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。

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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,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 MkWwRZBweHSxc3nzJGF{e2G7 M{f4PVHjiJN3wrFOwG0> M162ZlQ5KGh? MXvpcohq[mm2czDj[YxtKGe{b4f0bC=> NX7GeZptOjZ|Mkm2NFg>
PLC/PRF/5  M{TUUmFxd3C2b4Ppd{BCe3OjeR?= M3\XTVHjiJN3wrFOwG0> MX[0PEBp NHvR[5dqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MoXONlY{Ojl4MEi=
HepG2  MYTBdI9xfG:|aYOgRZN{[Xl? M1KyS|HjiJN3wrFOwG0> NYfuWm52PDhiaB?= Mle2bY5pcWKrdIOgZ4VtdCCpcn;3eIg> M2K4XVI3OzJ7NkC4
HEK293 Mnn3SpVv[3Srb36gRZN{[Xl? MXGwMlXjiIoQvF2= MXeyM|QwPiCq NIDubJFz\WS3Y3XzJGdTWDd6IHX4dJJme3Orb36= NGrUOWozPTh3OECzNi=>
GEO M4PZfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7TS5FZOC5yMT2yNEDPxE1? Mnr2PVYhcA>? MnTiSG1UVw>? M4TBfolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MYCyOVg{QDN7MR?=
SW48 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[wMlAyNTJyIN88US=> NV3Jb5p1QTZiaB?= MVnEUXNQ NWq4emozcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NWX6WW9TOjV6M{izPVE>
HT29 Mm\sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfmVpN2OC5yMT2yNEDPxE1? MUO5OkBp NV30[|dLTE2VTx?= NWDIS5dicW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NESzfWYzPTh|OEO5NS=>
SW480 NHOydIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DCPVAvODFvMkCg{txO MofmPVYhcA>? NYDNUVBHTE2VTx?= NFPzdIpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1nzTlI2QDN6M{mx
SW620 NVfWZ3AyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFezXZUxNjBzLUKwJO69VQ>? NYP6N|lHQTZiaB?= NV7RR49STE2VTx?= MWfpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MXWyOVg{QDN7MR?=
HCT116 MljUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYmwMlAyNTJyIN88US=> MnjEPVYhcA>? NYXDWpZpTE2VTx?= M2K5RolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M{\PUFI2QDN6M{mx
LOVO M321Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDEOnkxNjBzLUKwJO69VQ>? NVvvZWpKQTZiaB?= NV3GNFZnTE2VTx?= M{THT4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NFrVTYozPTh|OEO5NS=>
HCT150 NU\pWJQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVGwMlAyNTJyIN88US=> M3PXOlk3KGh? NUnnc2RmTE2VTx?= NWL2UWk{cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Mny4NlU5Ozh|OUG=
SW48-CR MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjOeI46OC5yMT2yNEDPxE1? NUX4UlF3QTZiaB?= MXrEUXNQ Ml\qbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NVTjPXVbOjV6M{izPVE>
GEO-CR M4LKOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfJ[HgxNjBzLUKwJO69VQ>? MWO5OkBp M2\NfGROW09? MlrIbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MoTkNlU5Ozh|OUG=
KB-31 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfUTWM2OD13LkZCtVAvOyCwTR?= NInwe28zPTd3M{O2NS=>
KB-G2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;DeWlEPTB;OT6xxtExNjFibl2= M2rwW|I2PzV|M{[x
LLC-PK1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7qc4JKSzVyPUSyMlDDuTNwMjDuUS=> NGThR5MzPTd3M{O2NS=>
LLC-PK1/MRP2 NXjDTY1nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTh{LkVCtVIvPyCwTR?= MmnqNlU4PTN|NkG=
