Regorafenib HCl(BAY-73-4506)

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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。

CAS NO:	835621-07-3
规格:	≥98%

包装与价格：

包装	价格(元)
5mg	电议
50mg	电议
100mg	电议
250mg	电议
500mg	电议
1g	电议

产品介绍

Regorafenib HCl, the hydrochloric acid salt of regorafenib (also known as BAY 73-4506), is a potent inhibitor of multi-kinase including VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 values of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. It is an orally bioavailable small molecule that has anticancer activity and has been approved by FDA for the treatment of liver cancer. Regorafenib strongly prevents VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs, regorafenib suppress PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. It also inhibits FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10.

理化性质和储存条件

Molecular Weight (MW)	519.28
Formula	C21H16Cl2F4N4O3
CAS No.	835621-07-3(HCI)
Storage	-20℃ for 3 years in powder form
Storage	-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 hydrochloric acid
Synonym	BAY-734506 HCl; 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

实验参考方法

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.

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.