Nutlin-3

目录号:S1061

仅限科研使用

Nutlin-3是一种有效的,选择性Mdm2(它自身和p53的环指依赖性泛素蛋白连接酶)拮抗剂,无细胞试验中IC50为90 nM;可稳定p53缺陷细胞中的p73。

Nutlin-3 Chemical Structure

CAS: 890090-75-2

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1515.15 现货
RMB 900.36 现货
RMB 3026.07 现货
RMB 7939.67 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Nutlin-3发表文献83篇:

产品安全说明书

MDM2/MDMX抑制剂选择性比较

相关MDM2/MDMX产品

生物活性

产品描述 Nutlin-3是一种有效的,选择性Mdm2(它自身和p53的环指依赖性泛素蛋白连接酶)拮抗剂,无细胞试验中IC50为90 nM;可稳定p53缺陷细胞中的p73。
靶点
MDM2 [5]
(Cell-free assay)
180 nM
体外研究

Nutlin-3有效抑制MDM2-p53相互作用,IC50 为 90 nM, 导致p53通路激活。Nutlin-3 处理含野生型p53的细胞,如HCT116, RKO 和SJSA-1,诱导MDM2 和p21表达, 且具有有效的抗增殖活性,IC50 为~1.5 μM, 但是作用于含突变型p53的细胞系 SW480和 MDA-MB-435没有效果。10 μM Nutlin-3处理 SJSA-1细胞48小时,显著诱导caspase依赖的细胞凋亡,凋亡达~45%。虽然Nutlin-3也抑制人皮肤 (1043SK) 和小鼠胚胎 (NIH/3T3) 的生长和活力,IC50分别为2.2 μM 和1.3 μM, 10 μM Nutlin-3处理一周后仍保留细胞活力,而3 μM Nutlin-3 处理SJSA-1细胞后,细胞则无活力。[1] Nutlin-3 不诱导p53在关键丝氨酸残基的磷酸化,在特定DNA结合序列没有区别,且与基因毒性药物Doxorubicin和Etoposide诱导的磷酸化p53相比, 使p53靶点基因转活,说明 p53 在关键丝氨酸残基的磷酸化对转录激活和凋亡是非必需的。[2] 虽然与MDM2相比,Nutlin-3 与MDMX 结合的效率低一点, Nutlin-3作用于视网膜母细胞瘤细胞(Weri1),能抑制MDMX–p53相互作用,且诱导 p53通路,IC50为0.7 μM。[3] 30 μM Nutlin-3作用于无野生型p53的细胞,也扰乱内源性p73-HDM2 相互作用,且增强p73稳定性和促凋亡活性, 导致细胞生长受抑制,和诱导凋亡。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SMMC-7721  MX7GeY5kfGmxbjDBd5NigQ>? NFrm[IUyOCEQvF2= Mm\YN|YhcA>? M3O1UmROW09? NVfSR5d3\G:5bj3y[Yd2dGG2ZYOgeIhmKHC{b4TlbY4h\XiycnXzd4lwdiCuZY\lcEBw\iCyaH;zdIhwNVOnckO5Nk1xPTN? NX\obXk3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyPFY{OTJpPkK0Nlg3OzF{PD;hQi=>
HuH-7 NX32fFJ1SXCxcITvd4l{KEG|c3H5 MWmyNEDPxE1? M2GxbVQ5KGh? NWXIfGVmTE2VTx?= NFL4WIFqdmS3Y3XzJIFxd3C2b4Ppdy=> Mm\jQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{OE[zNVIoRjJ2Mki2N|EzRC:jPh?=
SMMC-7721  MVTBdI9xfG:|aYOgRZN{[Xl? NW\US2pjOjBizszN NI\YT|Q1QCCq MmXMSG1UVw>? MnHSbY5lfWOnczDhdI9xfG:|aYO= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ6NkOxNkc,OjR{OE[zNVI9N2F-
HuH-7 MnuwR4VtdCCYaXHibYxqfHliQYPzZZk> MYCxMlI2NTJyIN88US=> NFnPUpMzPC92OD:3NkBp NEjK[WtFVVOR Mln3bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJIRwe2ViYX7kJJRqdWViZHXw[Y5l\W62bIm= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ6NkOxNkc,OjR{OE[zNVI9N2F-
SMMC-7721  MoDER4VtdCCYaXHibYxqfHliQYPzZZk> MofKNU4zPS1{MDFOwG0> Mkj4NlQwPDhxN{KgbC=> NXHkSmh[TE2VTx?= NGnaWVZqdmirYnn0d{Bk\WyuIIDyc4xq\mW{YYTpc44h\G:|ZTDhcoQhfGmvZTDk[ZBmdmSnboTsfS=> MljOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{OE[zNVIoRjJ2Mki2N|EzRC:jPh?=
RKO MWHGeY5kfGmxbjDBd5NigQ>? NGnDUpQzOCEQvF2= MV[yOEBp NGLBcnRqdmS3Y3XzJGhQNTFiZYjwdoV{e2mxbjDheEB1cGVibHX2[Ywhd2ZidILhcpNkemmydHnvci=> MmPJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nk[wNFcoRjJ2M{[2NFA4RC:jPh?=
U2OS  M3PKT2Z2dmO2aX;uJGF{e2G7 MnGzNlAh|ryP NHLsVoIzPCCq M33RVYlv\HWlZYOgTG8uOSCneIDy[ZN{cW:wIHH0JJRp\SCuZY\lcEBw\iC2cnHud4NzcXC2aX;u MnnuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nk[wNFcoRjJ2M{[2NFA4RC:jPh?=
RKO NYPTdmE2TnWwY4Tpc44hSXO|YYm= NGj0RowzOCEQvF2= MnHPNlQhcA>? NW[ydmZmcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKEiRLUGgdJJwfGWrbjDhd{B4\WyuIHHzJJRp\SCyNUOgdJJwfGWrbh?= NGLuR4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO2OlAxPyd-MkSzOlYxODd:L3G+
U2OS  MXHGeY5kfGmxbjDBd5NigQ>? NYm3TplXOjBizszN M4jCSVI1KGh? NF32cpNqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUhUE9vMTDwdo91\WmwIHHzJJdmdGxiYYOgeIhmKHB3MzDwdo91\Wmw MonEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|Nk[wNFcoRjJ2M{[2NFA4RC:jPh?=
MOLM MkDtSpVv[3Srb36gRZN{[Xl? NHLFNFUyOCEQvF2= NWjlPVNNOjRiaB?= NVuxcnFxfXC{ZXf1cIF1\XNidHjlJHNQS1NvMTDlfJBz\XO|aX;u NX[wU5N7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0O|M2PjJpPkK0OFc{PTZ{PD;hQi=>
OCI NY\HOmU5TnWwY4Tpc44hSXO|YYm= MoXCNVAh|ryP NILuPZgzPCCq NUTGeGJYfXC{ZXf1cIF1\XNidHjlJHNQS1NvMTDlfJBz\XO|aX;u MljzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2N{O1OlIoRjJ2NEezOVYzRC:jPh?=
BeWo NGrtZYZCeG:ydH;zbZMhSXO|YYm= MYezNEDDvU1? NYm2O4N2OjRiaB?= M2\GTYlv[3KnYYPld{BieG:ydH;zbZM> M4LiTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2NEm4NVU1Lz5{NES5PFE2PDxxYU6=
BeWo NWftNm1zTnWwY4Tpc44hSXO|YYm= MkDQN|AhyrWP MoH1NlQhcA>? MlzVbY5kemWjc3XzJJA2OyxiTXTtNkwheDJzIHHu[EBRfW2jIHH0JJRp\SCycn;0[YlvKGyndnXs NYHTbnZjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS0PVgyPTRpPkK0OFk5OTV2PD;hQi=>
MOML13 MVHGeY5kfGmxbjDBd5NigQ>? M2TUdVEx|ryP NU\Wcmh[Oi92IHi= NHXFO5JqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> MlTEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUm3OFkoRjJ2NkW5O|Q6RC:jPh?=
AML3 NH7sWlVHfW6ldHnvckBCe3OjeR?= MoiyNVDPxE1? MWCyM|QhcA>? NInic4FqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> NF\5RoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PVc1QSd-MkS2OVk4PDl:L3G+
AML2 NVrPe|RYTnWwY4Tpc44hSXO|YYm= NGrHdYwyOM7:TR?= MVqyM|QhcA>? NEXLdZVqdmO{ZXHz[ZMhfGinIHzleoVtKG:oIIC1Ny=> NEDydYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PVc1QSd-MkS2OVk4PDl:L3G+
MOML13 NEWzcW9CeG:ydH;zbZMhSXO|YYm= M1\sTVIwOTBizszN Ml3lNlQwPDhiaB?= MUnpcoR2[2W|IHHwc5B1d3Orcx?= NEGzbHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[1PVc1QSd-MkS2OVk4PDl:L3G+
AML2 MkPhRZBweHSxc3nzJGF{e2G7 MoD3Nk8yOCEQvF2= Mn;3NlQwPDhiaB?= MlT3bY5lfWOnczDhdI9xfG:|aYO= MlS3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NUm3OFkoRjJ2NkW5O|Q6RC:jPh?=
U2OS  MXvGeY5kfGmxbjDBd5NigQ>? M2HxUVIxKM7:TR?= MXWyOEBp MUfpcoNz\WG|ZYOgeIhmKG2UTlGgcIV3\Wy|IH;mxsBDS0x{QUGsJGJEVFiOwrDhcoRDS0yZ NFWwcmo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi2O|I2QSd-MkS4OlczPTl:L3G+
Hep3B NWG0WWM6SXCxcITvd4l{KEG|c3H5 MkPMbY5lfWOnczDhdI9xfG:|aYO= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh6NEiwPUc,OjR6OES4NFk9N2F-
Huh-7 MlLMRZBweHSxc3nzJGF{e2G7 MnjvbY5lfWOnczDhdI9xfG:|aYO= M1T1SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi0PFA6Lz5{NEi4OFgxQTxxYU6=
SMMC7721 MYXBdI9xfG:|aYOgRZN{[Xl? M4f5Tolv\HWlZYOgZZBweHSxc3nz NVPLdHZjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
HepG2 NHXJRVVCeG:ydH;zbZMhSXO|YYm= NGLIZZRqdmS3Y3XzJIFxd3C2b4Ppdy=> NYmxb3RqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
Hep3B M4nzemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LBelczKGh? M1uy[WROW09? NITRWpZKSzVyPUKwMlE5KMLzIEGuPFQh|ryP MoHsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OES4NFkoRjJ2OEi0PFA6RC:jPh?=
Huh-7 MnPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjDc|JZPzJiaB?= MnS0SG1UVw>? MoXWTWM2OD1|Mz65OkDDuSB|Lkmg{txO NWG1[5NiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
SMMC7721/Ac M1m2U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XFblczKGh? NX;vfHNRTE2VTx?= NH\Gd|JKSzVyPUW1MlIyKMLzIEWuNFMh|ryP NGm0[5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi4OFgxQSd-MkS4PFQ5ODl:L3G+
SMMC7721 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH3keXc4OiCq MojrSG1UVw>? NHnVXmtKSzVyPUOxMlI5KMLzIESuNkDPxE1? NWLtbJNjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4PFQ5ODlpPkK0PFg1QDB7PD;hQi=>
