY 734506; BAY734506; Regorafenib HCl. Brand name: Stivarga.
SMILES CodeO=C(NC1=CC=C(C(C(F)(F)F)=C1)Cl)NC2=CC=C(OC3=CC(C(NC)=O)=NC=C3)C=C2F.O
实验参考方法
In VitroRegorafenib 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 VivoRegorafenib 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 modelFemale athymic NCr nu/nu mice with Colo-205, MDA-MB-231 or 786-O
Formulation & DosagePEG400/125 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.
生物活性

Regorafenib inhibits growth-factor-stimulated VEGFR2 and VEGFR3 autophosphorylation in human umbilical vascular endothelialcells (HuVECs) and intracellular signaling and migration in lymphatic endothelial cells (LECs).


Regorafenib inhibits key kinase targets in cells expressing VEGFR2, TIE2, PDGFR‐β, or FGFR. Int J Cancer. 2011 Jul 1;129(1):245-55.


Regorafenib inhibits tumor vasculature and tumor growth in a rat GS9L glioblastoma model: time‐course analysis by DCE‐MRI. Int J Cancer. 2011 Jul 1;129(1):245-55.


Regorafenib significantly reduces tumor MVA in the Colo‐205 CRC xenograft model. Int J Cancer. 2011 Jul 1;129(1):245-55.


Regorafenib exhibits antitumorigenic and antiangiogenic effects in the MDA‐MB‐231 breast xenograft model. Int J Cancer. 2011 Jul 1;129(1):245-55.



In vivo antitumor efficacy of regorafenib. Int J Cancer. 2011 Jul 1;129(1):245-55.