Regorafenib (BAY 73-4506)

目录号:S1178 别名: Fluoro-Sorafenib

Regorafenib (BAY 73-4506) Chemical Structure

Molecular Weight(MW): 482.82

Regorafenib (BAY 73-4506)是一个多靶点抑制剂,作用于VEGFR1,VEGFR2,VEGFR3,PDGFR-β,Kit,RETRaf-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。

规格 价格 库存 购买数量  
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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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)是一个多靶点抑制剂,作用于VEGFR1,VEGFR2,VEGFR3,PDGFR-β,Kit,RETRaf-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。
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 MVLBdI9xfG:|aYOgRZN{[Xl? MlP4NgKBmzYEoN88US=> M2m3SVQ5KGh? M1rqe4lvcGmkaYTzJINmdGxiZ4Lve5Rp NH\IenUzPjN{OU[wPC=>
PLC/PRF/5  MYDBdI9xfG:|aYOgRZN{[Xl? M2\lNVHjiJN3wrFOwG0> Ml;1OFghcA>? NUnablJDcW6qaXLpeJMh[2WubDDndo94fGh? M1HRVVI3OzJ7NkC4
HepG2  NGnjN3JCeG:ydH;zbZMhSXO|YYm= MnLiNgKBmzYEoN88US=> NXSxZlVsPDhiaB?= M2XWTIlvcGmkaYTzJINmdGxiZ4Lve5Rp MYiyOlMzQTZyOB?=
HEK293 NGjrenpHfW6ldHnvckBCe3OjeR?= MX:wMlXjiIoQvF2= NF\aUGgzNzRxNjDo M2fK[JJm\HWlZYOgS3JRPzhiZYjwdoV{e2mxbh?= NHPXVlQzPTh3OECzNi=>
GEO NX:4e2xoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DOcVAvODFvMkCg{txO NYnlZWlQQTZiaB?= M1zae2ROW09? M4rZXolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MYSyOVg{QDN7MR?=
SW48 MnrPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULDSm5tOC5yMT2yNEDPxE1? M4mxdFk3KGh? NIfOWYRFVVOR M{L2PIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MUWyOVg{QDN7MR?=
HT29 NEi3dohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfHb5l2OC5yMT2yNEDPxE1? M1K3XFk3KGh? M1vrSGROW09? NVrHRVRycW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MlXiNlU5Ozh|OUG=
SW480 NI\kO4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfMWW9ROC5yMT2yNEDPxE1? MWO5OkBp MnzsSG1UVw>? M3nQS4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWTWb29POjV6M{izPVE>
SW620 NX\ZSYw{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\uO2wxNjBzLUKwJO69VQ>? NXTZXZo{QTZiaB?= M2TUXWROW09? M2HkdIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVzzUHA6OjV6M{izPVE>
HCT116 MmTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlj6NE4xOS1{MDFOwG0> MWS5OkBp MlPoSG1UVw>? NHrnVmFqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MViyOVg{QDN7MR?=
LOVO M2nqOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvod2MxNjBzLUKwJO69VQ>? M3XoZVk3KGh? MV7EUXNQ NGW4[HRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MVWyOVg{QDN7MR?=
HCT150 M4\kRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLrNE4xOS1{MDFOwG0> NFqyUYQ6PiCq NEXqcZNFVVOR MkftbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MXqyOVg{QDN7MR?=
SW48-CR NEG2[lJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVz4bIJFOC5yMT2yNEDPxE1? NUf1S5JRQTZiaB?= M4m3bWROW09? MmTCbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M1\Q[VI2QDN6M{mx
GEO-CR M4XsZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPVNE4xOS1{MDFOwG0> NHXmUGc6PiCq M4rIc2ROW09? MX7pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NV\rVZNMOjV6M{izPVE>
KB-31 NW\XS241T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPMWHZKSzVyPUWuOeKyOC5|IH7N NGrhO20zPTd3M{O2NS=>
KB-G2 M17T[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PvTWlEPTB;OT6xxtExNjFibl2= MXKyOVc2OzN4MR?=
LLC-PK1 NHTGd3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;vUWR2UUN3ME20Nk4xyrF|LkKgcm0> M4nTZ|I2PzV|M{[x
LLC-PK1/MRP2 MmfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTh{LkVCtVIvPyCwTR?= Mn;ZNlU4PTN|NkG=
HEK293 MkTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTFzLkFCtVEvOiCwTR?= MYKyOVc2OzN4MR?=
HEK293/OATP1B1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXr6OnRqUUN3ME22MlLDuTBwMzDuUS=> MlTmNlU4PTN|NkG=
HROC18 NUe2Z414T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXBTGJKSzVyPUGuN{DPxE1? MmK4NlU{ODl7MUS=
HROC24 NFnT[lZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrxVZNEUUN3ME20MlYh|ryP NFvpOogzPTNyOUmxOC=>
HROC43 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTVwMzFOwG0> NXjSNXhkOjV|MEm5NVQ>
HROC46 NXrQe|h1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzPTWM2OD1{LkSg{txO NHv0RWszPTNyOUmxOC=>
RJ345 MWXGeY5kfGmxbjDBd5NigQ>? M1vUeVAvPS93IN88US=> MUmyOEBp M1zqUmROW09? MnfDbY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u M4TURlI2OjV|OUm0
RJ348 MoLJSpVv[3Srb36gRZN{[Xl? M{\zclAvPS93IN88US=> NGfteWEzPCCq NGrnR5FFVVOR M2nCR4lvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> MkjyNlUzPTN7OUS=
MCF-7 MlP6SpVv[3Srb36gRZN{[Xl? NWf2UnV[OC53L{Wg{txO MorQNlQhcA>? MWLEUXNQ Mn7ibY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u MnXJNlUzPTN7OUS=
MDA-MB-231 MX3GeY5kfGmxbjDBd5NigQ>? MVGwMlUwPSEQvF2= MlTmNlQhcA>? M{fMcmROW09? NVnpfHlucW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v MkD1NlUzPTN7OUS=