HepG2/As MmfhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzoO|IhcA>? NYCycnh5TE2VTx?= MmDoTWM2OD14OD6xN{DDuSB7Lk[g{txO M3rWdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi0PFA6Lz5{NEi4OFgxQTxxYU6=
HepG2 M3;BdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTBW5BCPzJiaB?= M3jKXmROW09? NYX1XWNoUUN3ME2zOU45PiEEsTCyMlkh|ryP M3nZRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi0PFA6Lz5{NEi4OFgxQTxxYU6=
MOLM-13 NFfkOnFHfW6ldHnvckBCe3OjeR?= MlLBOuKh|ryP NWLFV|JNPiCq NUH4SWxiTE2VTx?= MXnlcohidmOnczD0bIUh[WOndInsZZRqd25ib3[gbIl{fG:wZTDINmIh[W6mIHjlZZQhe2ixY3ugdJJwfGWrboOgTJNxOjdiYX7kJGh{eDly MoriQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6OEWwPFIoRjJ2OEi1NFgzRC:jPh?=
MOLM-13 M37UcGZ2dmO2aX;uJGF{e2G7 NHK3fW03yqEQvF2= MWmwMVghcA>? NXS4ZWN4TE2VTx?= MlrQbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZicEWzMEBOTE1{LDDwNlEh[W6mIHHj[ZR6dGG2ZXSgdFU{ M{jCfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEi1NFgzLz5{NEi4OVA5OjxxYU6=
115 NUjwWJN6TnWwY4Tpc44hSXO|YYm= Mnj1OUDPxE1? MWm0PEBp M2GyNmROW09? M3Hod4lv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= NWTWd2FtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlc4QDdpPkK1NFY4Pzh5PD;hQi=>
A498 MWLGeY5kfGmxbjDBd5NigQ>? NGe0T3Y2KM7:TR?= Mm\XOFghcA>? NF\0SppFVVOR MYXpcoR2[2W|IIC1N{1l\XCnbnTlcpQhe2WwZYPj[Y5k\cLi MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4N{e4O{c,OjVyNke3PFc9N2F-
Caki-2 NWjl[WZETnWwY4Tpc44hSXO|YYm= MVi1JO69VQ>? M{Tv[VQ5KGh? NFvJfVVFVVOR MmrQbY5lfWOnczDwOVMu\GWyZX7k[Y51KHOnbnXzZ4Vv[2YEoB?= NH76R5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2O|c5Pyd-MkWwOlc4QDd:L3G+
ACHN Mk\zSpVv[3Srb36gRZN{[Xl? M3rLSVUh|ryP MUi0PEBp M4jrdmROW09? M2X3TYlv\HWlZYOgdFU{NWSncHXu[IVvfCC|ZX7ld4NmdmOnwrC= NV\JTlE{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlc4QDdpPkK1NFY4Pzh5PD;hQi=>
115 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrDOoVYPSEQvF2= MlzLOFghcA>? NXvKNpp7TE2VTx?= NF[0R4pqdmS3Y3XzJINmdGxiY4njcIUh[XK{ZYP0xsA> NHjqd3E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2O|c5Pyd-MkWwOlc4QDd:L3G+
A498 NGXZSW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYC1JO69VQ>? MY[0PEBp MYLEUXNQ MXnpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2wrC= NF3xOo89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUC2O|c5Pyd-MkWwOlc4QDd:L3G+
Caki-2 NF3RRodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETnR4c2KM7:TR?= NFXUZZc1QCCq NUfH[m9MTE2VTx?= MkPVbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dNMg MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4N{e4O{c,OjVyNke3PFc9N2F-
ACHN MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnzOUDPxE1? NYXtTJdWPDhiaB?= MUjEUXNQ NYjwe3A2cW6mdXPld{Bk\WyuIHP5Z4xmKGG{cnXzeOKh MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4N{e4O{c,OjVyNke3PFc9N2F-
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Assay
Methods Test Index PMID
Western blot MDM2 / p53 / ALKBH2 / p21 / PUMA RRM1 / RRM2 / p53R2 / p21 / p53 / pS6 / S6 23258843 28507282
Immunofluorescence Lamin A / Lamin C / p16 / H3K9me3 Merlin / cyclin D1 / p53 / MDM2 p53 30728349 30274821 24286312
Growth inhibition assay Cell viability 29286113
体内研究 Nutlin-3 按200 mg/kg 剂量口服处理,每天两次,持续3周,显著抑制SJAS-1移植瘤生长,抑制达90%, 而Doxorubicin抑制81%肿瘤生长。[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]

  • Biacore 研究:

    在Biacore S51上进行竞争性实验。衍生一系列S传感器芯片CM5,用于固定 PentaHis抗体,为了捕获 His-标记的p53。捕获的水平为~200反应单位(1 反应单位对应于1 pg 蛋白/ mm2)。MDM2蛋白浓度一直维持在300 nM。Nutlin-3 溶于DMSO,浓度为10 mM,然后进一步稀释,在每个MDM2实验样本中产生系列浓度的Nutlin-3。在电泳缓冲液(10 mM Hepes,0.15 M NaCl, 2% DMSO)中25oC下进行实验。在Nutlin-3存在时,计算MDM2-p53结合情况,作为结合百分数, 使用Microsoft Excel计算IC50。

细胞实验:

[1]

  • Cell lines: HCT116, RKO, SJSA-1, SW480, 和 MDA-MB-435
  • Concentrations: 溶于DMSO,终浓度为~ 30 μM
  • Incubation Time: 8, 24, 和 48 小时
  • Method:

    使用不同浓度Nutlin-3处理细胞8, 24和 48 小时。通过实时PCR分析p21 和MDM2基因转录水平,通过Western Blotting分析蛋白水平。通过MTT实验测定细胞活力。 通过末端脱氧核苷酸转移酶调节的脱氧尿苷三磷酸缺口末端标记法(TUNEL)染色,使用流式细胞仪和荧光显微镜测定细胞凋亡。

动物实验:

[1]

  • Animal Models: 皮下注射 SJSA-1细胞的雌性无胸腺Nu/Nu-nuBR裸鼠
  • Dosages: 200 mg/kg
  • Administration: 口服处理,每天两次

溶解度(25°C)

体外

* 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 581.5
化学式

C30H30Cl2N4O4

CAS号 890090-75-2
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

技术支持

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操作手册

如果有其他问题,请给我们留言。

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常见问题及建议解决方法

问题 1:
Is this a racemic mixture of Nutlin-3a and Nutlin-3b or just the Nutlin-3a enantiomer?

回答:
It is a racemate.

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