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
10mg	JPY 36800
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]

文献中Selleckの製品使用例(133)

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	M17tNGFxd3C2b4Ppd{BCe3OjeR?=	NFTiWYky6oDVNdMg{txO	NYTN[Gh5PDhiaB?=		NUPnXow{cW6qaXLpeJMh[2WubDDndo94fGh?	MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN{OU[wPEc,OjZ\|Mkm2NFg9N2F-
PLC/PRF/5	NX7aZmxCSXCxcITvd4l{KEG\|c3H5	M{HTW\|HjiJN3wrFOwG0>	MYm0PEBp		NWXOOHRLcW6qaXLpeJMh[2WubDDndo94fGh?	MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN{OU[wPEc,OjZ\|Mkm2NFg9N2F-
HepG2	Mk\ERZBweHSxc3nzJGF{e2G7	NYrEbox3OeLCk{ZCpO69VQ>?	NHHQ[G01QCCq		MWXpcohq[mm2czDj[YxtKGe{b4f0bC=>	NFnpO3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkOyPVYxQCd-Mk[zNlk3ODh:L3G+
HEK293	MUPGeY5kfGmxbjDBd5NigQ>?	NXTES4ZCOC534pEJ{txO	NUfrfVdLOi92L{[gbC=>		MVPy[YR2[2W\|IFfSVFc5KGW6cILld5Nqd25?	Mnq5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV6NUiwN\|IoRjJ3OEW4NFMzRC:jPh?=
GEO	M1\NRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4nR[FAvODFvMkCg{txO	MXS5OkBp	MWTEUXNQ	M{T4SYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh\|OEO5NUc,OjV6M{izPVE9N2F-
SW48	M176cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MkLiNE4xOS1{MDFOwG0>	M{TTUFk3KGh?	MmHOSG1UVw>?	MWDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	M3vLZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N\|kyLz5{NUizPFM6OTxxYU6=
HT29	Mni4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1nXRVAvODFvMkCg{txO	MmTyPVYhcA>?	NI[0cmxFVVOR	NXS4TlZ5cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	NVPEPXJQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N\|g{QTFpPkK1PFM5OzlzPD;hQi=>
SW480	M164RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MVmwMlAyNTJyIN88US=>	MnG2PVYhcA>?	NGTLZ4JFVVOR	M{fMeIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	NGW2dYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizPFM6OSd-MkW4N\|g{QTF:L3G+
SW620	MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NEnSdFQxNjBzLUKwJO69VQ>?	MX:5OkBp	NUiyWJp[TE2VTx?=	M1L3NIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	M1vHV\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N\|kyLz5{NUizPFM6OTxxYU6=
HCT116	NGXTO2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NIDQfpIxNjBzLUKwJO69VQ>?	NGexdGE6PiCq	M2i0dmROW09?	MnnpbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh\|OEO5NUc,OjV6M{izPVE9N2F-
LOVO	MnzXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2O4XFAvODFvMkCg{txO	MmP2PVYhcA>?	MYDEUXNQ	MYjpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	NFjheoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUizPFM6OSd-MkW4N\|g{QTF:L3G+
HCT150	M{\wU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWCwMlAyNTJyIN88US=>	NXPWV3FIQTZiaB?=	NHHLdppFVVOR	MnvobY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTh\|OEO5NUc,OjV6M{izPVE9N2F-
SW48-CR	Mkn3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NUW3eXF7OC5yMT2yNEDPxE1?	NWTBR2tPQTZiaB?=	MV;EUXNQ	MYDpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	M1i4VlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N\|kyLz5{NUizPFM6OTxxYU6=
GEO-CR	NWLB[XA1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MlHtNE4xOS1{MDFOwG0>	NHjsXnE6PiCq	MXvEUXNQ	MkfMbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	M2LSOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N\|kyLz5{NUizPFM6OTxxYU6=
KB-31	MmTuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MYTJR\|UxRTVwNdMxNE4{KG6P	NEXPVYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe1N\|M3OSd-MkW3OVM{PjF:L3G+