HT15 NH\WWWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXHPXQ4OS1{MDFOwG0> NGnRR4Y1QCCq MYPpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NHPHVFUzPTB5MUCxPC=>
DLD1 NYC1b29KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TDWFEuOjBizszN Mon3OFghcA>? M2jLSYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Mn\NNlUxPzFyMUi=
HT-29 MnPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYK3WFNOOS1{MDFOwG0> Mn;FOFghcA>? M37I[IlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGnVbm0zPTB5MUCxPC=>
Hct-116 NFXSNlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NES3fVcyNTJyIN88US=> MW[0PEBp MlG4bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NUjrbZdMOjVyN{GwNVg>
HT15 NEXZUZpCeG:ydH;zbZMhSXO|YYm= M2PvT|EuOTBizszN M{jzZ|Q5KGh? MUnpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MkfWNlUxPzFyMUi=
DLD1 M1jBUGFxd3C2b4Ppd{BCe3OjeR?= Mn3iNU0yOCEQvF2= MojvOFghcA>? M1v4NIlv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NUDvXGlpOjVyN{GwNVg>
HT-29 NIXsTGVCeG:ydH;zbZMhSXO|YYm= MXKxMVExKM7:TR?= NUWwcoREPDhiaB?= MmjsbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M1ztb|I2ODdzMEG4
Hct-116 MYfBdI9xfG:|aYOgRZN{[Xl? NV\VPHhsOS1zMDFOwG0> M{SzVFQ5KGh? NYHMOG5lcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4HiblI2ODdzMEG4
GBM5 NXTGfpZkSXCxcITvd4l{KEG|c3H5 NF\XZmgxNjYkgKOxMlDjiIoQvF2= NIqyeokzPCCq NWjURlBrTE2VTx?= NYr4N4Z2cW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp M2LsVFI1QTFzMkG1
GBM6 M2Pl[2Fxd3C2b4Ppd{BCe3OjeR?= MXWwMlXjiJNzLkFihKnPxE1? MVuyOEBp MlfPSG1UVw>? MWrpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= NIHleoYzPDlzMUKxOS=>
GBM12 NEHWOGhCeG:ydH;zbZMhSXO|YYm= M3P1WlAvPeLCk{GuNQKBkc7:TR?= M{nieVI1KGh? M4ftU2ROW09? NYnseVNycW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp MnuxNlQ6OTF{MUW=
GBM14  Ml;CRZBweHSxc3nzJGF{e2G7 MUWwMlXjiJNzLkFihKnPxE1? Ml\oNlQhcA>? NGDMRnlFVVOR MXzpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= NFWzZoUzPDlzMUKxOS=>
Hep3B M2f5Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXexT2FJOeLCk{KuOeKh|ryP NFjNV|AzPC92OD:3NkBp NFv6WYRqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MWiyOFg5PTh7MB?=
PLC/PRF/5  MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUGx5qCUOi53wrFOwG0> MYKyOE81QC95MjDo M1LNNolvcGmkaYTzJINmdGxiZ4Lve5Rp NGj3WGszPDh6NUi5NC=>
HepG2  M2C5PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXv5UFFKOeLCk{KuOeKh|ryP MnrHNlQwPDhxN{KgbC=> MXjpcohq[mm2czDj[YxtKGe{b4f0bC=> MoHINlQ5QDV6OUC=
HCT116  MkLzSpVv[3Srb36gRZN{[Xl? NFjqeY4yOC9{MD:0NEDPxE1? M4\0OVI1KGh? NUnNc|Z5cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJI1TVkFiZYjwdoV{e2mxbjDpckBiKGSxc3WtJIFv\CC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NF;VbIozPDd4M{[xNS=>
Lim2405 M4PzXmZ2dmO2aX;uJGF{e2G7 NEG2XW41OCEQvF2= NUDic|lpOjRiaB?= MXzpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NEXaVnIzPDd4M{[xNS=>
LoVo MlTvSpVv[3Srb36gRZN{[Xl? NGjae401OCEQvF2= NY\0WIcxOjRiaB?= MYjpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NV3mTWpROjR5NkO2NVE>
Lim1215 MWnGeY5kfGmxbjDBd5NigQ>? NIixNZI1OCEQvF2= M3z0[|I1KGh? NE\OUXNqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NXPsW|IzOjR5NkO2NVE>
SW48 Ml\hSpVv[3Srb36gRZN{[Xl? M1TyV|QxKM7:TR?= MojCNlQhcA>? Mm[zbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MoHqNlQ4PjN4MUG=
RKO  MYDGeY5kfGmxbjDBd5NigQ>? M1WxOlQxKM7:TR?= M{\wclI1KGh? NXSyZVFPcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MUiyOFc3OzZzMR?=
SW837 M4r2NGZ2dmO2aX;uJGF{e2G7 NIn2WXY1OCEQvF2= M1uxXFI1KGh? NYG3[G1rcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M{H4XVI1PzZ|NkGx
SW1463 MlnUSpVv[3Srb36gRZN{[Xl? Ml7GOFAh|ryP NHzDPY0zPCCq MkTzbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NUjwToxtOjR5NkO2NVE>
SW480 NHjEbVFHfW6ldHnvckBCe3OjeR?= MUS0NEDPxE1? NHzQPJYzPCCq MVjpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NV;SXodMOjR5NkO2NVE>
Vaco432 MXrGeY5kfGmxbjDBd5NigQ>? MmPVOFAh|ryP MViyOEBp MYfpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NHSzRnczPDd4M{[xNS=>
Vaco400 MnO1SpVv[3Srb36gRZN{[Xl? M{LuR|QxKM7:TR?= NUC0NYxiOjRiaB?= M{mzTolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NV7nXlZCOjR5NkO2NVE>
DLD1 MUPGeY5kfGmxbjDBd5NigQ>? Mk\aOFAh|ryP NXLxT2FbOjRiaB?= NVHTe2tKcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MnHSNlQ4PjN4MUG=
HT29  NWOzW4RXTnWwY4Tpc44hSXO|YYm= MmnVOFAh|ryP M2HJUVI1KGh? Mn60bY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NFzyc2czPDd4M{[xNS=>
PLC/PRF/5  NVfBc2tGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjn[W0y6oDVNdM1US=> M4PGUFI1NzR6L{eyJIg> NXG4R|JkcW6qaXLpeJMh[2WubDDndo94fGh? M4L6S|I{OTZ7MUS4
HepG2 NU\EVWRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILS[3Ay6oDVNdM1US=> NXvIVFVsOjRxNEivO|IhcA>? M4e3N4lvcGmkaYTzJINmdGxiZ4Lve5Rp MXWyN|E3QTF2OB?=
Hep3B  NWfXOllzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTQNgKBmzYEtV2= M4DmZlI1NzR6L{eyJIg> NYf4OlZXcW6qaXLpeJMh[2WubDDndo94fGh? NXPSO29nOjNzNkmxOFg>

