Regorafenib (BAY 73-4506)

For research use only. Not for use in humans.

目录号:S1178 别名: Fluoro-Sorafenib

Regorafenib (BAY 73-4506) Chemical Structure

CAS No. 755037-03-7

Regorafenib (BAY 73-4506, Fluoro-Sorafenib) 是一个多靶点抑制剂,作用于VEGFR1VEGFR2VEGFR3PDGFR-βKitRETRaf-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
RMB 972.87 现货
RMB 1733.78 现货
RMB 3830.98 现货
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117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 Regorafenib (BAY 73-4506, Fluoro-Sorafenib) 是一个多靶点抑制剂,作用于VEGFR1VEGFR2VEGFR3PDGFR-βKitRETRaf-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。
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)
1.5 nM 2.5 nM 4.2 nM 7 nM 13 nM
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KITK642E 和 RETC634W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 NH74eWlCeG:ydH;zbZMhSXO|YYm= MY[x5qCUPcLizszN Mn7oOFghcA>? MUfpcohq[mm2czDj[YxtKGe{b4f0bC=> MlLwNlY{Ojl4MEi=
PLC/PRF/5  NW\rdHY1SXCxcITvd4l{KEG|c3H5 MXyx5qCUPcLizszN MnG1OFghcA>? MYnpcohq[mm2czDj[YxtKGe{b4f0bC=> MUOyOlMzQTZyOB?=
HepG2  MXTBdI9xfG:|aYOgRZN{[Xl? NVnhXlhrOeLCk{ZCpO69VQ>? M1e3OlQ5KGh? NH7ONVNqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NEm4flIzPjN{OU[wPC=>
HEK293 NX7P[YtYTnWwY4Tpc44hSXO|YYm= MlizNE426oDLzszN Mny1Nk81NzZiaB?= MlS3doVlfWOnczDHVnA4QCCneIDy[ZN{cW:w M{XVNlI2QDV6MEOy
GEO M1TFRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUKwMlAyNTJyIN88US=> M33jTlk3KGh? NGO2VIRFVVOR MYnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NW\wfpVTOjV6M{izPVE>
SW48 MmfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfpSlQxNjBzLUKwJO69VQ>? NWDMRVRwQTZiaB?= MV\EUXNQ MXrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NXvPe|VSOjV6M{izPVE>
HT29 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1K2[VAvODFvMkCg{txO M4O0PFk3KGh? MkDXSG1UVw>? MmLvbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M4fUflI2QDN6M{mx
SW480 NEm3SlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkD0NE4xOS1{MDFOwG0> NWjG[JBlQTZiaB?= NHfrNGdFVVOR NInlVW5qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NUPYRndvOjV6M{izPVE>
SW620 NUHCXI14T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSwMlAyNTJyIN88US=> NXq2ZmZnQTZiaB?= NIfvTmNFVVOR MXzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NEnrOFIzPTh|OEO5NS=>
HCT116 NWDSSXZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFH6R2MxNjBzLUKwJO69VQ>? NIrVRog6PiCq M2rLPWROW09? MUfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mlr1NlU5Ozh|OUG=
LOVO NW[zSlJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3yxfFAvODFvMkCg{txO Mo\zPVYhcA>? NWTBWXBSTE2VTx?= M3jnbIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXXuZmR[OjV6M{izPVE>
HCT150 M4fVeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX33Oow2OC5yMT2yNEDPxE1? M3nlcVk3KGh? M1fRdGROW09? MV7pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M4jzSlI2QDN6M{mx
SW48-CR MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDuNnNzOC5yMT2yNEDPxE1? M4Kwelk3KGh? MlrxSG1UVw>? MonIbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYOyOVg{QDN7MR?=
GEO-CR NUn3PXRsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXW[ooxNjBzLUKwJO69VQ>? MlHKPVYhcA>? MnXrSG1UVw>? NGjKWItqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NV6wW2xmOjV6M{izPVE>
KB-31 NGK2OHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIO3NVVKSzVyPUWuOeKyOC5|IH7N MXOyOVc2OzN4MR?=
KB-G2 NGPXZVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHftNYhKSzVyPUmuNeKyOC5zIH7N NITpUnczPTd3M{O2NS=>
LLC-PK1 M{TkUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\IXnlKSzVyPUSyMlDDuTNwMjDuUS=> MWWyOVc2OzN4MR?=
LLC-PK1/MRP2 Mn;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;B[HZqUUN3ME24Nk41yrF{Lkegcm0> NWfycWp6OjV5NUOzOlE>
HEK293 M1HjcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7DTWM2OD1zMT6wxtEyNjJibl2= NH[wWmszPTd3M{O2NS=>
HEK293/OATP1B1 M2TGdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTZwMtMxNE4{KG6P M{P4UFI2PzV|M{[x
HROC18 MoDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTFwMzFOwG0> M2TWSlI2OzB7OUG0
HROC24 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUCzclR2UUN3ME20MlYh|ryP M3nXTVI2OzB7OUG0
HROC43 NWfjNGxqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPvWZRKSzVyPUWuN{DPxE1? M4n1R|I2OzB7OUG0
HROC46 NUXL[o5YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\WTWM2OD1{LkSg{txO M1jjSlI2OzB7OUG0
RJ345 M1TCdGZ2dmO2aX;uJGF{e2G7 MY[wMlUwPSEQvF2= NWP0PHJIOjRiaB?= NVjk[oZDTE2VTx?= M4\zdolvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> NFj1WG4zPTJ3M{m5OC=>
RJ348 M1;OcWZ2dmO2aX;uJGF{e2G7 NGnoco8xNjVxNTFOwG0> NWj6dYcyOjRiaB?= MYrEUXNQ M4fCdolvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> Mkn3NlUzPTN7OUS=
MCF-7 MWLGeY5kfGmxbjDBd5NigQ>? NHzjXpYxNjVxNTFOwG0> NHe4ZnEzPCCq MX;EUXNQ MYXpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= NXS5OWZXOjV{NUO5PVQ>
MDA-MB-231 Ml\QSpVv[3Srb36gRZN{[Xl? NVfWW2c4OC53L{Wg{txO NX\KRWVMOjRiaB?= M1;sV2ROW09? NIm1b41qdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> MYmyOVI2Ozl7NB?=
HT15 NUPWVpJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXvNU0zOCEQvF2= MmfJOFghcA>? MV3pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MVyyOVA4OTBzOB?=
DLD1 NVT3WJEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFf4eo0yNTJyIN88US=> NH2zVIg1QCCq NUDIUndKcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MlvENlUxPzFyMUi=
HT-29 M4XWXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLrTmJKOS1{MDFOwG0> NYfsbIc3PDhiaB?= MnKzbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M1O5S|I2ODdzMEG4
Hct-116 Mme1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWGxMVIxKM7:TR?= MnezOFghcA>? MWfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NYq0fJI3OjVyN{GwNVg>
HT15 NXT5[mhvSXCxcITvd4l{KEG|c3H5 M1jzV|EuOTBizszN MlPZOFghcA>? NHfQPHJqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NUjQfpBnOjVyN{GwNVg>
DLD1 MXzBdI9xfG:|aYOgRZN{[Xl? M2XBOFEuOTBizszN NFvTWpA1QCCq NUCxW2Y2cW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGH1e48zPTB5MUCxPC=>
HT-29 M3;5VGFxd3C2b4Ppd{BCe3OjeR?= MUmxMVExKM7:TR?= NIjGRYE1QCCq NFHKRW9qdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHO4T|AzPTB5MUCxPC=>
Hct-116 M1LzcWFxd3C2b4Ppd{BCe3OjeR?= M17vPFEuOTBizszN MVO0PEBp MXXpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MXOyOVA4OTBzOB?=
GBM5 NGHkNI5CeG:ydH;zbZMhSXO|YYm= NXPGNFFYOC534pETNU4x6oDLzszN M1TaRlI1KGh? NWi0R3NtTE2VTx?= MmTNbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo NHXpbmkzPDlzMUKxOS=>
GBM6 MYjBdI9xfG:|aYOgRZN{[Xl? MlrpNE426oDVMT6w5qCK|ryP NV7PNFF1OjRiaB?= NGK5VWJFVVOR NVjNdI9ocW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp Mn3TNlQ6OTF{MUW=
GBM12 MlvWRZBweHSxc3nzJGF{e2G7 MmfBNE426oDVMT6w5qCK|ryP NE\YVpczPCCq NUXneZRHTE2VTx?= NI\SWWZqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> NFfkdFYzPDlzMUKxOS=>
GBM14  NIrCPJBCeG:ydH;zbZMhSXO|YYm= NE\t[JcxNjYkgKOxMlDjiIoQvF2= MnHoNlQhcA>? NGDUeXdFVVOR MnTLbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo NGHqc4czPDlzMUKxOS=>
Hep3B M1T6PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjUNgKBmzJwNdMg{txO NUPjVYEzOjRxNEivO|IhcA>? NH3UPXJqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MlnINlQ5QDV6OUC=
PLC/PRF/5  MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LqcFHjiJN{LkZCpO69VQ>? MoPmNlQwPDhxN{KgbC=> NULIUG5ScW6qaXLpeJMh[2WubDDndo94fGh? M1;HcFI1QDh3OEmw
HepG2  NF\xbmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13qT|HjiJN{LkZCpO69VQ>? MkHZNlQwPDhxN{KgbC=> MkfMbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NIDQXVgzPDh6NUi5NC=>
HCT116  M3LpWmZ2dmO2aX;uJGF{e2G7 NYXiN|VOOTBxMkCvOFAh|ryP MXOyOEBp M13pUIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDtVm5CKGW6cILld5Nqd25iaX6gZUBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgcYFvdmW{ Mn3pNlQ4PjN4MUG=
Lim2405 NFnXfYNHfW6ldHnvckBCe3OjeR?= NVvvcmVuPDBizszN NIXjc5QzPCCq NVz2PIlVcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NHLZWGQzPDd4M{[xNS=>