HEK293 M4\SNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPqWIhKSzVyPUGxMlDDuTFwMjDuUS=> MVuyOVc2OzN4MR?=
HEK293/OATP1B1 NV[yRYI2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPFTWM2OD14LkNCtVAvOyCwTR?= NYjCdHRGOjV5NUOzOlE>
HROC18 NIW0bIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTFwMzFOwG0> MV2yOVMxQTlzNB?=
HROC24 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;kR2lEPTB;ND62JO69VQ>? NXm3PWl[OjV|MEm5NVQ>
HROC43 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{T1bWlEPTB;NT6zJO69VQ>? MnPFNlU{ODl7MUS=
HROC46 NXjndGdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHpTWM2OD1{LkSg{txO NWHZZmxOOjV|MEm5NVQ>
RJ345 MUfGeY5kfGmxbjDBd5NigQ>? M1fDSVAvPS93IN88US=> MVuyOEBp MYLEUXNQ Mn7ybY5pcWKrdIOgeIhmKGOnbHygcYloemG2aX;u NUnzeVhqOjV{NUO5PVQ>
RJ348 NID0d|BHfW6ldHnvckBCe3OjeR?= MkfuNE42NzVizszN MYqyOEBp Ml74SG1UVw>? MUfpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= NX\5[md4OjV{NUO5PVQ>
MCF-7 MnTOSpVv[3Srb36gRZN{[Xl? M{PrfFAvPS93IN88US=> M4q5eVI1KGh? M3fIbmROW09? NFvKRpJqdmirYnn0d{B1cGViY3XscEBucWe{YYTpc44> NVXRT49COjV{NUO5PVQ>
MDA-MB-231 MWnGeY5kfGmxbjDBd5NigQ>? MorjNE42NzVizszN MYWyOEBp MYnEUXNQ M{TuRolvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> MlzPNlUzPTN7OUS=
HT15 M4KyNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXENU0zOCEQvF2= NFHzNoI1QCCq NXrIdJdlcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MYWyOVA4OTBzOB?=
DLD1 MnrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDOd3kyNTJyIN88US=> NVzsO|BUPDhiaB?= NXL2PHpXcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M37sclI2ODdzMEG4
HT-29 NX3xeHN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DUbVEuOjBizszN NV;QSYF2PDhiaB?= MYrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NV7YRWtxOjVyN{GwNVg>
Hct-116 NHnTfWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjlXZUyNTJyIN88US=> MmHjOFghcA>? MVrpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NIH4dI8zPTB5MUCxPC=>
HT15 Mn\JRZBweHSxc3nzJGF{e2G7 MWOxMVExKM7:TR?= M3\GSFQ5KGh? MVPpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MV:yOVA4OTBzOB?=
DLD1 Ml\tRZBweHSxc3nzJGF{e2G7 M3K0RVEuOTBizszN NVHqOodGPDhiaB?= Mm\vbY5lfWOnczDj[YxtKGSnYYToJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NGXMeG8zPTB5MUCxPC=>
HT-29 MXHBdI9xfG:|aYOgRZN{[Xl? NXLXVmFbOS1zMDFOwG0> M3z4U|Q5KGh? NXrpSHlNcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M3;pVFI2ODdzMEG4
Hct-116 MkSzRZBweHSxc3nzJGF{e2G7 M1ex[VEuOTBizszN NIjEfWk1QCCq M4PHdIlv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M2H4XFI2ODdzMEG4
GBM5 MWPBdI9xfG:|aYOgRZN{[Xl? MY[wMlXjiJNzLkFihKnPxE1? MU[yOEBp MUXEUXNQ NEXPOmhqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> M1rBT|I1QTFzMkG1
GBM6 MX\BdI9xfG:|aYOgRZN{[Xl? MXGwMlXjiJNzLkFihKnPxE1? MWOyOEBp M{C0PGROW09? NVPMfZhQcW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp NUHkXpVoOjR7MUGyNVU>
GBM12 NG[4bFVCeG:ydH;zbZMhSXO|YYm= MmfDNE426oDVMT6w5qCK|ryP M1POOVI1KGh? M3zDNmROW09? MojJbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo NGT3T|UzPDlzMUKxOS=>
GBM14  MV\BdI9xfG:|aYOgRZN{[Xl? MWWwMlXjiJNzLkFihKnPxE1? NVTveVRCOjRiaB?= M2fMd2ROW09? MYjpcpRmemGldIOge4l1cCCuYYDheIlvcWJidH:gbY5lfWOnIHPlcIwh\GWjdHi= NVTFOZFIOjR7MUGyNVU>
Hep3B NVK3coh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDSNgKBmzJwNdMg{txO NGLGdoMzPC92OD:3NkBp NH7hRo1qdmirYnn0d{Bk\WyuIHfyc5d1cA>? MoDLNlQ5QDV6OUC=
PLC/PRF/5  NG\hS29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGGzUZYy6oDVMj61xsDPxE1? MUiyOE81QC95MjDo MXHpcohq[mm2czDj[YxtKGe{b4f0bC=> NH;nc24zPDh6NUi5NC=>
HepG2  MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;aTlHjiJN{LkZCpO69VQ>? MmTxNlQwPDhxN{KgbC=> M3XUNolvcGmkaYTzJINmdGxiZ4Lve5Rp M2H4[|I1QDh3OEmw
HCT116  M4nXV2Z2dmO2aX;uJGF{e2G7 NXvvbphIOTBxMkCvOFAh|ryP M1LLSFI1KGh? MVLpcoR2[2W|IGDVUWEheHKxdHXpckBidmRibWLORUBmgHC{ZYPzbY9vKGmwIHGg[I9{\S1iYX7kJJRqdWVvZHXw[Y5l\W62IH3hco5meg>? Ml7tNlQ4PjN4MUG=
Lim2405 NWG0UXFzTnWwY4Tpc44hSXO|YYm= NVnGXWxCPDBizszN MlTXNlQhcA>? MoXKbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NX31[HMzOjR5NkO2NVE>
LoVo M3q2UmZ2dmO2aX;uJGF{e2G7 MUK0NEDPxE1? NHfIT3ozPCCq MYDpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NIPJPGMzPDd4M{[xNS=>
Lim1215 MnPlSpVv[3Srb36gRZN{[Xl? NU\TS3hjPDBizszN M3\wS|I1KGh? NXzOR45xcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| NXr3enJSOjR5NkO2NVE>
SW48 MnWwSpVv[3Srb36gRZN{[Xl? MWi0NEDPxE1? MnjxNlQhcA>? MVvpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MknXNlQ4PjN4MUG=
RKO  NIm4ZXpHfW6ldHnvckBCe3OjeR?= MmLYOFAh|ryP NUWwTJJHOjRiaB?= Mn3UbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NFvXeY0zPDd4M{[xNS=>
SW837 MkD1SpVv[3Srb36gRZN{[Xl? NH;PdI81OCEQvF2= MXOyOEBp Ml7QbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MWiyOFc3OzZzMR?=
SW1463 NHXYbGZHfW6ldHnvckBCe3OjeR?= MmfXOFAh|ryP M1TXOFI1KGh? Ml\WbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ MlnXNlQ4PjN4MUG=
SW480 NIDyZmFHfW6ldHnvckBCe3OjeR?= MljBOFAh|ryP M4jFeFI1KGh? NVX2N2dTcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MkLSNlQ4PjN4MUG=
Vaco432 M2DxdmZ2dmO2aX;uJGF{e2G7 MVu0NEDPxE1? MmXFNlQhcA>? NHfCR|lqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? NIPxOVEzPDd4M{[xNS=>
Vaco400 NGPaN5ZHfW6ldHnvckBCe3OjeR?= NUDoXIk2PDBizszN NHjKS4ozPCCq M{LOT4lv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M1G4[VI1PzZ|NkGx
DLD1 NWTqcHF3TnWwY4Tpc44hSXO|YYm= NVnuNIR6PDBizszN Mnn5NlQhcA>? Mo\LbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ NWW5e4d4OjR5NkO2NVE>
HT29  MY\GeY5kfGmxbjDBd5NigQ>? NXGxb3pxPDBizszN NET3W|kzPCCq MUfpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> M{TiOFI1PzZ|NkGx
PLC/PRF/5  NWPVdII4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M16w[FHjiJN3wsXN M4rCZVI1NzR6L{eyJIg> NFSxfnNqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M2\DbFI{OTZ7MUS4
HepG2 MoL2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXex5qCUPcL3TR?= MXqyOE81QC95MjDo MVnpcohq[mm2czDj[YxtKGe{b4f0bC=> NXLKWItpOjNzNkmxOFg>
Hep3B  MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDhNnBsOeLCk{ZCuW0> NGrje5EzPC92OD:3NkBp NGLLXpRqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M3HRZ|I{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]
+ 展开
  • 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
稳定性 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