KB-G2	NHvlcmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M{PrVWlEPTB;OT6xxtExNjFibl2=	M37x[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{WzN\|YyLz5{NUe1N\|M3OTxxYU6=
LLC-PK1	NHvQ[oZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=				M3r5dWlEPTB;NEKuNOKyOy5{IH7N	MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd3M{O2NUc,OjV5NUOzOlE9N2F-
LLC-PK1/MRP2	MnzOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				M4izXGlEPTB;OEKuOOKyOi55IH7N	NV7ofXRWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OVM{PjFpPkK1O\|U{OzZzPD;hQi=>
HEK293	Ml;uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				NWHwNJd[UUN3ME2xNU4xyrFzLkKgcm0>	NYXjSWpWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW3OVM{PjFpPkK1O\|U{OzZzPD;hQi=>
HEK293/OATP1B1	MlLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				MlXGTWM2OD14LkNCtVAvOyCwTR?=	MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd3M{O2NUc,OjV5NUOzOlE9N2F-
HROC18	M3;U[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7				MX3JR\|UxRTFwMzFOwG0>	M{\aXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{C5PVE1Lz5{NUOwPVkyPDxxYU6=
HROC24	NXnCTYk2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NUTKbIF7UUN3ME20MlYh\|ryP	NIq5[XQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwPVkyPCd-MkWzNFk6OTR:L3G+
HROC43	NV3YUWI6T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=				NVe5SoRlUUN3ME21MlMh\|ryP	NG\NSGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUOwPVkyPCd-MkWzNFk6OTR:L3G+
HROC46	MoLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?				Ml3STWM2OD1{LkSg{txO	M4K3WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{C5PVE1Lz5{NUOwPVkyPDxxYU6=
RJ345	NV:wdlVTTnWwY4Tpc44hSXO\|YYm=	NXLrfW9zOC53L{Wg{txO	M4S3cFI1KGh?	MVrEUXNQ	MlfUbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ3M{m5OEc,OjV{NUO5PVQ9N2F-
RJ348	NV3iUJdLTnWwY4Tpc44hSXO\|YYm=	MkHxNE42NzVizszN	MmLjNlQhcA>?	MoLZSG1UVw>?	M{S2d4lvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=>	NXPTOG9jRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOVM6QTRpPkK1NlU{QTl2PD;hQi=>
MCF-7	M1G0emZ2dmO2aX;uJGF{e2G7	NIXLR4MxNjVxNTFOwG0>	MYmyOEBp	M1jPVGROW09?	MnLzbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u	NFvQNFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK1N\|k6PCd-MkWyOVM6QTR:L3G+
MDA-MB-231	NWTiWYdVTnWwY4Tpc44hSXO\|YYm=	NU\KR2I2OC53L{Wg{txO	NXzsS3RJOjRiaB?=	MVfEUXNQ	M2XpcYlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=>	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTJ3M{m5OEc,OjV{NUO5PVQ9N2F-
HT15	NHTIdJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MVyxMVIxKM7:TR?=	NYPmPFQ5PDhiaB?=		MYHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	M1nTTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEexNFE5Lz5{NUC3NVAyQDxxYU6=
DLD1	MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NUDzSYdOOS1{MDFOwG0>	NXm1TYZ7PDhiaB?=		MWrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=>	MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB5MUCxPEc,OjVyN{GwNVg9N2F-
HT-29	NGO4b2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M{HkXlEuOjBizszN	MnvROFghcA>?		M2\nWolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz	MmHOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyN{GwNVgoRjJ3MEexNFE5RC:jPh?=
Hct-116	NWfBfnl4T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NHrxN3IyNTJyIN88US=>	NWjJd484PDhiaB?=		NV7NfJY2cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ?	NWTvfXU6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwO\|ExOThpPkK1NFcyODF6PD;hQi=>
HT15	MVTBdI9xfG:\|aYOgRZN{[Xl?	M3\KOVEuOTBizszN	Ml3EOFghcA>?		Mni1bY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy	NXXnfWJERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwO\|ExOThpPkK1NFcyODF6PD;hQi=>
DLD1	M3vLbGFxd3C2b4Ppd{BCe3OjeR?=	M3vBdlEuOTBizszN	NIjCOYs1QCCq		NEXtN3RqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI>	NHSxd5A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC3NVAyQCd-MkWwO\|ExOTh:L3G+
HT-29	M3jTZmFxd3C2b4Ppd{BCe3OjeR?=	NWHScmlZOS1zMDFOwG0>	MofSOFghcA>?		MWnpcoR2[2W\|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=	M{fVR\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3MEexNFE5Lz5{NUC3NVAyQDxxYU6=
Hct-116	NV7WWYk6SXCxcITvd4l{KEG\|c3H5	NWLaW2hbOS1zMDFOwG0>	NUnkOFdYPDhiaB?=		MX7pcoR2[2W\|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK=	MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB5MUCxPEc,OjVyN{GwNVg9N2F-
GBM5	NX;ISZBESXCxcITvd4l{KEG\|c3H5	M{DNRVAvPeLCk{GuNQKBkc7:TR?=	MnzrNlQhcA>?	NXvvS214TE2VTx?=	NGnLZnpqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg>	MkT0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUGyNVUoRjJ2OUGxNlE2RC:jPh?=
GBM6	NHPYcnRCeG:ydH;zbZMhSXO\|YYm=	M4\RUlAvPeLCk{GuNQKBkc7:TR?=	NIHPd\|EzPCCq	MYDEUXNQ	MXHpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi=	M4PsOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUGxNlE2Lz5{NEmxNVIyPTxxYU6=
GBM12	MXPBdI9xfG:\|aYOgRZN{[Xl?	MYmwMlXjiJNzLkFihKnPxE1?	NGLpUXozPCCq	MlvpSG1UVw>?	NFrmUWVqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg>	M1vnWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUGxNlE2Lz5{NEmxNVIyPTxxYU6=
GBM14	NX32ZZB3SXCxcITvd4l{KEG\|c3H5	MkXNNE426oDVMT6w5qCK\|ryP	Mn[1NlQhcA>?	M2raN2ROW09?	NVHUW3l5cW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp	M3nufFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUGxNlE2Lz5{NEmxNVIyPTxxYU6=
Hep3B	MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXLIWVVOOeLCk{KuOeKh\|ryP	NX\vcG1lOjRxNEivO\|IhcA>?		MlW0bY5pcWKrdIOgZ4VtdCCpcn;3eIg>	M4PmeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi1PFkxLz5{NEi4OVg6ODxxYU6=
PLC/PRF/5	MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MmDuNgKBmzJwNdMg{txO	MV2yOE81QC95MjDo		MXfpcohq[mm2czDj[YxtKGe{b4f0bC=>	NXm2dHI5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFU5QTBpPkK0PFg2QDlyPD;hQi=>
HepG2	NWTTRoFxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4S2fFHjiJN{LkZCpO69VQ>?	NEfMeYozPC92OD:3NkBp		NF71UmJqdmirYnn0d{Bk\WyuIHfyc5d1cA>?	Mn7OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OEW4PVAoRjJ2OEi1PFkxRC:jPh?=
HCT116	NU\4eI9vTnWwY4Tpc44hSXO\|YYm=	NHH1[GEyOC9{MD:0NEDPxE1?	NXSyeZNKOjRiaB?=		M2XrWIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDtVm5CKGW6cILld5Nqd25iaX6gZUBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgcYFvdmW{	M2DK[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{[zOlEyLz5{NEe2N\|YyOTxxYU6=
Lim2405	MX7GeY5kfGmxbjDBd5NigQ>?	MoizOFAh\|ryP	NXLoe2RYOjRiaB?=		NYnpS\|RNcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m\|	NFr6[VY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe2N\|YyOSd-MkS3OlM3OTF:L3G+
LoVo	NIHVcnhHfW6ldHnvckBCe3OjeR?=	MojuOFAh\|ryP	M1[5ZVI1KGh?		NG\lc41qdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN?	MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd4M{[xNUc,OjR5NkO2NVE9N2F-
Lim1215	MV\GeY5kfGmxbjDBd5NigQ>?	MnT0OFAh\|ryP	NITKcVEzPCCq		M3;KZYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>?	NV\TTZRbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3OlM3OTFpPkK0O\|Y{PjFzPD;hQi=>
SW48	MW\GeY5kfGmxbjDBd5NigQ>?	M2rEbVQxKM7:TR?=	MmLaNlQhcA>?		NYC1[YhNcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m\|	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd4M{[xNUc,OjR5NkO2NVE9N2F-
RKO	MXrGeY5kfGmxbjDBd5NigQ>?	NYDVZ2EyPDBizszN	NUXzPYY5OjRiaB?=		MlXibY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{	NWnFfGJ5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3OlM3OTFpPkK0O\|Y{PjFzPD;hQi=>
SW837	MU\GeY5kfGmxbjDBd5NigQ>?	NFThd3o1OCEQvF2=	Mn3xNlQhcA>?		NXPtOWh[cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m\|	MlXkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR5NkO2NVEoRjJ2N{[zOlEyRC:jPh?=
SW1463	Mlz4SpVv[3Srb36gRZN{[Xl?	M1;qVVQxKM7:TR?=	NWLtNZduOjRiaB?=		M2\Xfolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>?	M4f3e\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{[zOlEyLz5{NEe2N\|YyOTxxYU6=
SW480	NYezXG9yTnWwY4Tpc44hSXO\|YYm=	M2HKd\|QxKM7:TR?=	MnX6NlQhcA>?		NVjQTHZicW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m\|	NWW1V5RXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3OlM3OTFpPkK0O\|Y{PjFzPD;hQi=>
Vaco432	NHTqe41HfW6ldHnvckBCe3OjeR?=	Mnm4OFAh\|ryP	MWKyOEBp		NF3sOldqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN?	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd4M{[xNUc,OjR5NkO2NVE9N2F-
Vaco400	M2\Dc2Z2dmO2aX;uJGF{e2G7	MmHtOFAh\|ryP	NFPjbIIzPCCq		NFq5RYhqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN?	M2jUWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{[zOlEyLz5{NEe2N\|YyOTxxYU6=
DLD1	NVTyUGhoTnWwY4Tpc44hSXO\|YYm=	M3\0dFQxKM7:TR?=	M4CzWFI1KGh?		M{XVZYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>?	NYjDW4RbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3OlM3OTFpPkK0O\|Y{PjFzPD;hQi=>
HT29	NWfqdpZpTnWwY4Tpc44hSXO\|YYm=	MnPhOFAh\|ryP	NYjwcVZROjRiaB?=		NX3ONoN7cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m\|	NF3lSo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEe2N\|YyOSd-MkS3OlM3OTF:L3G+
PLC/PRF/5	MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M171R\|HjiJN3wsXN	MXGyOE81QC95MjDo		MXTpcohq[mm2czDj[YxtKGe{b4f0bC=>	NV7jOphzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOxOlkyPDhpPkKzNVY6OTR6PD;hQi=>
HepG2	NUTJZoM2T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NFHKO3cy6oDVNdM1US=>	NVTPe4xXOjRxNEivO\|IhcA>?		M4P6bIlvcGmkaYTzJINmdGxiZ4Lve5Rp	NGO4PIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{G2PVE1QCd-MkOxOlkyPDh:L3G+
Hep3B	MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MV6x5qCUPcL3TR?=	M334SVI1NzR6L{eyJIg>		NYXSNVNEcW6qaXLpeJMh[2WubDDndo94fGh?	NFLxV3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{G2PVE1QCd-MkOxOlkyPDh:L3G+
BA/F3	NEHINJNIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NF\hXII4OiCqcoO=		NWHNV2FjUW6qaXLpeIlwdiCxZjDLbZQh\XixbjCxNUBl\WyndHnvckApPTV5IITvJFU2QCC{ZYPp[JVmeylibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkhfHKjboPm[YN1\WRiaX6gcY92e2ViQlGvSlMh[2WubIOgZZN{\XO\|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKGe{b4f0bEBqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO\|YYmsJGdKPTBiPTCwMlAzOSEQvF2u	Mmr2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
BA/F3	MlLOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MVO3NkBpenN?		MkfwTY5pcWKrdHnvckBw\iCWRVyt[pV{\WRiUFTHSnJj\XSjIDj1cotvd3ewIH;ybYdqdilidILhcpNn\WO2ZXSgbY4hdW:3c3WgRmEwTjNiY3XscJMh[XO\|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIHfyc5d1cCCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBOXFNiYYPzZZktKEeLNUCgQUAxNjB{OTFOwG0v	M3XHcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5\|MEKwOFQ1OTxxYU6=
BA/F3	MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NG\ndYE4OiCqcoO=		MojsTY5pcWKrdHnvckBw\iCNaYSg[ZhwdiBzMTDk[YxmfGmxbjCoOVU4KHSxIEW1PEBz\XOrZIXld{kh[W6mIFS4NVZJKG23dHHueEBidmRiVE[3NGkhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVAhRSByLkCzN{DPxE1w	M{HmN\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5\|MEKwOFQ1OTxxYU6=
BA/F3	NFPxWFNIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M4[4R\|czKGi{cx?=		NY\QdJd4UW6qaXLpeIlwdiCxZjDLbZQh\XixbjCxNUBl\WyndHnvckApPTV5IITvJFU2QCC{ZYPp[JVmeyliYX7kJGE5OjmSIH31eIFvfCCjbnSgXVgzO0RibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkhfHKjboPm[YN1\WRiaX6gcY92e2ViQlGvSlMh[2WubIOgZZN{\XO\|ZXSgZZMhcW6qaXLpeIlwdiCxZjDj[YxtKGe{b4f0bEBqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDNWHMh[XO\|YYmsJGdKPTBiPTCwMlA1PyEQvF2u	NHzwUG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9\|MEKwOFQ1OSd-M{CyNFQ1PDF:L3G+
BA/F3	MlnCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		M4fZZ\|czKGi{cx?=		M{XYNWlvcGmkaYTpc44hd2ZiS3n0JIV5d25iMUGg[IVt\XSrb36gLFU2PyC2bzC1OVghemW\|aXT1[ZMqKGGwZDDOPFIzUyCvdYThcpQh[W6mIGm4NlNFKG23dHHueEApfW6tbn;3ckBwemmpaX6pJJRz[W6\|ZnXjeIVlKGmwIH3veZNmKEKDL1[zJINmdGy\|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3XscEBoem:5dHigbY5kfWKjdHXkJIZweiB5MjDodpMh[nliTWTTJIF{e2G7LDDHTVUxKD1iMD6wOFkh\|ryPLh?=	NYjCW2NrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CyNFQ1PDFpPkOwNlA1PDRzPD;hQi=>
BA/F3	Ml7OS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NGDCfGY4OiCqcoO=		M4r1RmlvcGmkaYTpc44hd2ZiVFXMMYZ2e2WmIGDES2ZT[WyyaHGgLJVvc26xd36gc5Jq\2mwKTD0doFve2[nY4Tl[EBqdiCvb4Xz[UBDSS:IMzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGOnbHyg[5Jwf3SqIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KE2WUzDhd5NigSxiR1m1NEA:KDBwMEWxJO69VS5?	MnTzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{MES0OFEoRjNyMkC0OFQyRC:jPh?=
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BA/F3	NITZc4lIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MVK3NkBpenN?		MYPJcohq[mm2aX;uJI9nKEurdDDlfI9vKDFzIHTlcIV1cW:wIDi1OVchfG9iNUW4JJJme2mmdXXzLUBidmRiWUiyN2QhdXW2YX70JEh2dmuwb4fuJI9zcWerbjmgeJJidnOoZXP0[YQhcW5ibX;1d4UhSkFxRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iClZXzsJIdzd3e2aDDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSCPVGOgZZN{[XluIFfJOVAhRSByLkC5OEDPxE1w	M4XHeVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMkC0OFQyLz5\|MEKwOFQ1OTxxYU6=
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他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ

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MSDS/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MSDS/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 2021-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04476329	Recruiting	Drug: Regorafenib 40 MG	Hepatocellular Carcinoma	SC Liver Research Consortium LLC\|Bayer	December 15 2020	Phase 2
NCT04200404	Recruiting	Drug: CS1001\|Drug: Regorafenib	Advanced Refractory Solid Tumors	CStone Pharmaceuticals\|Bayer	December 13 2019	Phase 1\|Phase 2
NCT03793361	Recruiting	Drug: Regorafenib\|Drug: Placebo	Metastatic Soft Tissue Sarcoma	Centre Oscar Lambret	May 15 2019	Phase 2
NCT03829852	Recruiting	Drug: Regorafenib	Metastatic Colorectal Cancer	Taipei Veterans General Hospital Taiwan\|Chang Gung Memorial Hospital\|Koo Foundation Sun Yat-Sen Cancer Center	March 29 2019	--

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

Erlotinib (CP358774, NSC 718781, OSI-774) 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

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(133)

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 2021-01-06)

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