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，RET和Raf-1，在无细胞试验中IC50分别是13 nM，4.2 nM，46 nM，22 nM，7 nM，1.5 nM和2.5 nM。

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客户使用Selleck该产品发表文献16篇：

客户使用该产品的3个实验数据：

  • Hepatoma cells 24 h after plating were treated with vehicle (DMSO), regorafenib (REGO, 0.5 µM), PDE5 inhibitor (sildenafil, 2 µM); or the drugs in combination. 24 hours after treatment cells were isolated and viability determined by trypan blue (n=3, SEM). *P 0.05

    J Cell Physiol, 2015, 230(9): 2281-98. Regorafenib (BAY 73-4506) purchased from Selleck.

    regorafenib induced apoptosis-related signals in HCC cell lines

    Clin Cancer Res, 2014, 20(22):5768-76. Regorafenib (BAY 73-4506) purchased from Selleck.

  • Cytotoxic effects of regorafenib in vitro on PDAC cell lines. Analysis of cell viability (high cell viability corresponds to high OD measured photometrically) after 72-h incubation with 2 μM regorafenib or with a vehicle control (0.2% DMSO) (co). The data of five independent experiments are presented with SE and analyzed with the unpaired two-tailed t test, *p < 0.05, **p < 0.01, and ***p < 0.001.

    Naunyn Schmiedebergs Arch Pharmacol, 2017, 390(11):1125-1134. Regorafenib (BAY 73-4506) purchased from Selleck.

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，RET和Raf-1，在无细胞试验中IC50分别是13 nM，4.2 nM，46 nM，22 nM，7 nM，1.5 nM和2.5 nM。
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 MXvBdI9xfG:|aYOgRZN{[Xl? NELNSGUy6oDVNdMg{txO MorIOFghcA>? NUjDXGkycW6qaXLpeJMh[2WubDDndo94fGh? NXTFO4ZXOjZ|Mkm2NFg>
PLC/PRF/5  MWnBdI9xfG:|aYOgRZN{[Xl? NFHVdIUy6oDVNdMg{txO MXu0PEBp Ml[xbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NF3X[24zPjN{OU[wPC=>
HepG2  NFr6d4lCeG:ydH;zbZMhSXO|YYm= M3v4SVHjiJN3wrFOwG0> NHrPfmo1QCCq MUjpcohq[mm2czDj[YxtKGe{b4f0bC=> MlKzNlY{Ojl4MEi=
HEK293 MXPGeY5kfGmxbjDBd5NigQ>? MmHrNE426oDLzszN NVLvVVVCOi92L{[gbC=> NX;CVlcxemWmdXPld{BIWlB5ODDlfJBz\XO|aX;u MUKyOVg2QDB|Mh?=
GEO MmCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml72NE4xOS1{MDFOwG0> NWCxSnp5QTZiaB?= M{f5RmROW09? NYjwW5hwcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MX[yOVg{QDN7MR?=
SW48 MlW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFW2[pgxNjBzLUKwJO69VQ>? MlHsPVYhcA>? NVnGbW1vTE2VTx?= MnPNbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NFq2WYwzPTh|OEO5NS=>
HT29 M4C3e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDIO4JCOC5yMT2yNEDPxE1? Ml;5PVYhcA>? Mny2SG1UVw>? NEnqUJpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NXTVVGN6OjV6M{izPVE>
SW480 MkPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7ZNE4xOS1{MDFOwG0> M2rSXFk3KGh? MVjEUXNQ MUHpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NIDEWm8zPTh|OEO5NS=>
SW620 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLXV5AxNjBzLUKwJO69VQ>? MorUPVYhcA>? NI\pTFVFVVOR NY\LbINxcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NUHFSY41OjV6M{izPVE>
HCT116 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVr6ZXVWOC5yMT2yNEDPxE1? NIHmSpA6PiCq MVLEUXNQ NVHn[FFmcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M3fE[FI2QDN6M{mx
LOVO NGLld3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPPXFJIOC5yMT2yNEDPxE1? NVrLO2lVQTZiaB?= M2HjeWROW09? MoT4bY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NVPQRplnOjV6M{izPVE>
HCT150 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnHJNE4xOS1{MDFOwG0> MWO5OkBp M37jPWROW09? MlnhbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NHjqdoMzPTh|OEO5NS=>
SW48-CR MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NISwcIkxNjBzLUKwJO69VQ>? MnjlPVYhcA>? MWXEUXNQ NV7WT|BHcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M4WyUlI2QDN6M{mx
GEO-CR Mmj1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:wMlAyNTJyIN88US=> MX65OkBp MmHrSG1UVw>? NFW1PG5qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MUGyOVg{QDN7MR?=
KB-31 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\xW|dRUUN3ME21MlXDuTBwMzDuUS=> MVeyOVc2OzN4MR?=
KB-G2 NYrNdHBYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFj3WJRKSzVyPUmuNeKyOC5zIH7N NGjDWWczPTd3M{O2NS=>
LLC-PK1 M{T6c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrQclA{UUN3ME20Nk4xyrF|LkKgcm0> M3HabFI2PzV|M{[x
LLC-PK1/MRP2 MlG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmCwTWM2OD16Mj60xtEzNjdibl2= NUe3NWxjOjV5NUOzOlE>
HEK293 M{Xwc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\yN2lEPTB;MUGuNOKyOS5{IH7N MknmNlU4PTN|NkG=
HEK293/OATP1B1 M4XBXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTZwMtMxNE4{KG6P NFrPc3czPTd3M{O2NS=>
HROC18 MmD1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDOTWM2OD1zLkOg{txO MVKyOVMxQTlzNB?=
HROC24 NV7t[VZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnpdlR3UUN3ME20MlYh|ryP NXnhZ3B3OjV|MEm5NVQ>
HROC43 NWTQfohPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXVSY1NUUN3ME21MlMh|ryP NH6wfmgzPTNyOUmxOC=>
HROC46 NGHleGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTJwNDFOwG0> NFjzemkzPTNyOUmxOC=>
RJ345 MmHKSpVv[3Srb36gRZN{[Xl? MVOwMlUwPSEQvF2= MWKyOEBp MWXEUXNQ NFvG[FBqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> NWDITmE2OjV{NUO5PVQ>
RJ348 NF2weXFHfW6ldHnvckBCe3OjeR?= MV[wMlUwPSEQvF2= NFvWZ2MzPCCq NXXPe|MyTE2VTx?= MWrpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= M37y[lI2OjV|OUm0
MCF-7 M2fZWmZ2dmO2aX;uJGF{e2G7 MkfaNE42NzVizszN M3i5dlI1KGh? NXywOpprTE2VTx?= M2LYcolvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> NH3vRVIzPTJ3M{m5OC=>
MDA-MB-231 NV\nVnRVTnWwY4Tpc44hSXO|YYm= Mm\GNE42NzVizszN M3nV[|I1KGh? M1XiPWROW09? MVPpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= MWmyOVI2Ozl7NB?=
HT15 MmfFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHuZVMyNTJyIN88US=> Mor5OFghcA>? NYTmZY5OcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NUK2SWZqOjVyN{GwNVg>
DLD1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXHW4N[OS1{MDFOwG0> MYG0PEBp MnnabY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NW[1bWUxOjVyN{GwNVg>
