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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RMB 1375.55 现货
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RMB 1733.78 现货
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RMB 7954.71 现货
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客户使用该产品的2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.

    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 MU\BdI9xfG:|aYOgRZN{[Xl? MX[x5qCUPcLizszN MoH4OFghcA>? MX\pcohq[mm2czDj[YxtKGe{b4f0bC=> M1Lxb|I3OzJ7NkC4
PLC/PRF/5  MWnBdI9xfG:|aYOgRZN{[Xl? NGLR[|Iy6oDVNdMg{txO MXG0PEBp NUfkfWc1cW6qaXLpeJMh[2WubDDndo94fGh? NWPzcW01OjZ|Mkm2NFg>
HepG2  NXTueFJ{SXCxcITvd4l{KEG|c3H5 Ml\PNgKBmzYEoN88US=> M{n4bVQ5KGh? M1z6VolvcGmkaYTzJINmdGxiZ4Lve5Rp NH;RWYszPjN{OU[wPC=>
HEK293 NF3VTnlHfW6ldHnvckBCe3OjeR?= NV\sZoVtOC534pEJ{txO M{TObFIwPC94IHi= MWny[YR2[2W|IFfSVFc5KGW6cILld5Nqd25? NXT2doVZOjV6NUiwN|I>
GEO NHLtNm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3zNE4xOS1{MDFOwG0> M2r3dVk3KGh? NEDrR4hFVVOR NGWyRYhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M{XjelI2QDN6M{mx
SW48 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWWwMlAyNTJyIN88US=> M1jQRVk3KGh? M{j0dmROW09? MX7pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MV:yOVg{QDN7MR?=
HT29 M1LVSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGm2XZYxNjBzLUKwJO69VQ>? M1f0flk3KGh? NEnzc4RFVVOR M3HyZ4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHPhbWozPTh|OEO5NS=>
SW480 MmnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\MNE4xOS1{MDFOwG0> MUK5OkBp NEfNRYhFVVOR NIe2V25qdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M1PiV|I2QDN6M{mx
SW620 MlzGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVuwMlAyNTJyIN88US=> MoLRPVYhcA>? NW[3OJhRTE2VTx?= NHyzZ3hqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NGLJ[oIzPTh|OEO5NS=>
HCT116 NHTSeplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLIemwxNjBzLUKwJO69VQ>? NUPyXoVWQTZiaB?= MkP4SG1UVw>? NVHrc4NjcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MXyyOVg{QDN7MR?=
LOVO MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;yPWpsOC5yMT2yNEDPxE1? NH;r[Yc6PiCq MXfEUXNQ Mn7DbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NX24UotPOjV6M{izPVE>
HCT150 M2TSdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWqwMlAyNTJyIN88US=> MV:5OkBp MV3EUXNQ NHzWTFhqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? MnLzNlU5Ozh|OUG=
SW48-CR NIj4bIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjCcpoxNjBzLUKwJO69VQ>? NIrKOYg6PiCq MUDEUXNQ M{jWVolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NXi3RnpqOjV6M{izPVE>
GEO-CR M2izbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoriNE4xOS1{MDFOwG0> MXe5OkBp NFLNVpVFVVOR MX\pcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NXHYWWJwOjV6M{izPVE>
KB-31 NXzobZlVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvZc2dKSzVyPUWuOeKyOC5|IH7N MYOyOVc2OzN4MR?=
KB-G2 MlvYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPRTpJwUUN3ME25MlHDuTBwMTDuUS=> NFPOdXIzPTd3M{O2NS=>
LLC-PK1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoL6TWM2OD12Mj6wxtE{NjJibl2= MXKyOVc2OzN4MR?=
LLC-PK1/MRP2 NFTRZpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3RSmZqUUN3ME24Nk41yrF{Lkegcm0> NGHsUoozPTd3M{O2NS=>
HEK293 M4nwe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTFzLkFCtVEvOiCwTR?= M3z4blI2PzV|M{[x
HEK293/OATP1B1 NW\Nc3hUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEW5e|ZKSzVyPU[uNuKyOC5|IH7N Ml7BNlU4PTN|NkG=
HROC18 M2q5dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLBbYEzUUN3ME2xMlMh|ryP MUWyOVMxQTlzNB?=
HROC24 NHn5[|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTRwNjFOwG0> NU\NblVOOjV|MEm5NVQ>
HROC43 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\ZTWM2OD13LkOg{txO NXftdllyOjV|MEm5NVQ>
HROC46 Mk\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWr4OFdRUUN3ME2yMlQh|ryP MkfCNlU{ODl7MUS=
RJ345 Ml7mSpVv[3Srb36gRZN{[Xl? MX:wMlUwPSEQvF2= MofJNlQhcA>? MVnEUXNQ NUW1T5F{cW6qaXLpeJMhfGinIHPlcIwhdWmpcnH0bY9v M2TWb|I2OjV|OUm0
RJ348 MYfGeY5kfGmxbjDBd5NigQ>? NIfkblkxNjVxNTFOwG0> Mn\XNlQhcA>? NFvCb4tFVVOR M{TufYlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> MVqyOVI2Ozl7NB?=
MCF-7 Mk\KSpVv[3Srb36gRZN{[Xl? NFz4[4wxNjVxNTFOwG0> MlLiNlQhcA>? MlfQSG1UVw>? M3;YSolvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> NH;zSZYzPTJ3M{m5OC=>
MDA-MB-231 Mn;5SpVv[3Srb36gRZN{[Xl? MWGwMlUwPSEQvF2= NWSyXotvOjRiaB?= NVrVcVFHTE2VTx?= MUPpcohq[mm2czD0bIUh[2WubDDtbYdz[XSrb36= NYjreYV{OjV{NUO5PVQ>
HT15 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFL0RWQyNTJyIN88US=> MXq0PEBp NYDTbml6cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M4XBS|I2ODdzMEG4
DLD1 NGXEe2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LJRlEuOjBizszN NUDHRm5GPDhiaB?= MnHTbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MkLmNlUxPzFyMUi=
HT-29 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXi1WVByOS1{MDFOwG0> MYG0PEBp MmLubY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NY\0RWFtOjVyN{GwNVg>
Hct-116 M4XQUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTDNU0zOCEQvF2= MXu0PEBp NWO5UYNwcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MoXjNlUxPzFyMUi=
HT15 NFSxWYxCeG:ydH;zbZMhSXO|YYm= NUm0ZmhuOS1zMDFOwG0> M{W5c|Q5KGh? NY\mVGdHcW6mdXPld{Bk\WyuIHTlZZRpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4\mSFI2ODdzMEG4
DLD1 M3fPOGFxd3C2b4Ppd{BCe3OjeR?= NUGyTpFXOS1zMDFOwG0> MV[0PEBp M1;TSolv\HWlZYOgZ4VtdCCmZXH0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MkjmNlUxPzFyMUi=
HT-29 M1vNNmFxd3C2b4Ppd{BCe3OjeR?= NV;YXI5VOS1zMDFOwG0> Mor1OFghcA>? MUjpcoR2[2W|IHPlcIwh\GWjdHigbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NITwZXkzPTB5MUCxPC=>
Hct-116 NFLwVo5CeG:ydH;zbZMhSXO|YYm= MXmxMVExKM7:TR?= M3z1OlQ5KGh? NHrvR4JqdmS3Y3XzJINmdGxiZHXheIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M1G3WVI2ODdzMEG4
GBM5 MXrBdI9xfG:|aYOgRZN{[Xl? Moq2NE426oDVMT6w5qCK|ryP MXuyOEBp Mlz4SG1UVw>? NX:zV29icW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp NEO1VYIzPDlzMUKxOS=>
GBM6 NEPROlFCeG:ydH;zbZMhSXO|YYm= Mk\xNE426oDVMT6w5qCK|ryP MXKyOEBp NGiyT3JFVVOR MkTDbY51\XKjY4TzJJdqfGhibHHwZZRqdmmkIITvJIlv\HWlZTDj[YxtKGSnYYTo M4H1TVI1QTFzMkG1
GBM12 M3\Gc2Fxd3C2b4Ppd{BCe3OjeR?= M{XCdVAvPeLCk{GuNQKBkc7:TR?= NEDIb4kzPCCq NFHKO5BFVVOR NHLYcJdqdnSncnHjeJMhf2m2aDDsZZBifGmwaXKgeI8hcW6mdXPlJINmdGxiZHXheIg> NWG2clU1OjR7MUGyNVU>
GBM14  MWPBdI9xfG:|aYOgRZN{[Xl? NIW3fJExNjYkgKOxMlDjiIoQvF2= MVWyOEBp NXXRcmp2TE2VTx?= NX7PUIY3cW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp M4T1c|I1QTFzMkG1
Hep3B M1WxfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13XdVHjiJN{LkZCpO69VQ>? NXjS[VVIOjRxNEivO|IhcA>? MYjpcohq[mm2czDj[YxtKGe{b4f0bC=> MYCyOFg5PTh7MB?=
PLC/PRF/5  NEW5OIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV2x5qCUOi53wrFOwG0> MojqNlQwPDhxN{KgbC=> M4izSIlvcGmkaYTzJINmdGxiZ4Lve5Rp NVrmZZJwOjR6OEW4PVA>
HepG2  NWDIbJhYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml23NgKBmzJwNdMg{txO M4jPUVI1NzR6L{eyJIg> NUPaO2hFcW6qaXLpeJMh[2WubDDndo94fGh? MXeyOFg5PTh7MB?=
HCT116  M{jQUmZ2dmO2aX;uJGF{e2G7 MYWxNE8zOC92MDFOwG0> MUWyOEBp Ml\rbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIH3SUmEh\XiycnXzd4lwdiCrbjDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDtZY5v\XJ? NHr0WHEzPDd4M{[xNS=>
Lim2405 MkjZSpVv[3Srb36gRZN{[Xl? MYG0NEDPxE1? NWXreXdVOjRiaB?= NXHIe4g3cW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M2nyfVI1PzZ|NkGx
LoVo NFv2SmJHfW6ldHnvckBCe3OjeR?= MUG0NEDPxE1? MYSyOEBp M3f2bIlv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NF\OcoszPDd4M{[xNS=>
Lim1215 M13oeGZ2dmO2aX;uJGF{e2G7 MVm0NEDPxE1? MUOyOEBp MofzbY5lfWOnczDQWW1CKHC{b4TlbY4h[W6mIHPlcIwh[XCxcITvd4l{ M1ToNVI1PzZ|NkGx
SW48 MUPGeY5kfGmxbjDBd5NigQ>? NXLSVpBCPDBizszN M4TxVVI1KGh? NVjZ[|ZIcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MXiyOFc3OzZzMR?=
RKO  M3m5XWZ2dmO2aX;uJGF{e2G7 MkCxOFAh|ryP MkThNlQhcA>? M3nTbolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? M1HIOlI1PzZ|NkGx
SW837 MknJSpVv[3Srb36gRZN{[Xl? NIDuZXc1OCEQvF2= Mn\5NlQhcA>? NVTlVoRVcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| MoHmNlQ4PjN4MUG=
SW1463 MnjNSpVv[3Srb36gRZN{[Xl? M33ze|QxKM7:TR?= NEfCWoYzPCCq M4GwVolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NYO4boI2OjR5NkO2NVE>
SW480 M{faOmZ2dmO2aX;uJGF{e2G7 MWG0NEDPxE1? M4nkPVI1KGh? M1zmNolv\HWlZYOgVHVOSSCycn;0[YlvKGGwZDDj[YxtKGGyb4D0c5Nqew>? NUe3PVh3OjR5NkO2NVE>
Vaco432 NIP6colHfW6ldHnvckBCe3OjeR?= M1e4Z|QxKM7:TR?= NUnifHQxOjRiaB?= MVXpcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> NXLLS3JTOjR5NkO2NVE>
Vaco400 NXrldHFzTnWwY4Tpc44hSXO|YYm= NVnINVNtPDBizszN MlnxNlQhcA>? NEH6cXBqdmS3Y3XzJHBWVUFicILveIVqdiCjbnSgZ4VtdCCjcH;weI9{cXN? M3HKflI1PzZ|NkGx
DLD1 NHrDdZRHfW6ldHnvckBCe3OjeR?= NWTyXYpUPDBizszN NIjOd4czPCCq NYr0cHZPcW6mdXPld{BRXU2DIIDyc5RmcW5iYX7kJINmdGxiYYDvdJRwe2m| M1rtdlI1PzZ|NkGx
HT29  MWrGeY5kfGmxbjDBd5NigQ>? M4nVUFQxKM7:TR?= NHzMVnEzPCCq MU\pcoR2[2W|IGDVUWEheHKxdHXpckBidmRiY3XscEBieG:ydH;zbZM> MlnpNlQ4PjN4MUG=
PLC/PRF/5  MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXsPVBmOeLCk{ZCuW0> MlPHNlQwPDhxN{KgbC=> MlzmbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NIj2XIYzOzF4OUG0PC=>
HepG2 NUPXN|dsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlKzNgKBmzYEtV2= M1znPVI1NzR6L{eyJIg> MlfwbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M4fReVI{OTZ7MUS4
Hep3B  MmLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWKx5qCUPcL3TR?= M3;1PVI1NzR6L{eyJIg> M3L2PYlvcGmkaYTzJINmdGxiZ4Lve5Rp M{nXeFI{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
NCT03081494 Active not recruiting Metastatic Colorectal Cancer Novartis Pharmaceuticals|Novartis June 9 2017 Phase 1
NCT02042144 Completed Neoplasms Bayer April 8 2014 --
NCT01298570 Active not recruiting Colorectal Cancer Metastatic UNC Lineberger Comprehensive Cancer Center|Bayer April 7 2011 Phase 2
NCT03099486 Recruiting Colorectal Cancer Fox Chase Cancer Center October 6 2017 Phase 2
NCT02080260 Completed Pancreatic Cancer Stuart Salmon MD|Bayer|Carolinas Healthcare System June 6 2014 Phase 2
NCT02788279 Active not recruiting Colorectal Cancer Hoffmann-La Roche July 5 2016 Phase 3

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