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Regorafenib (BAY 73-4506)

目录号：S1178 别名: Fluoro-Sorafenib, Resihance, Stivarga

仅限科研使用

Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) 是一个多靶点抑制剂，作用于VEGFR1，VEGFR2，VEGFR3，PDGFR-β，Kit (c-Kit)，RET (c-RET)和Raf-1，在无细胞试验中IC50分别是13 nM，4.2 nM，46 nM，22 nM，7 nM，1.5 nM和2.5 nM。Regorafenib 可诱导自噬。

Regorafenib (BAY 73-4506) Chemical Structure

CAS: 755037-03-7

规格	价格	库存
10mM (1mL in DMSO)	RMB 1375.55	现货
5mg	RMB 972.87	现货
25mg	RMB 3830.98	现货
100mg	RMB 7954.71	现货
大包装	有超大折扣

今日订购，明日送达全国免运费分装免费分装成小规格产品（单支最小为1mg）如1支10mg产品可分装为10支1mg产品全国免费电话：400-668-6834 \| Email：info@selleck.cn

客户使用Selleck生产的Regorafenib (BAY 73-4506)发表文献165篇：

产品安全说明书

VEGFR抑制剂选择性比较

生物活性

产品描述

特性

Regorafenib是一个新的口服多激酶抑制剂。

靶点

RET ^[1] (Cell-free assay)	Raf-1 ^[1] (Cell-free assay)	VEGFR2 ^[1] (Cell-free assay)	Kit ^[1] (Cell-free assay)	VEGFR1 ^[1] (Cell-free assay)	点击更多
1.5 nM	2.5 nM	4.2 nM	7 nM	13 nM	点击更多

体外研究

在 NIH-3T3细胞中 Regorafenib 强烈抑制 VEGFR2的自磷酸化， IC50 为3 nM. 在HAoSMCs中, Regorafenib 抑制 PDGFR-β经过PDGF-BB刺激后的自磷酸化, IC50 为90 nM. 在MCF-7 乳腺癌细胞中， Regorafenib 也会抑制FGF10刺激后 FGFR 的信号传导. Regorafenib 非常有效的抑制KIT^K642E 和 RET^C634W这两个突变的受体, IC50 分别是大约 20 nM 和 10 nM。 Regorafenib 抑制经过VEGF¹⁶⁵ 刺激后的 HUVECs细胞的增值, IC50 为大约 3 nM. Regorafenib抑制 FGF2刺激后的 HUVECs和PDGF-BB刺激后的HAoSMCs细胞的增殖， IC50分别是127 nM 和 146 nM ^[1]。 Regorafenib通过抑制酪氨酸激酶受体(VEGFR, KIT, RET, FGFR和 PDGFR)和丝氨酸/ 苏氨酸激酶受体(RAF 和 p38MAPK)来靶向作用于肿瘤细胞增殖和肿瘤脉管系统^[2]。Regorafenib以浓度依赖和时间依赖方式抑制人Hep3B, PLC/PRF/5 和 HepG2 细胞的生长^[3]。

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

Hep3B	M1y5[GFxd3C2b4Ppd{BCe3OjeR?=	M1m5bFHjiJN3wrFOwG0>	M1zXZlQ5KGh?		NWrnfHBOcW6qaXLpeJMh[2WubDDndo94fGh?	M2X3eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{K5OlA5Lz5{NkOyPVYxQDxxYU6=
PLC/PRF/5	NWL3UHluSXCxcITvd4l{KEG\|c3H5	NVy4RoNmOeLCk{ZCpO69VQ>?	MoWyOFghcA>?		NVjjdmlJcW6qaXLpeJMh[2WubDDndo94fGh?	M1HNe\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{K5OlA5Lz5{NkOyPVYxQDxxYU6=
HepG2	NFPKV3NCeG:ydH;zbZMhSXO\|YYm=	NHvTTlQy6oDVNdMg{txO	NVf6eIplPDhiaB?=		MnrQbY5pcWKrdIOgZ4VtdCCpcn;3eIg>	MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN{OU[wPEc,OjZ\|Mkm2NFg9N2F-
HEK293	MU\GeY5kfGmxbjDBd5NigQ>?	Mo\BNE426oDLzszN	NVfoNlF2Oi92L{[gbC=>		MX\y[YR2[2W\|IFfSVFc5KGW6cILld5Nqd25?	M3fRdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEW4NFMzLz5{NUi1PFA{OjxxYU6=
GEO	Mn:3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Ml:wNE4xOS1{MDFOwG0>	Mn3tPVYhcA>?	MmHxSG1UVw>?	M17XTYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	M4TGTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N\|kyLz5{NUizPFM6OTxxYU6=
SW48	MknHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NWqzNFNoOC5yMT2yNEDPxE1?	NGHNR206PiCq	M4eyNWROW09?	NYraZoNKcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	NVq2cZFJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N\|g{QTFpPkK1PFM5OzlzPD;hQi=>
HT29	NF7rRY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXLpcnczOC5yMT2yNEDPxE1?	MnrsPVYhcA>?	MmDCSG1UVw>?	NV7UNYRucW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	NULJR\|lzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N\|g{QTFpPkK1PFM5OzlzPD;hQi=>
SW480	Mn;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mle1NE4xOS1{MDFOwG0>	NVOwTHdDQTZiaB?=	Mnn1SG1UVw>?	NYj4U5ZMcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	M2joVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N\|kyLz5{NUizPFM6OTxxYU6=
SW620	NIT6Z2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MoT1NE4xOS1{MDFOwG0>	MXq5OkBp	MonGSG1UVw>?	M1nGR4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	NWjIc5o3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N\|g{QTFpPkK1PFM5OzlzPD;hQi=>
HCT116	MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M{HWclAvODFvMkCg{txO	NFPwU\|k6PiCq	MVHEUXNQ	NFi0WHhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh\|OEO5NUc,OjV6M{izPVE9N2F-
LOVO	NH\YZlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Mo\xNE4xOS1{MDFOwG0>	MlP0PVYhcA>?	MYjEUXNQ	M1zwVolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	M4HuTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N\|kyLz5{NUizPFM6OTxxYU6=
HCT150	NXLK[mtPT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MoixNE4xOS1{MDFOwG0>	MnjqPVYhcA>?	NX3SWJlDTE2VTx?=	NFTVUItqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	M1m0U\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N\|kyLz5{NUizPFM6OTxxYU6=
SW48-CR	NY\MdZRWT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Ml[5NE4xOS1{MDFOwG0>	NED6cYk6PiCq	NGnr[49FVVOR	M4jk[YlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	NVmxR5lNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N\|g{QTFpPkK1PFM5OzlzPD;hQi=>
GEO-CR	MorLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NH;FU3AxNjBzLUKwJO69VQ>?	MVm5OkBp	MVHEUXNQ	M3LX[YlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	M{Hke\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N\|kyLz5{NUizPFM6OTxxYU6=
KB-31	MmS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MlX4TWM2OD13LkZCtVAvOyCwTR?=	NEHKd\|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe1N\|M3OSd-MkW3OVM{PjF:L3G+
KB-G2	NWPvXGNIT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MVXJR\|UxRTlwMdMxNE4yKG6P	MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd3M{O2NUc,OjV5NUOzOlE9N2F-
LLC-PK1	NV7G[242T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NYnVdm1CUUN3ME20Nk4xyrF\|LkKgcm0>	MmDUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NUOzOlEoRjJ3N{WzN\|YyRC:jPh?=
LLC-PK1/MRP2	M3r5[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NGTrRWtKSzVyPUiyMlTDuTJwNzDuUS=>	NF3GVnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe1N\|M3OSd-MkW3OVM{PjF:L3G+
HEK293	NH3IZ5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M33oXmlEPTB;MUGuNOKyOS5{IH7N	NFPpeHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe1N\|M3OSd-MkW3OVM{PjF:L3G+
HEK293/OATP1B1	MlOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M1H1PWlEPTB;Nj6yxtExNjNibl2=	NHjRW\|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe1N\|M3OSd-MkW3OVM{PjF:L3G+
HROC18	NWC4fJZET3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				Mmq1TWM2OD1zLkOg{txO	MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyOUmxOEc,OjV\|MEm5NVQ9N2F-
HROC24	M4HnTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NV7JXoQ2UUN3ME20MlYh\|ryP	MoXqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV\|MEm5NVQoRjJ3M{C5PVE1RC:jPh?=
HROC43	MkC4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NVmyUpdzUUN3ME21MlMh\|ryP	NF;lZXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwPVkyPCd-MkWzNFk6OTR:L3G+
HROC46	NVLrb41mT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NYDU[JRrUUN3ME2yMlQh\|ryP	NEHWdIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwPVkyPCd-MkWzNFk6OTR:L3G+
RJ345	M1jNTGZ2dmO2aX;uJGF{e2G7	NEL4enoxNjVxNTFOwG0>	NYTZV4tpOjRiaB?=	MoK4SG1UVw>?	M{T5cYlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=>	NGHmeW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK1N\|k6PCd-MkWyOVM6QTR:L3G+
RJ348	NHTBOWdHfW6ldHnvckBCe3OjeR?=	NFLk[mwxNjVxNTFOwG0>	Mle5NlQhcA>?	NWDjeY1xTE2VTx?=	NYjGd\|BMcW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v	NUT1e4tSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOVM6QTRpPkK1NlU{QTl2PD;hQi=>
MCF-7	NE\hcYhHfW6ldHnvckBCe3OjeR?=	MYGwMlUwPSEQvF2=	NX61OFN[OjRiaB?=	NFTrNWtFVVOR	M{eyWYlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=>	NYrOT\|V5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOVM6QTRpPkK1NlU{QTl2PD;hQi=>
MDA-MB-231	MVfGeY5kfGmxbjDBd5NigQ>?	NIC2XWYxNjVxNTFOwG0>	NYDCNotkOjRiaB?=	M1zzcGROW09?	NHXuO2hqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44>	M3zFeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkWzPVk1Lz5{NUK1N\|k6PDxxYU6=
HT15	NXX4SJZyT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	Mo\qNU0zOCEQvF2=	NXTHR3c1PDhiaB?=		MYXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	NUDrTphwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwO\|ExOThpPkK1NFcyODF6PD;hQi=>
DLD1	M2r5fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MmPXNU0zOCEQvF2=	MWO0PEBp		NHrz[ZpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB5MUCxPEc,OjVyN{GwNVg9N2F-
HT-29	NY\4WIlsT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MkK2NU0zOCEQvF2=	NYjkRlVoPDhiaB?=		M2CwPIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	MX68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB5MUCxPEc,OjVyN{GwNVg9N2F-
Hct-116	NXPkflBnT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M{KxelEuOjBizszN	NGTpbZY1QCCq		NFfHPYtqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	M{PwW\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEexNFE5Lz5{NUC3NVAyQDxxYU6=
HT15	M2jVXWFxd3C2b4Ppd{BCe3OjeR?=	MV:xMVExKM7:TR?=	M{\0S\|Q5KGh?		M3fYXolv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	NXnoZmZIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwO\|ExOThpPkK1NFcyODF6PD;hQi=>
DLD1	M1HydWFxd3C2b4Ppd{BCe3OjeR?=	NIPp[3cyNTFyIN88US=>	M{jXeFQ5KGh?		MXHpcoR2[2W\|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=	MlHRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyN{GwNVgoRjJ3MEexNFE5RC:jPh?=
HT-29	Ml3vRZBweHSxc3nzJGF{e2G7	NYjUbYI{OS1zMDFOwG0>	NHLUXoQ1QCCq		MV7pcoR2[2W\|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=	M1PuWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEexNFE5Lz5{NUC3NVAyQDxxYU6=
Hct-116	NEOx[4NCeG:ydH;zbZMhSXO\|YYm=	NIC0fpgyNTFyIN88US=>	MUG0PEBp		MXPpcoR2[2W\|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=	M3nTZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEexNFE5Lz5{NUC3NVAyQDxxYU6=
GBM5	NFzoU29CeG:ydH;zbZMhSXO\|YYm=	NYf0W2w2OC534pETNU4x6oDLzszN	MljENlQhcA>?	MX3EUXNQ	M4DiXIlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=>	MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlzMUKxOUc,OjR7MUGyNVU9N2F-
GBM6	MlPLRZBweHSxc3nzJGF{e2G7	MkXiNE426oDVMT6w5qCK\|ryP	NUC3e2RTOjRiaB?=	M3L3eWROW09?	M{nGcIlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=>	M1vCcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUGxNlE2Lz5{NEmxNVIyPTxxYU6=
GBM12	NWSxbIQ4SXCxcITvd4l{KEG\|c3H5	NF7rTIsxNjYkgKOxMlDjiIoQvF2=	Mn\nNlQhcA>?	NFjNRoZFVVOR	NYHFTGl4cW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp	M{\oNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUGxNlE2Lz5{NEmxNVIyPTxxYU6=
GBM14	NUXLfJNsSXCxcITvd4l{KEG\|c3H5	NXzhb4dIOC534pETNU4x6oDLzszN	NH;rS\|kzPCCq	M1rnUWROW09?	M3L0TYlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=>	NEG1UWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxNVIyPSd-MkS5NVEzOTV:L3G+
Hep3B	NUDJUVl7T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NUC3V2tCOeLCk{KuOeKh\|ryP	NWL6RoZOOjRxNEivO\|IhcA>?		MUfpcohq[mm2czDj[YxtKGe{b4f0bC=>	NVzURXU6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFU5QTBpPkK0PFg2QDlyPD;hQi=>
PLC/PRF/5	M2L3SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MnrpNgKBmzJwNdMg{txO	MoG3NlQwPDhxN{KgbC=>		NHfLU5dqdmirYnn0d{Bk\WyuIHfyc5d1cA>?	NV\wVVlRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFU5QTBpPkK0PFg2QDlyPD;hQi=>
HepG2	MoTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NIDUNncy6oDVMj61xsDPxE1?	NXrGcXE5OjRxNEivO\|IhcA>?		NHK0fIlqdmirYnn0d{Bk\WyuIHfyc5d1cA>?	M{fTWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi1PFkxLz5{NEi4OVg6ODxxYU6=
HCT116	M3XlVmZ2dmO2aX;uJGF{e2G7	Mn3sNVAwOjBxNECg{txO	NV\aOJYzOjRiaB?=		NW\yVlVTcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJI1TVkFiZYjwdoV{e2mxbjDpckBiKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK=	NEnWUoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe2N\|YyOSd-MkS3OlM3OTF:L3G+
Lim2405	NUmyRYVuTnWwY4Tpc44hSXO\|YYm=	M2fhNVQxKM7:TR?=	NWTXcYd[OjRiaB?=		MVLpcoR2[2W\|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM>	NXe1epRbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3OlM3OTFpPkK0O\|Y{PjFzPD;hQi=>
LoVo	M1zQNmZ2dmO2aX;uJGF{e2G7	NUPnfoJEPDBizszN	NWTlXHBoOjRiaB?=		NXPYNYY{cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m\|	MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd4M{[xNUc,OjR5NkO2NVE9N2F-
Lim1215	MXvGeY5kfGmxbjDBd5NigQ>?	NF6yRoc1OCEQvF2=	NFT2Z4gzPCCq		MoDVbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{	MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd4M{[xNUc,OjR5NkO2NVE9N2F-
SW48	Mn;zSpVv[3Srb36gRZN{[Xl?	MljWOFAh\|ryP	NWTiV4hNOjRiaB?=		MV3pcoR2[2W\|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM>	NUPH[ZdXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3OlM3OTFpPkK0O\|Y{PjFzPD;hQi=>
RKO	NUX0TGZNTnWwY4Tpc44hSXO\|YYm=	MUi0NEDPxE1?	MnXoNlQhcA>?		NELqU5FqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN?	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd4M{[xNUc,OjR5NkO2NVE9N2F-
SW837	MV7GeY5kfGmxbjDBd5NigQ>?	MUK0NEDPxE1?	NV\3R\|dFOjRiaB?=		NIHp[FBqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN?	NWL0O3RQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3OlM3OTFpPkK0O\|Y{PjFzPD;hQi=>
SW1463	NVHXZ20zTnWwY4Tpc44hSXO\|YYm=	M2DyWlQxKM7:TR?=	MYiyOEBp		NX;BSlhScW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m\|	NYXkfGFYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3OlM3OTFpPkK0O\|Y{PjFzPD;hQi=>
SW480	MWTGeY5kfGmxbjDBd5NigQ>?	NXvxNZdSPDBizszN	MXGyOEBp		NVTLUW5OcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m\|	NEfZW5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe2N\|YyOSd-MkS3OlM3OTF:L3G+
Vaco432	NUfZdVhtTnWwY4Tpc44hSXO\|YYm=	NUDHUZpOPDBizszN	NEfCT5AzPCCq		NEe1e\|BqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN?	NGrVWJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe2N\|YyOSd-MkS3OlM3OTF:L3G+
Vaco400	NW\UdHlyTnWwY4Tpc44hSXO\|YYm=	NY\XcG9NPDBizszN	MVSyOEBp		NVfYbmc{cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m\|	M1X0OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{[zOlEyLz5{NEe2N\|YyOTxxYU6=
DLD1	MULGeY5kfGmxbjDBd5NigQ>?	MWC0NEDPxE1?	MWWyOEBp		NEHJZW9qdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN?	NGHqSok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe2N\|YyOSd-MkS3OlM3OTF:L3G+
HT29	M3jMcGZ2dmO2aX;uJGF{e2G7	Mn;LOFAh\|ryP	M2qxUlI1KGh?		NYrFeml{cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m\|	NW\wWVVIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3OlM3OTFpPkK0O\|Y{PjFzPD;hQi=>
PLC/PRF/5	MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3LZflHjiJN3wsXN	M3PQd\|I1NzR6L{eyJIg>		NVPYSXhtcW6qaXLpeJMh[2WubDDndo94fGh?	MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzF4OUG0PEc,OjNzNkmxOFg9N2F-
HepG2	NEXhT41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MUmx5qCUPcL3TR?=	NXW4foV4OjRxNEivO\|IhcA>?		M3vz[YlvcGmkaYTzJINmdGxiZ4Lve5Rp	NHvUOWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{G2PVE1QCd-MkOxOlkyPDh:L3G+
Hep3B	MlLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVKx5qCUPcL3TR?=	M4LHV\|I1NzR6L{eyJIg>		NVexTnZHcW6qaXLpeJMh[2WubDDndo94fGh?	MmD1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNzNkmxOFgoRjJ\|MU[5NVQ5RC:jPh?=
BA/F3	M2fzb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7		Ml;LO\|IhcHK\|		NUPmNVdSUW6qaXLpeIlwdiCxZjDLbZQh\XixbjCxNUBl\WyndHnvckApPTV5IITvJFU2QCC{ZYPp[JVmeylibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkhfHKjboPm[YN1\WRiaX6gcY92e2ViQlGvSlMh[2WubIOgZZN{\XO\|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKGe{b4f0bEBqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO\|YYmsJGdKPTBiPTCwMlAzOSEQvF2u	NH7z[Yg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
BA/F3	M1nsemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NXH4doYzPzJiaILz		M3XJfmlvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIGDES2ZT[mW2YTCoeY5sdm:5bjDvdolocW5rIITyZY5{\mWldHXkJIlvKG2xdYPlJGJCN0Z\|IHPlcIx{KGG\|c3Xzd4VlKGG\|IHnubIljcXSrb36gc4Yh[2WubDDndo94fGhiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwJF0hOC5yMkmg{txONg>?	MkDrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
BA/F3	NFrCXYdIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MWi3NkBpenN?		M1;Ie2lvcGmkaYTpc44hd2ZiS3n0JIV5d25iMUGg[IVt\XSrb36gLFU2PyC2bzC1OVghemW\|aXT1[ZMqKGGwZDDEPFE3UCCvdYThcpQh[W6mIGS2O\|BKKG23dHHueEApfW6tbn;3ckBwemmpaX6pJJRz[W6\|ZnXjeIVlKGmwIH3veZNmKEKDL1[zJINmdGy\|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxKD1iMD6wN\|Mh\|ryPLh?=	MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
BA/F3	NITUZ21Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NHnhVW04OiCqcoO=		NIPv[lJKdmirYnn0bY9vKG:oIFvpeEBmgG:wIEGxJIRmdGW2aX;uJEg2PTdidH:gOVU5KHKnc3nkeYV{MSCjbnSgRVgzQVBibYX0ZY51KGGwZDDZPFI{TCCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUB1emGwc3\lZ5Rm\CCrbjDtc5V{\SCEQT;GN{Bk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIHPlcIwh\3Kxd4ToJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IF3UV{Bie3OjeTygS2k2OCB;IECuNFQ4KM7:TT6=	NYWycph[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
BA/F3	M3zyfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MUS3NkBpenN?		M1LuVGlvcGmkaYTpc44hd2ZiS3n0JIV5d25iMUGg[IVt\XSrb36gLFU2PyC2bzC1OVghemW\|aXT1[ZMqKGGwZDDOPFIzUyCvdYThcpQh[W6mIGm4NlNFKG23dHHueEApfW6tbn;3ckBwemmpaX6pJJRz[W6\|ZnXjeIVlKGmwIH3veZNmKEKDL1[zJINmdGy\|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxKD1iMD6wOFkh\|ryPLh?=	MonmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
BA/F3	MoO1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MnizO\|IhcHK\|		NXG3RmU3UW6qaXLpeIlwdiCxZjDUSWwu\nW\|ZXSgVGRITlKjbIDoZUApfW6tbn;3ckBwemmpaX6pJJRz[W6\|ZnXjeIVlKGmwIH3veZNmKEKDL1[zJINmdGy\|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxKD1iMD6wOVEh\|ryPLh?=	Mn;ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
BA/F3	NFPnTHZIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M17rTFczKGi{cx?=		M3iwe2lvcGmkaYTpc44hd2ZiS3n0JIV5d25iMUGg[IVt\XSrb36gLFU2PyC2bzC1OVghemW\|aXT1[ZMqKGGwZDDEPFIxSSCvdYThcpQh[W6mIFS4NlBCKG23dHHueEApfW6tbn;3ckBwemmpaX6pJJRz[W6\|ZnXjeIVlKGmwIH3veZNmKEKDL1[zJINmdGy\|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxKD1iMD6wOlMh\|ryPLh?=	M4KyU\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5\|MEKwOFQ1OTxxYU6=
BA/F3	M{HZWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NVLkNYM3PzJiaILz		NV[5Ono3UW6qaXLpeIlwdiCxZjDLbZQh\XixbjCxNUBl\WyndHnvckApPTV5IITvJFU2QCC{ZYPp[JVmeyliYX7kJHk5OjOGIH31eIFvfCBqdX7rco94diCxcnnnbY4qKHS{YX7z[oVkfGWmIHnuJI1wfXOnIFLBM2Y{KGOnbHzzJIF{e2W\|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCpcn;3eIghcW6ldXLheIVlKG[xcjC3NkBpenNiYomgUXRUKGG\|c3H5MEBIUTVyIE2gNE4xQTRizszNMi=>	NFfxNpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
BA/F3	NYnOU2ZzT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NG[5OnY4OiCqcoO=		M1nmNmlvcGmkaYTpc44hd2ZiS3n0JHY2PjCGIH31eIFvfCBqdX7rco94diCxcnnnbY4qKHS{YX7z[oVkfGWmIHnuJI1wfXOnIFLBM2Y{KGOnbHzzJIF{e2W\|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCpcn;3eIghcW6ldXLheIVlKG[xcjC3NkBpenNiYomgUXRUKGG\|c3H5MEBIUTVyIE2gNE4yODhizszNMi=>	M4njRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5\|MEKwOFQ1OTxxYU6=
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LAN-5	MXzxTHRUKGG\|c3H5				M4TGbZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?=	Mn3TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
Rh18	NEPIWGdyUFSVIHHzd4F6				M2D5bZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEG4JINmdGy\|	M3jXflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot	PUMA / p53 Bim / Bid / Bak / Bcl-Xl / Mcl-1 p-p65(S536) / p65 p-FGFR2 / p-FRS2α / p-AKT / p-MAPK / p-P90RSK / FGFR2 / AKT / MAPK / p90RSK Cyclin D / Cyclin E / Cyclin A / Cyclin B / p27 / p21 p-STAT3 / STAT3 / PARP / Caspase-9	24763611 29573334 25071018
Immunofluorescence	p65 F-actin / Vimentin / E-cadherin	24763611 27580057
Growth inhibition assay	GI50 Cell viability	29573334 25071018

体内研究

在多种临床前人类异种移植的小鼠模型上， Regorafenib有着很好的肿瘤生长抑制性，这种抑制具有剂量依赖特性, 表现为在乳腺 MDA-MB-231 和肾脏 786-O 肿瘤模型中肿瘤减小. Regorafenib 不仅阻止了同源主要的 4T1乳腺肿瘤在脂肪垫中的原位生长，也抑制了肿瘤转移到肺部^[1]。

激酶实验： ^[1]	激酶活性测定: 体外激酶实验用重组的VEGFR2 (鼠源， aa785–aa1367), VEGFR3 (鼠源 aa818–aa1363), PDGFR-β (aa561–aa1106), RAF-1 (aa305–aa648) 和 BRAFV600E (aa409–aa765)的激酶活性区域进行。初始的激酶抑制反应将Regorafenib的浓度固定为1 μM. IC50的值根据选定的相应的激酶来测定, 如VEGFR1 和 RET. TIE2 的激酶抑制效果采用均相时间分辨荧光分析法测定，利用重组的TIE2细胞内区域的GST融合蛋白和生物素化的-Ahx-EPKDDAYPLYSDFG多肽作为底物。
细胞实验： ^[1]	Cell lines: GIST 882 和 TT 细胞 Concentrations: 5 nM-10 μM Incubation Time: 96 小时 Method: 为了分析细胞增殖情况, 将GIST 882 和 TT 细胞培养在含有L-glutamine谷氨酸的RPMI 培养基中,MDA-MB-231, HepG2和A375 细胞培养在含有10% hiFBS 的 DMEM 培养基中。将细胞用胰酶消化, 按5× 10⁴ 个每孔接种在96孔板中并在含有10% FBS 的完全培养基中37°C培养过夜。第二天, 将对照和Regorafenib用培养基稀释成从10 μM 到5 nM的连续终浓度, 加入 0.2% DMSO,加入细胞培养基中并继续培养96小时。将细胞增殖情况进行量化。
动物实验： ^[1]	Animal Models: 携带Colo-205, MDA-MB-231 细胞或者 786-O肿瘤的雌性无胸腺NCr nu/nu 小鼠 Dosages: 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg Administration: 口服

参考文献	[1] Wilhelm SM, et al. Int J Cancer, 2011, 129(1), 245-255. [2] Heng DY, et al. Ther Adv Med Oncol, 2010, 2(1), 39-49. [3] Carr BI, et al. J Cell Physiol, 2013, 228(2), 292-297.

溶解度（25°C）

体外


体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 点击购买： PEG300 Tween 80	5mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量	482.82
化学式	C₂₁H₁₅ClF₄N₄O₃
CAS号	755037-03-7
储存条件	3年	-20°C	粉状
储存条件	2年	-80°C	溶于溶剂

Download Regorafenib (BAY 73-4506) SDF

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

临床试验信息

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05370807	Not yet recruiting	Drug: Regorafenib 40 MG Oral Tablet	Melanoma Stage III\|Melanoma Stage IV	Universitair Ziekenhuis Brussel	May 2022	Phase 2
NCT05289726	Not yet recruiting	Drug: Traditional chinese medicine TDX105\|Drug: Placebo	Hand and Foot Skin Reaction\|Colorectal Cancer Stage IV	Cancer Institute and Hospital Chinese Academy of Medical Sciences	April 18 2022	Phase 2
NCT05023720	Recruiting	Other: nonintervention	Metastatic Colorectal Cancer	Henan Cancer Hospital	July 20 2021	--
NCT04920422	Active not recruiting	Other: No intervention	Metastatic Colorectal Cancer	Bayer	July 15 2021	--
NCT05024539	Recruiting	Other: nonintervention	Hepatocellular Carcinoma	Shujun Yang\|Henan Cancer Hospital	June 20 2021	--

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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常见问题及建议解决方法

问题 1:
How to resuspend Regorafenib for in vivo studies?

回答：
For in vivo study, we recommend to use 2% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 5mg/ml.

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