Regorafenib (BAY 73-4506)

For research use only. Not for use in humans.

製品コードS1178 別名：Fluoro-Sorafenib, Resihance, Stivarga

CAS No. 755037-03-7

Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy.

サイズ

価格(税別)

10mM (1mL in DMSO)	JPY 29800
5mg	JPY 21900
25mg	JPY 80000
100mg	JPY 163000

最寄りの販売代理店を探す

東京
北海道
東北
北関東
南関東
東海
北信越
近畿
中国
四国
九州

お探しのディーラーが見当たらない場合は直接こちらのメールアドレスまでお問い合わせください：[email protected]

バルク問合せ

代表番号: 03-5615-9297|電子メール：[email protected]|よく尋ねられる質問

文献中Selleckの製品使用例(160)

製品安全説明書

VEGFR阻害剤の選択性比較

生物活性

製品説明

ターゲット

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)	もっとクリックする
1.5 nM	2.5 nM	4.2 nM	7 nM	13 nM	もっとクリックする

体外試験

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. Regorafenib also inhibits FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10. Regorafenib very potently inhibited the mutant receptors KIT^K642E and RET^C634W, with IC50 of approximately 20 nM and 10 nM, respectively. Regorafenib inhibits the proliferation of VEGF¹⁶⁵-stimulated HUVECs, with an IC50 of approximately 3 nM. Regorafenib prevents the proliferation of FGF2-stimulated HUVECs and of PDGF-BB-stimulated HAoSMCs with IC50 of 127 nM and 146 nM, respectively. ^[1] 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). ^[2] Regorafenib suppresses growth of human Hep3B, PLC/PRF/5 and HepG2 cells in a concentration- and time-dependent manner. ^[3]

細胞データ

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
Hep3B	NU\McIxoSXCxcITvd4l{KEG\|c3H5	MoCxNgKBmzYEoN88US=>	NGPPcWw1QCCq		M3zTeIlvcGmkaYTzJINmdGxiZ4Lve5Rp	NFrmR2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkOyPVYxQCd-Mk[zNlk3ODh:L3G+
PLC/PRF/5	MUPBdI9xfG:\|aYOgRZN{[Xl?	NU\aSWxqOeLCk{ZCpO69VQ>?	MmjmOFghcA>?		NWD3UINycW6qaXLpeJMh[2WubDDndo94fGh?	MmPjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ\|Mkm2NFgoRjJ4M{K5OlA5RC:jPh?=
HepG2	M2PodGFxd3C2b4Ppd{BCe3OjeR?=	NYT5PXBPOeLCk{ZCpO69VQ>?	MlTuOFghcA>?		NWLjVZk{cW6qaXLpeJMh[2WubDDndo94fGh?	M3\ybVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{K5OlA5Lz5{NkOyPVYxQDxxYU6=
HEK293	MmrjSpVv[3Srb36gRZN{[Xl?	Ml2zNE426oDLzszN	MYSyM\|QwPiCq		MkTudoVlfWOnczDHVnA4QCCneIDy[ZN{cW:w	MlPaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NUiwN\|IoRjJ3OEW4NFMzRC:jPh?=
GEO	M1vMTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MlPBNE4xOS1{MDFOwG0>	MlnRPVYhcA>?	MmHUSG1UVw>?	NEPh[ZRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	NHTM[YY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizPFM6OSd-MkW4N\|g{QTF:L3G+
SW48	MkfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M37L[lAvODFvMkCg{txO	Ml3PPVYhcA>?	MXLEUXNQ	MlvBbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	M2jVNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N\|kyLz5{NUizPFM6OTxxYU6=
HT29	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4fUfVAvODFvMkCg{txO	MX:5OkBp	Ml\DSG1UVw>?	M1T5V4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	M4rST\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N\|kyLz5{NUizPFM6OTxxYU6=
SW480	NWfFcnVjT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVn3e4xyOC5yMT2yNEDPxE1?	MUO5OkBp	NH;FVXlFVVOR	MWDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	NUjqXItwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N\|g{QTFpPkK1PFM5OzlzPD;hQi=>
SW620	M1fpdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NYjJe\|RwOC5yMT2yNEDPxE1?	MkSzPVYhcA>?	MWHEUXNQ	M1zvOolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	MoHlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6M{izPVEoRjJ3OEO4N\|kyRC:jPh?=
HCT116	MlzzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MkH4NE4xOS1{MDFOwG0>	NXXPdm1ZQTZiaB?=	Mmf3SG1UVw>?	MYDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	Mon0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6M{izPVEoRjJ3OEO4N\|kyRC:jPh?=
LOVO	M3\ydWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NGrYbFYxNjBzLUKwJO69VQ>?	NF3Ue4I6PiCq	MnvRSG1UVw>?	MWLpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	MkTmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6M{izPVEoRjJ3OEO4N\|kyRC:jPh?=
HCT150	M4rxTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mnj4NE4xOS1{MDFOwG0>	NVTF[lljQTZiaB?=	MWHEUXNQ	NXz5[m86cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh\|OEO5NUc,OjV6M{izPVE9N2F-
SW48-CR	M2XkUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NIjXc\|UxNjBzLUKwJO69VQ>?	MkizPVYhcA>?	MUDEUXNQ	MknXbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	MoXIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6M{izPVEoRjJ3OEO4N\|kyRC:jPh?=
GEO-CR	M3XyO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NUPjUos{OC5yMT2yNEDPxE1?	MX:5OkBp	NYfkfJZOTE2VTx?=	Ml\VbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	NX75[FF7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N\|g{QTFpPkK1PFM5OzlzPD;hQi=>
KB-31	MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				MVjJR\|UxRTVwNdMxNE4{KG6P	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd3M{O2NUc,OjV5NUOzOlE9N2F-
KB-G2	M4e2WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				Mmm0TWM2OD17LkJCtVAvOSCwTR?=	MmjXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NUOzOlEoRjJ3N{WzN\|YyRC:jPh?=
LLC-PK1	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NW\tZ5ZWUUN3ME20Nk4xyrF\|LkKgcm0>	MlHHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NUOzOlEoRjJ3N{WzN\|YyRC:jPh?=
LLC-PK1/MRP2	M{XGb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7				M1TFemlEPTB;OEKuOOKyOi55IH7N	NVm3W3c3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OVM{PjFpPkK1O\|U{OzZzPD;hQi=>
HEK293	MoWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NXrnW2huUUN3ME2xNU4xyrFzLkKgcm0>	NFj0bFk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe1N\|M3OSd-MkW3OVM{PjF:L3G+
HEK293/OATP1B1	NVLoV\|l5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				MWHJR\|UxRTZwMtMxNE4{KG6P	M4XIeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{WzN\|YyLz5{NUe1N\|M3OTxxYU6=
HROC18	MlLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MUnJR\|UxRTFwMzFOwG0>	M4rJXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{C5PVE1Lz5{NUOwPVkyPDxxYU6=
HROC24	MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				M2\m[WlEPTB;ND62JO69VQ>?	M3L5WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{C5PVE1Lz5{NUOwPVkyPDxxYU6=
HROC43	M2jlZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				NFfCfJBKSzVyPUWuN{DPxE1?	MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyOUmxOEc,OjV\|MEm5NVQ9N2F-
HROC46	MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?				NGrPSVRKSzVyPUKuOEDPxE1?	NHT4[3Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwPVkyPCd-MkWzNFk6OTR:L3G+
RJ345	NGi2bmFHfW6ldHnvckBCe3OjeR?=	MYOwMlUwPSEQvF2=	Mm[2NlQhcA>?	NYnUNI1ZTE2VTx?=	NEjwN\|JqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44>	M4f5[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkWzPVk1Lz5{NUK1N\|k6PDxxYU6=
RJ348	NV[2THJHTnWwY4Tpc44hSXO\|YYm=	NHzLNpAxNjVxNTFOwG0>	MmnrNlQhcA>?	NUH4fIdRTE2VTx?=	M{PTZolvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=>	NVvmUJFTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOVM6QTRpPkK1NlU{QTl2PD;hQi=>
MCF-7	NILEW2FHfW6ldHnvckBCe3OjeR?=	M{ntNVAvPS93IN88US=>	MUOyOEBp	MnLaSG1UVw>?	MXTpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36=	M2Lmd\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MkWzPVk1Lz5{NUK1N\|k6PDxxYU6=
MDA-MB-231	MlzFSpVv[3Srb36gRZN{[Xl?	MVywMlUwPSEQvF2=	NFPBTYMzPCCq	NVmwVVhFTE2VTx?=	MUTpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36=	MmW0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{NUO5PVQoRjJ3MkWzPVk1RC:jPh?=
HT15	MoLyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MYmxMVIxKM7:TR?=	MnjYOFghcA>?		MYDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB5MUCxPEc,OjVyN{GwNVg9N2F-
DLD1	MoDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MVKxMVIxKM7:TR?=	NGXnT4M1QCCq		NFLO[5BqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>?	Mn[5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyN{GwNVgoRjJ3MEexNFE5RC:jPh?=
HT-29	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MXuxMVIxKM7:TR?=	MVW0PEBp		MmnjbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	NYfzdYVjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwO\|ExOThpPkK1NFcyODF6PD;hQi=>
Hct-116	M3ryNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MYqxMVIxKM7:TR?=	MUe0PEBp		NYnKdJBkcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	MmrYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyN{GwNVgoRjJ3MEexNFE5RC:jPh?=
HT15	NWD3e41oSXCxcITvd4l{KEG\|c3H5	NGTjUmsyNTFyIN88US=>	M1LFUFQ5KGh?		MlzFbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy	NUPs[\|ZqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwO\|ExOThpPkK1NFcyODF6PD;hQi=>
DLD1	M1zBdmFxd3C2b4Ppd{BCe3OjeR?=	M1HoOlEuOTBizszN	MlvpOFghcA>?		Mni1bY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy	NX\xTo95RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwO\|ExOThpPkK1NFcyODF6PD;hQi=>
HT-29	M3S4TGFxd3C2b4Ppd{BCe3OjeR?=	NHLMPFgyNTFyIN88US=>	NF:1XIE1QCCq		NHrm[HNqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB5MUCxPEc,OjVyN{GwNVg9N2F-
Hct-116	NHTSfWpCeG:ydH;zbZMhSXO\|YYm=	MXqxMVExKM7:TR?=	MUC0PEBp		M3fBWIlv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	NYTmfG5uRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwO\|ExOThpPkK1NFcyODF6PD;hQi=>
GBM5	MlvmRZBweHSxc3nzJGF{e2G7	NGXybpcxNjYkgKOxMlDjiIoQvF2=	MojKNlQhcA>?	NWT1[3ZSTE2VTx?=	M3TYfolvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=>	NHXhZ2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxNVIyPSd-MkS5NVEzOTV:L3G+
GBM6	MWXBdI9xfG:\|aYOgRZN{[Xl?	MkjVNE426oDVMT6w5qCK\|ryP	NHP3e5kzPCCq	NITINHJFVVOR	MlvibY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo	MmrLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUGyNVUoRjJ2OUGxNlE2RC:jPh?=
GBM12	M{nVUGFxd3C2b4Ppd{BCe3OjeR?=	MUWwMlXjiJNzLkFihKnPxE1?	NX;TZppkOjRiaB?=	MV\EUXNQ	MV;pcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi=	NWrHZmFTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVEzOTVpPkK0PVEyOjF3PD;hQi=>
GBM14	MX3BdI9xfG:\|aYOgRZN{[Xl?	MYmwMlXjiJNzLkFihKnPxE1?	NHfTXZczPCCq	NF7PPGdFVVOR	NXm3emJGcW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp	NYrBR25uRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NVEzOTVpPkK0PVEyOjF3PD;hQi=>
Hep3B	M1fZUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWLlPXdMOeLCk{KuOeKh\|ryP	MUKyOE81QC95MjDo		M2W4U4lvcGmkaYTzJINmdGxiZ4Lve5Rp	MlzoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OEW4PVAoRjJ2OEi1PFkxRC:jPh?=
PLC/PRF/5	MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NFHOOGky6oDVMj61xsDPxE1?	MYOyOE81QC95MjDo		MWDpcohq[mm2czDj[YxtKGe{b4f0bC=>	NGnnVWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OVg6OCd-MkS4PFU5QTB:L3G+
HepG2	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NYLT[GdqOeLCk{KuOeKh\|ryP	M363VFI1NzR6L{eyJIg>		NYDSdlFocW6qaXLpeJMh[2WubDDndo94fGh?	NVn1W5ExRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFU5QTBpPkK0PFg2QDlyPD;hQi=>
HCT116	NVfQc4FnTnWwY4Tpc44hSXO\|YYm=	MlXaNVAwOjBxNECg{txO	NV\3cohuOjRiaB?=		NYDiVZRQcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJI1TVkFiZYjwdoV{e2mxbjDpckBiKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK=	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd4M{[xNUc,OjR5NkO2NVE9N2F-
Lim2405	NHnBVodHfW6ldHnvckBCe3OjeR?=	M{PM[\|QxKM7:TR?=	NFXkepQzPCCq		NFvCfZpqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN?	M4KwUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{[zOlEyLz5{NEe2N\|YyOTxxYU6=
LoVo	Mmq4SpVv[3Srb36gRZN{[Xl?	MonkOFAh\|ryP	MkPYNlQhcA>?		NVrndpVscW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m\|	M2DDVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{[zOlEyLz5{NEe2N\|YyOTxxYU6=
Lim1215	NYPQeVNSTnWwY4Tpc44hSXO\|YYm=	MV[0NEDPxE1?	NXL1dGdJOjRiaB?=		MmPqbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{	M3;NO\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{[zOlEyLz5{NEe2N\|YyOTxxYU6=
SW48	NXPaWllsTnWwY4Tpc44hSXO\|YYm=	MUC0NEDPxE1?	MXSyOEBp		M33iNYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>?	NFXZWVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe2N\|YyOSd-MkS3OlM3OTF:L3G+
RKO	NHzqdGxHfW6ldHnvckBCe3OjeR?=	MmnwOFAh\|ryP	MUSyOEBp		M2\D[4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>?	M4rZbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{[zOlEyLz5{NEe2N\|YyOTxxYU6=
SW837	NW\iV\|BoTnWwY4Tpc44hSXO\|YYm=	NY\FNpVKPDBizszN	MlS5NlQhcA>?		NV:0eFBCcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m\|	NV22Vm16RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3OlM3OTFpPkK0O\|Y{PjFzPD;hQi=>
SW1463	MYTGeY5kfGmxbjDBd5NigQ>?	NV:3WnprPDBizszN	MWiyOEBp		MlP0bY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{	Ml;aQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5NkO2NVEoRjJ2N{[zOlEyRC:jPh?=
SW480	NEj2NpJHfW6ldHnvckBCe3OjeR?=	NIHlZVc1OCEQvF2=	NE\YNm4zPCCq		MUDpcoR2[2W\|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM>	MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd4M{[xNUc,OjR5NkO2NVE9N2F-
Vaco432	M2n6OWZ2dmO2aX;uJGF{e2G7	M4K3WFQxKM7:TR?=	NXXVT213OjRiaB?=		MUfpcoR2[2W\|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM>	M3LGOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{[zOlEyLz5{NEe2N\|YyOTxxYU6=
Vaco400	NXLIOVVuTnWwY4Tpc44hSXO\|YYm=	NELLO4Q1OCEQvF2=	MnTjNlQhcA>?		NY\Nfpk5cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m\|	M2jFNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{[zOlEyLz5{NEe2N\|YyOTxxYU6=
DLD1	M3\abGZ2dmO2aX;uJGF{e2G7	M2jYcVQxKM7:TR?=	M2HTXlI1KGh?		NHW1NHRqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN?	M4TxflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{[zOlEyLz5{NEe2N\|YyOTxxYU6=
HT29	M3jJe2Z2dmO2aX;uJGF{e2G7	NFH3b5Q1OCEQvF2=	MljmNlQhcA>?		MYXpcoR2[2W\|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM>	M1r4dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{[zOlEyLz5{NEe2N\|YyOTxxYU6=
PLC/PRF/5	NYW3OXd1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHjMbWcy6oDVNdM1US=>	MXiyOE81QC95MjDo		M3TXWIlvcGmkaYTzJINmdGxiZ4Lve5Rp	MkHlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNzNkmxOFgoRjJ\|MU[5NVQ5RC:jPh?=
HepG2	MmHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXTtU\|RWOeLCk{ZCuW0>	M2jOTlI1NzR6L{eyJIg>		MnHzbY5pcWKrdIOgZ4VtdCCpcn;3eIg>	MmHRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjNzNkmxOFgoRjJ\|MU[5NVQ5RC:jPh?=
Hep3B	NV;mSJhlT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4HLN\|HjiJN3wsXN	M{fXOFI1NzR6L{eyJIg>		NYPuR5dIcW6qaXLpeJMh[2WubDDndo94fGh?	MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzF4OUG0PEc,OjNzNkmxOFg9N2F-
BA/F3	NYLTfXlsT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MnjaO\|IhcHK\|		MYHJcohq[mm2aX;uJI9nKEurdDDlfI9vKDFzIHTlcIV1cW:wIDi1OVchfG9iNUW4JJJme2mmdXXzLUBufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NEA:KDBwMEKxJO69VS5?	MoTUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
BA/F3	NEHXUJlIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M{PMOlczKGi{cx?=		Ml;NTY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiUFTHSnJj\XSjIDj1cotvd3ewIH;ybYdqdilidILhcpNn\WO2ZXSgbY4hdW:3c3WgRmEwTjNiY3XscJMh[XO\|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIHfyc5d1cCCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBOXFNiYYPzZZktKEeLNUCgQUAxNjB{OTFOwG0v	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
BA/F3	Moj4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		Mke4O\|IhcHK\|		Ml\DTY5pcWKrdHnvckBw\iCNaYSg[ZhwdiBzMTDk[YxmfGmxbjCoOVU4KHSxIEW1PEBz\XOrZIXld{kh[W6mIFS4NVZJKG23dHHueEBidmRiVE[3NGkhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVAhRSByLkCzN{DPxE1w	NFrwZYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
BA/F3	M3\ubGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NF:zZpE4OiCqcoO=		M4rP[mlvcGmkaYTpc44hd2ZiS3n0JIV5d25iMUGg[IVt\XSrb36gLFU2PyC2bzC1OVghemW\|aXT1[ZMqKGGwZDDBPFI6WCCvdYThcpQh[W6mIGm4NlNFKG23dHHueEApfW6tbn;3ckBwemmpaX6pJJRz[W6\|ZnXjeIVlKGmwIH3veZNmKEKDL1[zJINmdGy\|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxKD1iMD6wOFch\|ryPLh?=	MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJyNES0NUc,OzB{MES0OFE9N2F-
BA/F3	NHf1cnRIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MV:3NkBpenN?		M{L1d2lvcGmkaYTpc44hd2ZiS3n0JIV5d25iMUGg[IVt\XSrb36gLFU2PyC2bzC1OVghemW\|aXT1[ZMqKGGwZDDOPFIzUyCvdYThcpQh[W6mIGm4NlNFKG23dHHueEApfW6tbn;3ckBwemmpaX6pJJRz[W6\|ZnXjeIVlKGmwIH3veZNmKEKDL1[zJINmdGy\|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxKD1iMD6wOFkh\|ryPLh?=	M1S2WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5\|MEKwOFQ1OTxxYU6=
BA/F3	MmG3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		M2nFelczKGi{cx?=		MlzYTY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiUFTHSnJidHCqYTCoeY5sdm:5bjDvdolocW5rIITyZY5{\mWldHXkJIlvKG2xdYPlJGJCN0Z\|IHPlcIx{KGG\|c3Xzd4VlKGG\|IHnubIljcXSrb36gc4Yh[2WubDDndo94fGhiaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCJSUWwJF0hOC5yNUGg{txONg>?	M{DROVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5\|MEKwOFQ1OTxxYU6=
BA/F3	M{HhWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NFrFeXI4OiCqcoO=		NXnuT2RbUW6qaXLpeIlwdiCxZjDLbZQh\XixbjCxNUBl\WyndHnvckApPTV5IITvJFU2QCC{ZYPp[JVmeyliYX7kJGQ5OjCDIH31eIFvfCCjbnSgSFgzOEFibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkhfHKjboPm[YN1\WRiaX6gcY92e2ViQlGvSlMh[2WubIOgZZN{\XO\|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKGe{b4f0bEBqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO\|YYmsJGdKPTBiPTCwMlA3OyEQvF2u	NI\iOY49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
BA/F3	NYPHclFxT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MX23NkBpenN?		NWfUNWtsUW6qaXLpeIlwdiCxZjDLbZQh\XixbjCxNUBl\WyndHnvckApPTV5IITvJFU2QCC{ZYPp[JVmeyliYX7kJHk5OjOGIH31eIFvfCBqdX7rco94diCxcnnnbY4qKHS{YX7z[oVkfGWmIHnuJI1wfXOnIFLBM2Y{KGOnbHzzJIF{e2W\|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCpcn;3eIghcW6ldXLheIVlKG[xcjC3NkBpenNiYomgUXRUKGG\|c3H5MEBIUTVyIE2gNE4xQTRizszNMi=>	MnK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
BA/F3	NEi2fVZIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M2H1fFczKGi{cx?=		M3nEOWlvcGmkaYTpc44hd2ZiS3n0JHY2PjCGIH31eIFvfCBqdX7rco94diCxcnnnbY4qKHS{YX7z[oVkfGWmIHnuJI1wfXOnIFLBM2Y{KGOnbHzzJIF{e2W\|c3XkJIF{KGmwaHnibZRqd25ib3[gZ4VtdCCpcn;3eIghcW6ldXLheIVlKG[xcjC3NkBpenNiYomgUXRUKGG\|c3H5MEBIUTVyIE2gNE4yODhizszNMi=>	NXPYdFdURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
BA/F3	M2Gyb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NHXzWGo4OiCqcoO=		MV\Jcohq[mm2aX;uJI9nKEurdDDlfI9vKDliQWm1NFIhfG9iNUCzJIlve2W{dHnvckBufXSjboSgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NEA:KDBwMUG0JO69VS5?	M1XiflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5\|MEKwOFQ1OTxxYU6=
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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

体内試験

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. ^[1]

お薦めの試験操作（参考用のみ）

キナーゼ試験：^[1]	- 合併 Kinase assays: In vitro assays using recombinant VEGFR2 (murine aa785–aa1367), VEGFR3 (murine aa818–aa1363), PDGFRβ (aa561–aa1106), Raf-1 (aa305–aa648) and BRafV600E (aa409–aa765) kinase domains are performed. Initial in vitro kinase inhibition profiling is performed at a fixed 1 μM Regorafenib concentration. Inhibitory concentration of 50% (IC50) values are determined from selected responding kinases, e.g., VEGFR1 and RET. TIE2 kinase inhibition is measured with a homogeneous time-resolved fluorescence (HTRF) assay using a recombinant fusion protein of glutathione-S-transferase, the intracellular domain of TIE2 and the peptide biotin-Ahx-EPKDDAYPLYSDFG as substrate.
細胞試験： ^[1]	- 合併細胞株： GIST 882 and TT cells 濃度： 5 nM-10 μM 反応時間： 96 hours 実験の流れ： For proliferation assays, GIST 882 and TT cells are grown in RPMI medium containing L-glutamine, and MDA-MB-231, HepG2 and A375 cells in DMEM always containing 10% hiFBS. Cells are trypsinized, plated at 5×104 cells/well in 96-well plates in complete media containing 10% FBS and grown overnight at 37 °C. The next day, vehicle or Regorafenib serially diluted in complete growth media to between 10 μM and 5 nM final concentrations, and 0.2% DMSO, is added and incubation is continued for 96 hours. Cell proliferation is quantified. (参考用のみ)
動物試験：^[1]	- 合併動物モデル： Female athymic NCr nu/nu mice with Colo-205, MDA-MB-231 or 786-O 投薬量： 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg 投与方法： Orally (参考用のみ)

参考

溶解度 (25°C)

体外	DMSO	97 mg/mL (200.9 mM)
	Water	Insoluble
	Ethanol	Insoluble
体内	左から（NMPから）右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ): 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 混合させたのち直ちに使用することを推奨します。	5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報 Regorafenib (BAY 73-4506) SDFをダウンロードする

分子量	482.82
化学式	C₂₁H₁₅ClF₄N₄O₃
CAS No.	755037-03-7
Storage	3 years-20°C powder 2 years-80°C in solvent
別名	Fluoro-Sorafenib, Resihance, Stivarga
Smiles	CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F

投与溶媒組成計算器(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量

mg/kg

動物平均体重

投与体積（動物毎）

動物数

匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO+ % + % Tween 80+ % ddH₂O

計算リセット

計算結果:

投与溶媒濃度： mg/ml；

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL，注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。）

投与溶媒調製方法：μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

便利ツール

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

質量

濃度

体積

分子量
=

×

×

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとSDS/COA（製品ページで利用可能な）。

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます：

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます：C1V1 = C2V2 ( 入力出力 )

C1

V1

C2

V2
×

=

×

常に貯蔵液を準備するとき、小びんラベルとSDS/COA（オンラインで利用できる）で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

連続希釈剤
初めの濃度：
稀釈倍数：

計算結果

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):

分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください：

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

臨床試験 (data from https://clinicaltrials.gov, updated on 2022-01-17)

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	Terminated	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

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須
*大学・企業名:
*名前:
*電子メール:
*電話番号:
*内容:

よくある質問（FAQ）

質問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シグナル伝達経路

VEGFR Inhibitors with Unique Features

Selective VEGFR Inhibitors

Vandetanib (ZD6474) : VEGFR2-selective, IC50=40 nM.
Most Potent VEGFR Inhibitor

Cabozantinib (XL184, BMS-907351) : VEGFR2, IC50=0.035 nM.
FDA-approved VEGFR Inhibitor

Axitinib : Approved by FDA for Renal Cell Carcinoma.
Classic VEGFR Inhibitor

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.

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SU5402

SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.
Erlotinib (OSI-774)

Erlotinib (OSI-774, CP358774, NSC 718781, Tarceva) is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. Erlotinib induces autophagy.
Bemcentinib (R428)

Bemcentinib (R428, BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective).
Axitinib (AG 013736)

Axitinib (AG 013736) is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.

Features:Superior as second-line therapy relative to sorafenib (current standard-of-care).
Cabozantinib (BMS-907351)

Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway.
Nintedanib (BIBF 1120)

Nintedanib (BIBF 1120, Intedanib, Vargatef, Ofev) is a 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 in cell-free assays. Phase 3.
Vandetanib (ZD6474)

Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).

研究分野別

製品類型

Regorafenib (BAY 73-4506)

文献中Selleckの製品使用例(160)

製品安全説明書

VEGFR阻害剤の選択性比較

生物活性

お薦めの試験操作（参考用のみ）

参考

溶解度 (25°C)

化学情報 Regorafenib (BAY 73-4506) SDFをダウンロードする

投与溶媒組成計算器(クリア溶液)

便利ツール

モル濃度計算器

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

希釈計算器

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

連続希釈計算器方程式

連続希釈剤

計算結果

分子量计算器

総分子量：g/mol

モル濃度計算器

臨床試験 (data from https://clinicaltrials.gov, updated on 2022-01-17)

技術サポート

よくある質問（FAQ）

VEGFRシグナル伝達経路

VEGFR Inhibitors with Unique Features

相関VEGFR製品