| CAS NO: | 1019206-88-2 |
| 规格: | ≥98% |
| 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 |
| Molecular Weight (MW) | 500.83 |
|---|---|
| Formula | C21H17ClF4N4O4 |
| 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 Name | 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea monohydrate |
| Synonym | BAY-734506 monohydratel; BAY 734506; BAY734506; Regorafenib HCl. Brand name: Stivarga. |
| SMILES Code | O=C(NC1=CC=C(C(C(F)(F)F)=C1)Cl)NC2=CC=C(OC3=CC(C(NC)=O)=NC=C3)C=C2F.O |
| In Vitro | 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. |
 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. |
m.cnreagent.com