... 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]
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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]
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  • 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]
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  • 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
  • Formulation: 聚乙二醇400/125 mM 甲磺酸水溶液 (80/20) 或者聚丙烯 乙二醇/聚乙二醇400/Pluronic F68 (42.5/42.5/15 + 20% 水溶液)
  • 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 powder
in solvent
别名 Fluoro-Sorafenib

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 (g) = 浓度 (mol/L) x 体积 (L) 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 Conditions Sponsor/Collaborators Start Date Phases
NCT03829852 Not yet recruiting Metastatic Colorectal Cancer Taipei Veterans General Hospital Taiwan|Chang Gung Memorial Hospital March 1 2019 --
NCT03829852 Not yet recruiting Metastatic Colorectal Cancer Taipei Veterans General Hospital Taiwan|Chang Gung Memorial Hospital March 1 2019 --
NCT03829462 Not yet recruiting Metastatic Colorectal Cancer (mCRC) Institut du Cancer de Montpellier - Val d''Aurelle February 2019 Phase 3
NCT03880877 Recruiting Metastatic Colorectal Cancer Kaohsiung Medical University Chung-Ho Memorial Hospital February 26 2019 Phase 2
NCT03657641 Not yet recruiting Colorectal Cancer|Colorectal Cancer Metastatic University of Southern California|National Cancer Institute (NCI) February 25 2019 Phase 1|Phase 2
NCT03644511 Recruiting Hepatocellular Carcinoma Bayer February 28 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID