Trametinib (GSK1120212)

目录号:S2673 别名: JTP-74057, Mekinist

仅限科研使用

Trametinib (GSK1120212, JTP-74057, Mekinist)是一种高特异性的,有效的MEK1/2抑制剂,无细胞试验中IC50为0.92 nM/1.8 nM,对c-Raf, B-Raf, ERK1/2没有抑制活性。Trametinib 可激活自噬并诱导凋亡。

Trametinib (GSK1120212) Chemical Structure

CAS: 871700-17-3

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2359.39 现货
RMB 986.85 现货
RMB 1731.16 现货
RMB 5471.22 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Trametinib (GSK1120212)发表文献1090篇:

产品安全说明书

MEK抑制剂选择性比较

相关MEK产品

生物活性

产品描述 Trametinib (GSK1120212, JTP-74057, Mekinist)是一种高特异性的,有效的MEK1/2抑制剂,无细胞试验中IC50为0.92 nM/1.8 nM,对c-Raf, B-Raf, ERK1/2没有抑制活性。Trametinib 可激活自噬并诱导凋亡。
特性 药效大于PD0325901或AZD6244
靶点
MEK1 [1]
(Cell-free assay)
MEK2 [1]
(Cell-free assay)
0.92 nM 1.8 nM
体外研究

GSK1120212抑制 MBP 的磷酸化,对于不同亚型的Raf和MEK 而言,IC50在0.92 nM-3.4 nM。GSK1120212对c-Raf, B-Raf, ERK1和ERK2的激酶活性没有抑制作用。另外,GSK1120212对于其它98种激酶没有很强的抑制作用。GSK1120212对于人结肠癌细胞系有很强的抑制作用,其中HT-29和COLO205细胞组成型表达有活性的B-Raf突变,这两种细胞对GSK1120212最为敏感,IC50分别是0.48 nM 和 0.52 nM。含有k-Raf突变的细胞系对GSK1120212的敏感性介于如下范围,IC50是2.2-174 nM. 相反地,COLO320 DM细胞中B-Raf 和K-Ras均为野生型,因而即便在10 μM都对GSK1120212有抗性。用GSK1120212处理24小时可以诱导所有敏感细胞的细胞周期停滞在G1期。与此一致,GSK1120212处理使得大部分人结肠癌细胞系中p15INK4b 和/或p27KIP1的表达量上升。GSK1120212能诱导HT-29和COLO205细胞的凋亡,COLO205细胞更为敏感。[1] GSK1120212抑制外周血单核细胞产生肿瘤坏死因子-α和白介素-6。 [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231, SW480 and SW1116 cells MmXZSpVv[3Srb36gZZN{[Xl? NEnjdXIyODEkgJnuUS=> M3LvelI1KGh? NXLYfnRFfHKjbXX0bY5q[iClb4Xs[EBl\WO{ZXHz[UB[SVBibHX2[Yx{KGGwZDDpcohq[mm2IFzNRk1qdmS3Y3XkJHlCWCC3cILl[5Vt[XSrb36gbY4hVUSDLV3CMVI{OSxiU2exNVE3KGGwZDDTW|Q5OCClZXzsdy=> MknYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB6M{O2OlUoRjNyOEOzOlY2RC:jPh?=
RG7388-resistant U87MG cells NGjUTHVHfW6ldHnvckBie3OjeR?= M4fSVFExKG6P MkTRNlQhcA>? M3qwZmROW09? MYfUdoFu\XSrbnniJJRz\WG2bXXueEBz\WS3Y3XkJJRp\SCrbo\hd4l3\SCyaHXuc5R6eGVib3[gVmc4Ozh6IILld4l{fGGwdDDj[Yxtey5? Mm\WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{N{S5PFQoRjNyMke0PVg1RC:jPh?=
BJAB cells NGTvU5dHfW6ldHnvckBie3OjeR?= MnvCNE4xOc7:TR?= NYrSbY5YOjRiaB?= NV3WcY4yOC5yMTFOwG0hfHKjbXX0bY5q[iCnZn\lZ5RqfmWueTDzeZBxemW|c3XkJJRp\SCHUlugbJlx\XKjY4TpeoF1cW:wIHnuJGJLSUJiY3XscJMh[2G3c3XkJIJ6KHSqZTDjc41jcW6nZDD0doVifG2nboSgc4YhSkuPMUKwJIFv\CCGYX71d4VzfGmkLh?= M2TDVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOUS3OVc3Lz5|MEm0O|U4PjxxYU6=
Human PDAC cell lines (MIA-PACA, PANC-1, CFPAC-1, PL45, CAPAN-2 and HPAF-II) M1HiOGZ2dmO2aX;uJIF{e2G7 MorKNVAhdk1ib4KgNVAxKG6P NWKwenQxOy2mYYnzJI9zKDZvZHH5dy=> NILJd|VVcGViY3;uZ4VvfHKjdHnvckBw\iBzMDDuUUB1emGvZYTpcoljKGOxboPpd5RmdnSueTDwdo9lfWOnZDDzbYdvcW[rY3HueEBlcW[oZYLlcoNmeyCkZYT3[YVvKGenZnn0bY5q[iCjbnSgeJJidWW2aX7pZkBidG:wZTDjc41x[XKnZDD0c{Bkd22kaX7heIlwdiCpZX\peIlvcWJiYX7kJJRz[W2ndHnubYIhcW5iYXzsJIZwfXJic3Xud4l1cX[nIHPlcIwhdGmwZYOgLGNHWEGFLUGsJJBtPDVuIFPBVGFPNTJiYX7kJGhRSUZvSVmpMkBPdyCjZHTpeIl3\SCnZn\lZ5Qhf2G|IH;id4VzfmWmIHnuJJRp\SCpZX\peIlvcWJiaX7z[Y5{cXSrdnWgc5Ih\XilaYTheI9zgSClZXzsJIxqdmW|IDjNTWEuWGGlYTDhcoQhWEGQQz2xLS=> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl{MUO1NUc,OzB7MkGzOVE9N2F-
Transitional cell carcinoma (TCC) cell lines MlXQSpVv[3Srb36gZZN{[Xl? NEX4RlczPSCwTR?= MXm2MVI1KGh? MWjDZY5qdmViVFPDJINmdGxibHnu[ZMh[XKnIIPlcpNqfGm4ZTD0c{BOTUtiaX7obYJqfGmxbh?= NUPMNllRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GwOFg2PDhpPkOxNFQ5PTR6PD;hQi=>
COLO205 M3TCcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX7J[Y02PzJiaB?= MlHTTWM2OCB;IECuNFAyKM7:TR?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
HT-29 NXS3OGpYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MY[3NkBp NGe0dZZKSzVyIE2gNE4xODFizszN MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
COLO205 M1vBN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVS4Z2ZtPzJiaB?= M2S3OWlEPTBiPTCwMlAxOSEQvF2= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
MV522 NUfsO4FLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1rBdFczKGh? Moj4TWM2OCB;IECuNFAyKM7:TR?= MmraQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
HT-29 MoTvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn\jO|IhcA>? MlnNTWM2OCB;IECuNFAzKM7:TR?= NWPQXndERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
MV522 M1[ybWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3PWeFczKGh? MYHJR|UxKD1iMD6wNFIh|ryP NHHwe5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
NCI-H727 MnPCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYS3NkBp MnP4TWM2OCB;IECuNFAzKM7:TR?= M{jjeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H727 Mn;hS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEP0XYk4OiCq M33sXmlEPTBiPTCwMlAxOiEQvF2= NGrnOos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW1417 NFfSZnVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXe3NkBp MljTTWM2OCB;IECuNFA{KM7:TR?= NH3KNZg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW1417 MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF\DdnM4OiCq NGLFOFFKSzVyIE2gNE4xODNizszN NX60doVFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
Calu6 MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2[4fVczKGh? NUn3Z|lHUUN3MDC9JFAvODB|IN88US=> M1ywS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
LS1034 MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4ezV|czKGh? MoLRTWM2OCB;IECuNFA1KM7:TR?= M3LhW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
SW1463 NFPBRYpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M33hR|czKGh? M{f1[WlEPTBiPTCwMlAxPCEQvF2= MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
SW1463 Ml3jS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWPqV4tvPzJiaB?= NXTa[lJkUUN3MDC9JFAvODB2IN88US=> NVm3RpUyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
Calu6 NFzoOYNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmLkO|IhcA>? MUDJR|UxKD1iMD6wNFQh|ryP NIWyc3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
LS1034 NWPaelhET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoPMO|IhcA>? M4ewTmlEPTBiPTCwMlAxPSEQvF2= MoK4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
RKO NEjybJBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEftSGo4OiCq M2P0V2lEPTBiPTCwMlAxPSEQvF2= MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
NCI-H508 M1\pO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnXDO|IhcA>? NYTX[nBVUUN3MDC9JFAvODB6IN88US=> M{n3WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
KM12 MlfrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4i0T|czKGh? MUTJR|UxKD1iMD6wNUDPxE1? NH\kWY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
A427 NYftOGgxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUfjWGtrPzJiaB?= NGixUplKSzVyIE2gNE4xOSEQvF2= NH22OWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
NCI-H1155 M3fWdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4HMe|czKGh? NF3kTlBKSzVyIE2gNE4xOSEQvF2= M2XvdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
HCT8 NGOwd3dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEPFNHE4OiCq NGTGWFRKSzVyIE2gNE4xOTRizszN NVTk[oZGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
MDA-MB-175-VII M36zcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYDxXnhNPzJiaB?= MkD4TWM2OCB;IECuNFE3KM7:TR?= M2T3XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
A549 M{XxXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHjkR2s4OiCq MXHJR|UxKD1iMD6wNVYh|ryP MnLNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
RKO MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mmf2O|IhcA>? MYfJR|UxKD1iMD6wNVgh|ryP Ml\kQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
NCI-H23 NGC0RpJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3PHTVczKGh? NELvW|hKSzVyIE2gNE4xOiEQvF2= M33mTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
A427 MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVi3NkBp NH3QV3RKSzVyIE2gNE4xOjJizszN MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
KM12 M37oSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV23NkBp M1fwWmlEPTBiPTCwMlAzOyEQvF2= NEX6VnI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
NCI-H508 NHvEZ5BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlfjO|IhcA>? Mn71TWM2OCB;IECuNFI{KM7:TR?= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
MDA-MB-231 M4\VOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NW\FTo9JOyCmYYnz NUDGXZdHT0l3MDC9JFAvODJ3IN88US=> M{nTdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
SW837 M2LZR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEXiSXY4OiCq NXO3XZZWUUN3MDC9JFAvODJ3IN88US=> M3vpPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
SW480 MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlTSO|IhcA>? Mn;aTWM2OCB;IECuNFI3KM7:TR?= M2naSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H1355 NXyyelBsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHrw[W84OiCq MX7JR|UxKD1iMD6wNlch|ryP NGnHe2o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
NCI-H23 MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoHIO|IhcA>? NF:1ZZVKSzVyIE2gNE4xOjlizszN MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
EFM19 NW\HRm9JT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUDObnJ6PzJiaB?= MUTJR|UxKD1iMD6wN{DPxE1? NX;SUppmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
T84 M2jVe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkPJO|IhcA>? MkjUTWM2OCB;IECuNFMh|ryP MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
A549 NIfFUXpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{XIdlczKGh? MYDJR|UxKD1iMD6wN|Qh|ryP MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
NCI-H1792 M2W3bGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV70WllpPzJiaB?= MWPJR|UxKD1iMD6wN|Uh|ryP M3n2ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
SW480 MlPCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXvCR2hVPzJiaB?= NXzo[G5FUUN3MDC9JFAvODN5IN88US=> M2LPbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
COR-L23 NFnUfJNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWmwNmJKPzJiaB?= NEfwb2RKSzVyIE2gNE4xOzdizszN MnLJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
SW1573 MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXe3NkBp NYS4Tlk{UUN3MDC9JFAvODN6IN88US=> MmOzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
Calu3 Mnq5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MY[3NkBp M1iwW2lEPTBiPTCwMlA{QSEQvF2= M1PYV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
HCC827 NWHV[2o2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{e4elczKGh? NVLPNW5vUUN3MDC9JFAvODRizszN MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
HOP62 MmjhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYX6ZmM4PzJiaB?= NHnHVVFKSzVyIE2gNE4xPSEQvF2= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
NCI-H1355 NUD3NY9rT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4TlVFczKGh? NH;QdI5KSzVyIE2gNE4xPTJizszN MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
NCI-H1792 Ml7aS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHTGbYI4OiCq NFK3XodKSzVyIE2gNE4xPTNizszN MmXDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
HCT8 MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3nsNVczKGh? Mm\4TWM2OCB;IECuNFU2KM7:TR?= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
T84 MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYC3NkBp MkTXTWM2OCB;IECuNFYyKM7:TR?= NIHROWc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW900 NFHweXhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXLOdIRRPzJiaB?= NELoTJlKSzVyIE2gNE4xPzJizszN M1TwOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
SW837 NW\6S2FXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn;qO|IhcA>? M1TaNGlEPTBiPTCwMlA4PCEQvF2= MkPxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
DLD1 M4[2fGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH2xOoo4OiCq MWjJR|UxKD1iMD6wPVMh|ryP MoDnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
MDA-MB-175-VII MknvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnLQO|IhcA>? MnPpTWM2OCB;IECuNFk3KM7:TR?= MlLsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
SW900 MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{TZblczKGh? M{CwcGlEPTBiPTCwMlEzPyEQvF2= NHP1O4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
Calu3 MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYO3NkBp M1PLdWlEPTBiPTCwMlE2QCEQvF2= Ml:1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
COR-L23 NIXtTlZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mlv4O|IhcA>? NHnpd|VKSzVyIE2gNE4{OjlizszN M{WyU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
DLD1 NYrFfI1KT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlLUO|IhcA>? M2e5dGlEPTBiPTCwMlY{OiEQvF2= NFO4XpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
Assay
Methods Test Index PMID
Western blot ERRα / IDH3 / c-Myc / Cyclin D1 pERK /ERK / pS6 / S6 β-catenin 30185207 29133622 28422736
Growth inhibition assay Cell proliferation MTT assay 30185207 26832408
Immunofluorescence phospho-PR(S345) β-catenin 29237804 28422736
体内研究 按0.3 mg/kg或1 mg/kg 的剂量口服GSK1120212(一天一次共14天)能有效抑制HT-29肿瘤,1 mg/kg 的剂量可完全抑制肿瘤生长。在癌症组织中,一次口服1 mg/kg GSK1120212能完全抑制ERK1/2的磷酸化,14天后能提高p15INK4b和p27KIP1的表达量。在COLO205肿瘤模型中,0.3 mg/kg剂量的GSK1120212就足以抑制肿瘤生长,1 mg/kg剂量的GSK1120212可以使2/3的老鼠的肿瘤消退至可检测水平之下。[1] 0.1 mg/kg剂量的GSK1120212完全抑制佐剂性关节炎(AIA)和II型胶原诱导的关节炎(CIA) Lewis大鼠或DBA1/J小鼠。[2]

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]
  • Raf-MEK-ERK级联激酶检测:

    非磷酸化的髓鞘碱性蛋白(MBP)涂覆到ELISA板上,B-Raf/c-Raf的活性形式与非磷酸化MEK1/MEK2和ERERK2混合在10 μM ATP和12.5 mM MgCl2,其MOPS缓冲液中含有不同浓度的GSK1120212。 MBP的磷酸化是由抗磷酸化的MBP抗体进行检测。

细胞实验:[1]
  • Cell lines: HT-29, HCT-15, HCT116, COLO205, LS-174T, SW480, SW620, T84, LoVo和COLO320
  • Concentrations: 溶解在DMSO中至终浓度约10 μM
  • Incubation Time: 3天或4天
  • Method: 指数生长的细胞预培养在96孔组织培养板中24小时后用GSK1120212孵育。细胞生长是通过体外毒理学测定试剂盒(基于磺酰罗丹明B)检测。对于细胞凋亡测定,漂浮和贴壁细胞被收集并用70%乙醇固定。用PBS洗涤后,将细重胞悬在100微克/毫升RNA酶和25微克/毫升的碘化丙啶(PI)中,至于37℃黑暗中30分钟。每一个单细胞的DNA含量是用流式细胞仪Cytomics FC500或番石榴EasyCyte来确定。
动物实验:[1]
  • Animal Models: 雌雄BALB/c-nu/nu小鼠皮下注射HT-29或COLO205细胞
  • Dosages: 1 mg/kg/day
  • 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):
4% DMSO+corn oil

3mg/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 615.39
化学式

C26H23FIN5O4

CAS号 871700-17-3
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
NCT04454476 Not yet recruiting Drug: Trametinib treatment|Procedure: Endoscopy Gastric Cancer|Metaplasia|Stage I Gastric Cancer|Initial-onset Gastric Cancer Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) December 2022 Phase 1
NCT05275374 Not yet recruiting Drug: XP-102|Drug: Trametinib Cancer|BRAF V600 Mutation|Melanoma|Colorectal Cancer|Thyroid Cancer|Nonsmall Cell Lung Cancer Xynomic Pharmaceuticals Inc. June 2022 Phase 1|Phase 2
NCT04566133 Recruiting Drug: Trametinib|Drug: Hydroxychloroquine Bile Duct Cancer|Biliary Cancer|Biliary Tract Neoplasms|Cholangiocarcinoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) February 15 2022 Phase 2
NCT04961619 Recruiting Drug: dabrafenib|Drug: trametinib Melanoma Novartis Pharmaceuticals|Novartis December 1 2021 --

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

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操作手册

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常见问题及建议解决方法

问题 1:
Could you help us with the best way to prepare Trametinib for in vivo i.p. injections?

回答:
S2673 can be dissovled in 4% DMSO/corn oil at 3 mg/ml clearly.

问题 2:
How to solve the problem that this product didn't dissolve up to 10mM in DMSO at room temperature?

回答:
The solution can be heated up to 50 degree to help dissolve. Besides, sonication (with a probe sonicator) also helped greatly.

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