HT-29 NXzLUZFzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2mxW|EuOjBizszN Mk\mOFghcA>? M{m3UYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4fDe|I2ODdzMEG4
Hct-116 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rmbFEuOjBizszN M{T1eVQ5KGh? NXLoOHNScW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NXrrVlhCOjVyN{GwNVg>
HT15 NHnFbphCeG:ydH;zbZMhSXO|YYm= M2j1cFEuOTBizszN M{\PO|Q5KGh? MoOybY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MnmwNlUxPzFyMUi=
DLD1 NF\NXGVCeG:ydH;zbZMhSXO|YYm= NIrTZlAyNTFyIN88US=> NE\1ZnM1QCCq M4HTcYlv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MV:yOVA4OTBzOB?=
HT-29 MmHwRZBweHSxc3nzJGF{e2G7 NWPISY5ROS1zMDFOwG0> MVS0PEBp NGfTcYdqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NXHRTXVEOjVyN{GwNVg>
Hct-116 MUjBdI9xfG:|aYOgRZN{[Xl? NEnyZmgyNTFyIN88US=> MXS0PEBp NVf0b4t3cW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXvWemdPOjVyN{GwNVg>
GBM5 Mnj4RZBweHSxc3nzJGF{e2G7 NY\FOXpxOC534pETNU4x6oDLzszN MnPFNlQhcA>? MUnEUXNQ NUPlbIpLcW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp MUeyOFkyOTJzNR?=
GBM6 M4TpUmFxd3C2b4Ppd{BCe3OjeR?= MlzUNE426oDVMT6w5qCK|ryP MXyyOEBp MXvEUXNQ MnjsbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo M4POWVI1QTFzMkG1
GBM12 MmH6RZBweHSxc3nzJGF{e2G7 MXywMlXjiJNzLkFihKnPxE1? NWPpWotCOjRiaB?= M2fHOGROW09? M2\LOIlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> MWiyOFkyOTJzNR?=
GBM14  Mn7JRZBweHSxc3nzJGF{e2G7 MlLjNE426oDVMT6w5qCK|ryP NU\BPFI2OjRiaB?= NVPnTItSTE2VTx?= M1vodYlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> NHvP[WYzPDlzMUKxOS=>
Hep3B NGDxXZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLPNgKBmzJwNdMg{txO MWqyOE81QC95MjDo Mn7kbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MmH6NlQ5QDV6OUC=
PLC/PRF/5  M1rGVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL2PYxNOeLCk{KuOeKh|ryP NYj6NYxMOjRxNEivO|IhcA>? NULmSG9ucW6qaXLpeJMh[2WubDDndo94fGh? MmLONlQ5QDV6OUC=
HepG2  NWey[pZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWqx5qCUOi53wrFOwG0> NYP0ZnRSOjRxNEivO|IhcA>? M4HwUYlvcGmkaYTzJINmdGxiZ4Lve5Rp MYiyOFg5PTh7MB?=
HCT116  M17WZWZ2dmO2aX;uJGF{e2G7 MoS2NVAwOjBxNECg{txO NFnqXpQzPCCq NEP5VlhqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgcXJPSSCneIDy[ZN{cW:wIHnuJIEh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JI1idm6nch?= M3jpdVI1PzZ|NkGx
Lim2405 MWrGeY5kfGmxbjDBd5NigQ>? MWK0NEDPxE1? MVOyOEBp NEf3coVqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MoLGNlQ4PjN4MUG=
LoVo MXzGeY5kfGmxbjDBd5NigQ>? NVHU[IpFPDBizszN Mnf1NlQhcA>? NV3NU2pGcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MlL3NlQ4PjN4MUG=
Lim1215 M3zmPGZ2dmO2aX;uJGF{e2G7 NVSzbo9wPDBizszN M1\NbVI1KGh? MYrpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MV2yOFc3OzZzMR?=
SW48 M4LYPWZ2dmO2aX;uJGF{e2G7 NXLpU4h7PDBizszN M1LVNFI1KGh? NWjSflV{cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MnS1NlQ4PjN4MUG=
RKO  MmXpSpVv[3Srb36gRZN{[Xl? MojtOFAh|ryP Mnn0NlQhcA>? M3XlUolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NWTqdmlIOjR5NkO2NVE>
SW837 NFPZe45HfW6ldHnvckBCe3OjeR?= M2X3b|QxKM7:TR?= M3q4fVI1KGh? Mnr5bY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NF7LN|EzPDd4M{[xNS=>
SW1463 M{LPN2Z2dmO2aX;uJGF{e2G7 MlTJOFAh|ryP M4i4O|I1KGh? MnHibY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MlvkNlQ4PjN4MUG=
SW480 NW\CcYt6TnWwY4Tpc44hSXO|YYm= NFHjU2M1OCEQvF2= MnLCNlQhcA>? NFnL[XdqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MkH0NlQ4PjN4MUG=
Vaco432 M4roUmZ2dmO2aX;uJGF{e2G7 NEXhWVM1OCEQvF2= MnXvNlQhcA>? M3vjPYlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NUT1b2QzOjR5NkO2NVE>
Vaco400 NGrr[oNHfW6ldHnvckBCe3OjeR?= MnvYOFAh|ryP MWGyOEBp MmqybY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NGXk[oQzPDd4M{[xNS=>
DLD1 NYjyfWdZTnWwY4Tpc44hSXO|YYm= NVS5d2VPPDBizszN MknBNlQhcA>? NH7zW|hqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MVSyOFc3OzZzMR?=
HT29  MYfGeY5kfGmxbjDBd5NigQ>? MV20NEDPxE1? MmLlNlQhcA>? NFuyPGlqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? MoW2NlQ4PjN4MUG=
PLC/PRF/5  M2Ww[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYCx5qCUPcL3TR?= M1LCc|I1NzR6L{eyJIg> MX3pcohq[mm2czDj[YxtKGe{b4f0bC=> NGOxdGwzOzF4OUG0PC=>
HepG2 NGGyZY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjCUlUy6oDVNdM1US=> MWKyOE81QC95MjDo NXnzVnlQcW6qaXLpeJMh[2WubDDndo94fGh? NH\5[ngzOzF4OUG0PC=>
Hep3B  NYXDS20xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjpVnc2OeLCk{ZCuW0> NEnpPJAzPC92OD:3NkBp Ml;EbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M2PUVFI{OTZ7MUS4

... Click to View More Cell Line Experimental Data
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。