Regorafenib (BAY 73-4506)

For research use only. Not for use in humans.

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

Regorafenib (BAY 73-4506) Chemical Structure

CAS No. 755037-03-7

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。

规格

价格

库存

购买数量

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
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客户使用Selleck生产的Regorafenib (BAY 73-4506)发表文献145篇：

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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	NY\FPWNNSXCxcITvd4l{KEG\|c3H5	MVux5qCUPcLizszN	NIjo[4Q1QCCq		Mn\HbY5pcWKrdIOgZ4VtdCCpcn;3eIg>	M4S4[\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{K5OlA5Lz5{NkOyPVYxQDxxYU6=
PLC/PRF/5	NFLKW2FCeG:ydH;zbZMhSXO\|YYm=	NVHEZ5BPOeLCk{ZCpO69VQ>?	M1jwd\|Q5KGh?		M17FPIlvcGmkaYTzJINmdGxiZ4Lve5Rp	NGH4[Wo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkOyPVYxQCd-Mk[zNlk3ODh:L3G+
HepG2	NInvTWVCeG:ydH;zbZMhSXO\|YYm=	MnPYNgKBmzYEoN88US=>	NXryNXh4PDhiaB?=		NFTndJFqdmirYnn0d{Bk\WyuIHfyc5d1cA>?	M4PKbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{K5OlA5Lz5{NkOyPVYxQDxxYU6=
HEK293	Mmq2SpVv[3Srb36gRZN{[Xl?	MkmzNE426oDLzszN	M1;JbFIwPC94IHi=		MWTy[YR2[2W\|IFfSVFc5KGW6cILld5Nqd25?	MkPVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NUiwN\|IoRjJ3OEW4NFMzRC:jPh?=
GEO	MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXOxeWV6OC5yMT2yNEDPxE1?	MWi5OkBp	NXjPUIxwTE2VTx?=	MnzZbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	M1nubFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N\|kyLz5{NUizPFM6OTxxYU6=
SW48	NV7tbot2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NFr5TYExNjBzLUKwJO69VQ>?	NUjs[ldoQTZiaB?=	M1nxO2ROW09?	Mn7kbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	MmfsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6M{izPVEoRjJ3OEO4N\|kyRC:jPh?=
HT29	NF\6fnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWDLdHp6OC5yMT2yNEDPxE1?	NUDBdHJOQTZiaB?=	MkG3SG1UVw>?	MX\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	NW\zO\|lDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N\|g{QTFpPkK1PFM5OzlzPD;hQi=>
SW480	NH:4RoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHLPUGQxNjBzLUKwJO69VQ>?	MoDaPVYhcA>?	M3nqO2ROW09?	MUXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	M{LDSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N\|kyLz5{NUizPFM6OTxxYU6=
SW620	MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M2DTTlAvODFvMkCg{txO	M2DHNFk3KGh?	NHLSeXdFVVOR	NW\UdppvcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	M{[5WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N\|kyLz5{NUizPFM6OTxxYU6=
HCT116	NIiydWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NV\FPXZ7OC5yMT2yNEDPxE1?	MVS5OkBp	MVrEUXNQ	NWLQU3h7cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	NGG0R5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizPFM6OSd-MkW4N\|g{QTF:L3G+
LOVO	M{nmbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlfmNE4xOS1{MDFOwG0>	M1TaR\|k3KGh?	NEPwbopFVVOR	MWfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	NXTnWYhJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N\|g{QTFpPkK1PFM5OzlzPD;hQi=>
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BA/F3	M2XXfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MYi3NkBpenN?		NYrQfJl4UW6qaXLpeIlwdiCxZjDLbZQhTDhzNm[gcZV1[W62IDj1cotvd3ewIH;ybYdqdilidILhcpNn\WO2ZXSgbY4hdW:3c3WgRmEwTjNiY3XscJMh[XO\|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIHfyc5d1cCCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBOXFNiYYPzZZktKEeLNUCgQUAzNjN5MTFOwG0v	M2nie\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5\|MEKwOFQ1OTxxYU6=
GIST430	M1P6d2N6fG:2b4jpZ4l1gSCjc4PhfS=>		M3[5T\|czKGi{cx?=		MofhR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gS2lUXDR\|MDDj[YxteyCqYYLic5JqdmdiS1nUJHY3PTSDIH31eIFvfCCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBE\WyuVHn0[ZJIdG9iYYPzZZktKEeLNUCgQUA{KM7:TT6=	NVT5O4FnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5PVE1PjVpPkK4PVkyPDZ3PD;hQi=>
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U-2 OS	MWDxTHRUKGG\|c3H5				NEW3[lZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiVT2yJG9UKGOnbHzz	Mlq2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
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Saos-2	NIn5Vo9yUFSVIHHzd4F6				NVnMdpZbeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPhc5MuOiClZXzsdy=>	NFvJWYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
BT-37	MmLzdWhVWyCjc4PhfS=>				M1LKNpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?=	NXi1V4pMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD	M3\JS5FJXFNiYYPzZZk>				NWTrS4E1eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGLEJINmdGy\|	M3nt[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-12	NG\VZ\|lyUFSVIHHzd4F6				NVK3SXg3eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz	MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
MG 63 (6-TG R)	M4S5e5FJXFNiYYPzZZk>				MWTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN?	NIPZ[nY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
NB1643	NYX2WlVOeUiWUzDhd5NigQ>?				MW\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy\|	NY\xOXB5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50	MkS3dWhVWyCjc4PhfS=>				M2fDOpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO=	NYn3[pdRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2	Mm\VdWhVWyCjc4PhfS=>				NULRRZNIeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM>	M2mxOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC	M4LkbJFJXFNiYYPzZZk>				MnfZdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO=	NXPz[YZVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB-EBc1	MlXDdWhVWyCjc4PhfS=>				M{jN[JFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
LAN-5	M2jWZ5FJXFNiYYPzZZk>				M1vUSJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?=	NYS0U2UyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18	M1vMXJFJXFNiYYPzZZk>				MmP4dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN?	NX;vSoMzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	PUMA / p53; PubMed: 24763611 Clin Cancer Res WT and p53-KO HCT116 cells were treated with 40 μmol/L regorafenib for 24 hours. PUMA expression was analyzed by Western blotting. Bim / Bid / Bak / Bcl-Xl / Mcl-1; PubMed: 24763611 Clin Cancer Res The expression of indicated Bcl-2 family members was analyzed by Western blotting in HCT116 cells treated with 40 μmol/L regorafenib at indicated time points. p-p65(S536) / p65; PubMed: 24763611 Clin Cancer Res HCT116 cells were treated with 40 μmol/L regorafenib. Expression of p-p65 (S536) and β-actin at indicated time points was analyzed by Western blotting. p-FGFR2 / p-FRS2α / p-AKT / p-MAPK / p-P90RSK / FGFR2 / AKT / MAPK / p90RSK; PubMed: 29573334 Mol Oncol Changes in FGFR2 signaling molecules after regorafenib treatment. Immunoblotting assays were performed after treatment with increasing concentrations of regorafenib for 24 h. Cyclin D / Cyclin E / Cyclin A / Cyclin B / p27 / p21; PubMed: 29573334 Mol Oncol Changes in cell cycle and/or apoptosis‐related molecules. p-STAT3 / STAT3 / PARP / Caspase-9; PubMed: 25071018 Oncotarget p-STAT3(Tyr705), STAT3, the cleaved fragments of PARP and the cleaved fragments of caspase-9 were measured by western blotting at the times indicated after Hct-15 and DLD1 cells were treated with regorafenib at 5 μM. β-actin was used as a loading control. The cleaved fragments of PARP and the cleaved fragments of caspase-9 were indicated by arrows.	24763611 29573334 25071018
Immunofluorescence	p65; PubMed: 24763611 Clin Cancer Res HCT116 cells were treated with 40 μmol/L regorafenib for 3 hours and then fixed. Immunofluorescence was carried out as described in the Materials and Methods for p65 (green) and DAPI (blue). Representative pictures (400×) are shown. Arrows indicate cells with p65 nuclear translocation. F-actin / Vimentin / E-cadherin ; PubMed: 27580057 Oncotarget Immunofluorescence microscopy analysis of rhodamine phalloidin-stained F-actin, DAPI-stained nuclei, vimentin and E-cadherin in the cells.	24763611 27580057
Growth inhibition assay	GI50; PubMed: 29573334 Mol Oncol Screening of in vitro sensitivity to regorafenib in 14 gastric and 10 colorectal cancer cell lines. MTT cell proliferation assays were performed with increasing concentrations of regorafenib for 72 h. GI 50 values were averaged from at least three independent experiments in hexaplicate. Cell viability; PubMed: 25071018 Oncotarget MTT assay was performed to measure the cell viability in the colon cancer cell lines 2 days after treatment with regorafenib in a dose-dependent manner.	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]	- 合并激酶活性测定: 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]	- 合并 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。 (Only for Reference)
动物实验：^[1]	- 合并 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 (Only for Reference)

参考文献

溶解度 (25°C)

体外	DMSO	97 mg/mL (200.9 mM)
	Water	Insoluble
	Ethanol	Insoluble
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	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 Download Regorafenib (BAY 73-4506) SDF

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

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

每只动物给药体积

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

计算重置

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。

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。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-09-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
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	--
NCT04476329	Recruiting	Drug: Regorafenib 40 MG	Hepatocellular Carcinoma	SC Liver Research Consortium LLC\|Bayer	January 21 2021	Phase 2
NCT04200404	Recruiting	Drug: CS1001\|Drug: Regorafenib	Advanced Refractory Solid Tumors	CStone Pharmaceuticals\|Bayer	December 13 2019	Phase 1\|Phase 2

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

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.

VEGFR Signaling Pathway Map

VEGFR Inhibitors with Unique Features

选择性强的VEGFR抑制剂

Vandetanib (ZD6474) : VEGFR2-selective, IC50=40 nM.
活性最高的VEGFR抑制剂

Cabozantinib (XL184, BMS-907351) : VEGFR2, IC50=0.035 nM.
FDA批准的VEGFR抑制剂

Axitinib : Approved by FDA for Renal Cell Carcinoma.
经典的VEGFR抑制剂

Nintedanib (BIBF 1120) : Potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM. Phase 3.

研究领域

产品类型

定制您的化合物库

Regorafenib (BAY 73-4506)

客户使用Selleck生产的Regorafenib (BAY 73-4506)发表文献145篇：

产品安全说明书

VEGFR抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Regorafenib (BAY 73-4506) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-09-06)

技术支持

常见问题及建议解决方法

VEGFR Signaling Pathway Map

VEGFR Inhibitors with Unique Features

相关VEGFR产品