LoVo NYfIVlg5TnWwY4Tpc44hSXO|YYm= MlfPOFAh|ryP MWqyOEBp MlTIbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NYT5[IFzOjR5NkO2NVE>
Lim1215 NV\OW49CTnWwY4Tpc44hSXO|YYm= MnvrOFAh|ryP MWOyOEBp M4fOOIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NHywNpMzPDd4M{[xNS=>
SW48 M3j2SWZ2dmO2aX;uJGF{e2G7 M3;hTFQxKM7:TR?= M3nGNVI1KGh? Mk\tbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NWTFfmFWOjR5NkO2NVE>
RKO  MmrOSpVv[3Srb36gRZN{[Xl? MWm0NEDPxE1? MVeyOEBp MXHpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NXLBR4h6OjR5NkO2NVE>
SW837 MW\GeY5kfGmxbjDBd5NigQ>? NEDTdnQ1OCEQvF2= MoTmNlQhcA>? M3r0NYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? MXuyOFc3OzZzMR?=
SW1463 NIfZNZZHfW6ldHnvckBCe3OjeR?= NUC4bVhIPDBizszN M2XIRVI1KGh? M2f1bIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M4m5Z|I1PzZ|NkGx
SW480 MlLISpVv[3Srb36gRZN{[Xl? MWi0NEDPxE1? M4DW[|I1KGh? NWnrNXRmcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M1TsbVI1PzZ|NkGx
Vaco432 NGn5PFJHfW6ldHnvckBCe3OjeR?= MkXoOFAh|ryP M{TLR|I1KGh? NYDLZm5qcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NULhOnk2OjR5NkO2NVE>
Vaco400 NFLX[IhHfW6ldHnvckBCe3OjeR?= MlXMOFAh|ryP MX6yOEBp NIi4Sm1qdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MVeyOFc3OzZzMR?=
DLD1 Mnq0SpVv[3Srb36gRZN{[Xl? MnrLOFAh|ryP M1TxVlI1KGh? MlPzbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NF\rZ2QzPDd4M{[xNS=>
HT29  NWX4XHNDTnWwY4Tpc44hSXO|YYm= MVy0NEDPxE1? NUnHcmpVOjRiaB?= NFfJ[IpqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M4DmclI1PzZ|NkGx
PLC/PRF/5  NIToR|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17FdlHjiJN3wsXN M1n0SVI1NzR6L{eyJIg> NUGyUVZscW6qaXLpeJMh[2WubDDndo94fGh? M1mxVVI{OTZ7MUS4
HepG2 MkHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVqx5qCUPcL3TR?= MmPwNlQwPDhxN{KgbC=> M1vPfYlvcGmkaYTzJINmdGxiZ4Lve5Rp MnzpNlMyPjlzNEi=
Hep3B  NEXmRmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjXSGwy6oDVNdM1US=> Ml3rNlQwPDhxN{KgbC=> MmD0bY5pcWKrdIOgZ4VtdCCpcn;3eIg> MX:yN|E3QTF2OB?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
PUMA / p53; 

PubMed: 24763611     


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     


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     


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     


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     


Changes in cell cycle and/or apoptosis‐related molecules.

p-STAT3 / STAT3 / PARP / Caspase-9; 

PubMed: 25071018     


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     


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     


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     


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     


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]

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)

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)

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

分子量 482.82
化学式

C21H15ClF4N4O3

CAS号 755037-03-7
储存条件 粉状
溶于溶剂
别名 Fluoro-Sorafenib

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 ul 动物数量
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

计算器

摩尔浓度计算器

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、MSDS / 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

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、MSDS / 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

  • 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

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

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

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04476329 Not yet recruiting Drug: Regorafenib 40 MG Hepatocellular Carcinoma SC Liver Research Consortium LLC|Bayer August 2020 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。

  • * 必填项

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

相关VEGFR产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID