Regorafenib (BAY 73-4506)

目录号:S1178 别名: Fluoro-Sorafenib, Resihance, Stivarga

仅限科研使用

Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) 是一个多靶点抑制剂,作用于VEGFR1VEGFR2VEGFR3PDGFR-βKit (c-Kit)RET (c-RET)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。Regorafenib 可诱导自噬。

Regorafenib (BAY 73-4506) Chemical Structure

CAS: 755037-03-7

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 3830.98 现货
RMB 7954.71 现货
大包装 有超大折扣

今日订购,明日送达 全国免运费 分装免费 分装成小规格产品(单支最小为1mg)
如1支10mg产品可分装为10支1mg产品

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Regorafenib (BAY 73-4506)发表文献165篇:

产品安全说明书

VEGFR抑制剂选择性比较

相关VEGFR产品

生物活性

产品描述 Regorafenib (BAY 73-4506, Fluoro-Sorafenib, Resihance, Stivarga) 是一个多靶点抑制剂,作用于VEGFR1VEGFR2VEGFR3PDGFR-βKit (c-Kit)RET (c-RET)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。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)
点击更多
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 M1y5[GFxd3C2b4Ppd{BCe3OjeR?= M1m5bFHjiJN3wrFOwG0> M1zXZlQ5KGh? NWrnfHBOcW6qaXLpeJMh[2WubDDndo94fGh? M2X3eFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{K5OlA5Lz5{NkOyPVYxQDxxYU6=
PLC/PRF/5  NWL3UHluSXCxcITvd4l{KEG|c3H5 NVy4RoNmOeLCk{ZCpO69VQ>? MoWyOFghcA>? NVjjdmlJcW6qaXLpeJMh[2WubDDndo94fGh? M1HNe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{K5OlA5Lz5{NkOyPVYxQDxxYU6=
HepG2  NFPKV3NCeG:ydH;zbZMhSXO|YYm= NHvTTlQy6oDVNdMg{txO NVf6eIplPDhiaB?= MnrQbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN{OU[wPEc,OjZ|Mkm2NFg9N2F-
HEK293 MU\GeY5kfGmxbjDBd5NigQ>? Mo\BNE426oDLzszN NVfoNlF2Oi92L{[gbC=> MX\y[YR2[2W|IFfSVFc5KGW6cILld5Nqd25? M3fRdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEW4NFMzLz5{NUi1PFA{OjxxYU6=
GEO Mn:3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml:wNE4xOS1{MDFOwG0> Mn3tPVYhcA>? MmHxSG1UVw>? M17XTYlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4TGTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N|kyLz5{NUizPFM6OTxxYU6=
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HT29 NF7rRY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLpcnczOC5yMT2yNEDPxE1? MnrsPVYhcA>? MmDCSG1UVw>? NV7UNYRucW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NULJR|lzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|g{QTFpPkK1PFM5OzlzPD;hQi=>
SW480 Mn;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mle1NE4xOS1{MDFOwG0> NVOwTHdDQTZiaB?= Mnn1SG1UVw>? NYj4U5ZMcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M2joVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N|kyLz5{NUizPFM6OTxxYU6=
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LOVO NH\YZlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\xNE4xOS1{MDFOwG0> MlP0PVYhcA>? MYjEUXNQ M1zwVolvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4HuTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N|kyLz5{NUizPFM6OTxxYU6=
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SW48-CR NY\MdZRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml[5NE4xOS1{MDFOwG0> NED6cYk6PiCq NGnr[49FVVOR M4jk[YlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NVmxR5lNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW4N|g{QTFpPkK1PFM5OzlzPD;hQi=>
GEO-CR MorLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH;FU3AxNjBzLUKwJO69VQ>? MVm5OkBp MVHEUXNQ M3LX[YlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M{Hke|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OEO4N|kyLz5{NUizPFM6OTxxYU6=
KB-31 MmS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlX4TWM2OD13LkZCtVAvOyCwTR?= NEHKd|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe1N|M3OSd-MkW3OVM{PjF:L3G+
KB-G2 NWPvXGNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTlwMdMxNE4yKG6P MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTd3M{O2NUc,OjV5NUOzOlE9N2F-
LLC-PK1 NV7G[242T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnVdm1CUUN3ME20Nk4xyrF|LkKgcm0> MmDUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV5NUOzOlEoRjJ3N{WzN|YyRC:jPh?=
LLC-PK1/MRP2 M3r5[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTrRWtKSzVyPUiyMlTDuTJwNzDuUS=> NF3GVnk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe1N|M3OSd-MkW3OVM{PjF:L3G+
HEK293 NH3IZ5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33oXmlEPTB;MUGuNOKyOS5{IH7N NFPpeHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe1N|M3OSd-MkW3OVM{PjF:L3G+
HEK293/OATP1B1 MlOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1H1PWlEPTB;Nj6yxtExNjNibl2= NHjRW|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUe1N|M3OSd-MkW3OVM{PjF:L3G+
HROC18 NWC4fJZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmq1TWM2OD1zLkOg{txO MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTNyOUmxOEc,OjV|MEm5NVQ9N2F-
HROC24 M4HnTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7JXoQ2UUN3ME20MlYh|ryP MoXqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|MEm5NVQoRjJ3M{C5PVE1RC:jPh?=
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MCF-7 NE\hcYhHfW6ldHnvckBCe3OjeR?= MYGwMlUwPSEQvF2= NX61OFN[OjRiaB?= NFTrNWtFVVOR M{eyWYlvcGmkaYTzJJRp\SClZXzsJI1q\3KjdHnvci=> NYrOT|V5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyOVM6QTRpPkK1NlU{QTl2PD;hQi=>
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GBM12 NWSxbIQ4SXCxcITvd4l{KEG|c3H5 NF7rTIsxNjYkgKOxMlDjiIoQvF2= Mn\nNlQhcA>? NFjNRoZFVVOR NYHFTGl4cW62ZYLhZ5R{KHerdHigcIFx[XSrbnniJJRwKGmwZIXj[UBk\WyuIHTlZZRp M{\oNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUGxNlE2Lz5{NEmxNVIyPTxxYU6=
GBM14  NUXLfJNsSXCxcITvd4l{KEG|c3H5 NXzhb4dIOC534pETNU4x6oDLzszN NH;rS|kzPCCq M1rnUWROW09? M3L0TYlvfGW{YXP0d{B4cXSqIHzhdIF1cW6rYjD0c{BqdmS3Y3WgZ4VtdCCmZXH0bC=> NEG1UWY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxNVIyPSd-MkS5NVEzOTV:L3G+
Hep3B NUDJUVl7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUC3V2tCOeLCk{KuOeKh|ryP NWL6RoZOOjRxNEivO|IhcA>? MUfpcohq[mm2czDj[YxtKGe{b4f0bC=> NVzURXU6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFU5QTBpPkK0PFg2QDlyPD;hQi=>
PLC/PRF/5  M2L3SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrpNgKBmzJwNdMg{txO MoG3NlQwPDhxN{KgbC=> NHfLU5dqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NV\wVVlRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFU5QTBpPkK0PFg2QDlyPD;hQi=>
HepG2  MoTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDUNncy6oDVMj61xsDPxE1? NXrGcXE5OjRxNEivO|IhcA>? NHK0fIlqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M{fTWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi1PFkxLz5{NEi4OVg6ODxxYU6=
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Assay
Methods Test Index PMID
Western blot PUMA / p53 Bim / Bid / Bak / Bcl-Xl / Mcl-1 p-p65(S536) / p65 p-FGFR2 / p-FRS2α / p-AKT / p-MAPK / p-P90RSK / FGFR2 / AKT / MAPK / p90RSK Cyclin D / Cyclin E / Cyclin A / Cyclin B / p27 / p21 p-STAT3 / STAT3 / PARP / Caspase-9 24763611 29573334 25071018
Immunofluorescence p65 F-actin / Vimentin / E-cadherin 24763611 27580057
Growth inhibition assay GI50 Cell viability 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]

  • 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]

  • 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。

动物实验:

[1]

  • 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

溶解度(25°C)

体外

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05370807 Not yet recruiting Drug: Regorafenib 40 MG Oral Tablet Melanoma Stage III|Melanoma Stage IV Universitair Ziekenhuis Brussel May 2022 Phase 2
NCT05289726 Not yet recruiting Drug: Traditional chinese medicine TDX105|Drug: Placebo Hand and Foot Skin Reaction|Colorectal Cancer Stage IV Cancer Institute and Hospital Chinese Academy of Medical Sciences April 18 2022 Phase 2
NCT05023720 Recruiting Other: nonintervention Metastatic Colorectal Cancer Henan Cancer Hospital July 20 2021 --
NCT04920422 Active not recruiting Other: No intervention Metastatic Colorectal Cancer Bayer July 15 2021 --
NCT05024539 Recruiting Other: nonintervention Hepatocellular Carcinoma Shujun Yang|Henan Cancer Hospital June 20 2021 --

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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.

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