Trametinib (GSK1120212)

For research use only.

Catalog No.S2673 Synonyms: JTP-74057, Mekinist

941 publications

Trametinib (GSK1120212) Chemical Structure

CAS No. 871700-17-3

Trametinib (GSK1120212, JTP-74057, Mekinist) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2. Trametinib activates autophagy and induces apoptosis.

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Selleck's Trametinib (GSK1120212) has been cited by 941 publications

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Biological Activity

Description Trametinib (GSK1120212, JTP-74057, Mekinist) is a highly specific and potent MEK1/2 inhibitor with IC50 of 0.92 nM/1.8 nM in cell-free assays, no inhibition of the kinase activities of c-Raf, B-Raf, ERK1/2. Trametinib activates autophagy and induces apoptosis.
Features More potent than PD0325901 or AZD6244.
Targets
MEK1 [1]
(Cell-free assay)
MEK2 [1]
(Cell-free assay)
0.92 nM 1.8 nM
In vitro

GSK1120212 inhibits the phosphorylation of MBP regardless of the isotype of Raf and MEK, with IC50 ranging from 0.92 nM to 3.4 nM. GSK1120212 demonstrates no inhibition of the kinase activities of c-Raf, B-Raf, ERK1 and ERK2. In addition, GSK1120212 does not show drastic inhibitory activity against the other 98 kinases. GSK1120212 displays potent inhibitory activity against human colorectal cancer cell lines. HT-29 and COLO205 cells, which are known to have a constitutively active B-Raf mutant, are most sensitive to GSK1120212 with IC50 0.48 nM and 0.52 nM, respectively. The cell lines bearing a K-Ras mutation show a wide range of sensitivity to GSK1120212 with IC50 of 2.2-174 nM. In contrast, COLO320 DM cells, bearing the wild-type gene in both B-Raf and K-Ras, are found to be resistant to GSK1120212 even at 10 μM. GSK1120212 treatment for 24 hours induces cell-cycle arrest at the G1 phase in all sensitive cell lines. Consistently, GSK1120212 treatment leads to upregulation of p15INK4b and/or p27KIP1 in most of the colorectal cancer cell lines. GSK1120212 inhibits constitutive ERK phosphorylation in all sensitive cell lines. GSK1120212 induces apoptosis both in HT-29 and COLO205 cells, but that COLO205 cells are more sensitive to GSK1120212 than HT-29 cells in terms of apoptosis induction. [1] GSK1120212 blocks tumor necrosis factor-α and interleukin-6 production from peripheral blood mononuclear cells (PBMCs). [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231, SW480 and SW1116 cells MWLGeY5kfGmxbjDhd5NigQ>? M{DRbFExOOLCiX7N MXKyOEBp MUH0doFu\XSrbnniJINwfWymIHTlZ5Jm[XOnIGnBVEBt\X[nbIOgZY5lKGmwaHnibZQhVE2ELXnu[JVk\WRiWVHQJJVxemWpdXzheIlwdiCrbjDNSGEuVUJvMkOxMEBUXzFzMU[gZY5lKFOZNEiwJINmdGy| MmmxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB6M{O2OlUoRjNyOEOzOlY2RC:jPh?=
RG7388-resistant U87MG cells MX\GeY5kfGmxbjDhd5NigQ>? NFX6d2oyOCCwTR?= NHi2Z3MzPCCq MoD5SG1UVw>? NG[2TY1VemGvZYTpcoljKHS{ZXH0cYVvfCC{ZXT1Z4VlKHSqZTDpcpZie2m4ZTDwbIVvd3S7cHWgc4YhWkd5M{i4JJJme2m|dHHueEBk\Wyucz6= MnTiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{N{S5PFQoRjNyMke0PVg1RC:jPh?=
BJAB cells NHi2NZFHfW6ldHnvckBie3OjeR?= MVuwMlAy|ryP MoXONlQhcA>? M{[y[VAvODFizszNJJRz[W2ndHnubYIh\W[oZXP0bZZmdHlic4XwdJJme3OnZDD0bIUhTVKNIHj5dIVz[WO2aY\heIlwdiCrbjDCTmFDKGOnbHzzJINifXOnZDDifUB1cGViY3;tZolv\WRidILlZZRu\W62IH;mJGJMVTF{MDDhcoQhTGGwdYPldpRq[i5? MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl2N{W3Okc,OzB7NEe1O|Y9N2F-
Human PDAC cell lines (MIA-PACA, PANC-1, CFPAC-1, PL45, CAPAN-2 and HPAF-II) M1rXPGZ2dmO2aX;uJIF{e2G7 MX6xNEBvVSCxcjCxNFAhdk1? NWLNTIlDOy2mYYnzJI9zKDZvZHH5dy=> M2q1cnRp\SClb37j[Y51emG2aX;uJI9nKDFyIH7NJJRz[W2ndHnubYIh[2:wc3nzeIVvfGy7IIDyc4R2[2WmIIPp[45q\mmlYX70JIRq\m[ncnXuZ4V{KGKndIfl[Y4h\2WoaYTpcoljKGGwZDD0doFu\XSrbnniJIFtd26nIHPvcZBiemWmIITvJINwdWKrbnH0bY9vKGenZnn0bY5q[iCjbnSgeJJidWW2aX7pZkBqdiCjbHyg[o92eiC|ZX7zbZRqfmViY3XscEBtcW6nczCoR2ZRSUNvMTygdIw1PSxiQ1HQRW4uOiCjbnSgTHBCTi2LSTmuJG5wKGGmZHn0bZZmKGWoZnXjeEB4[XNib3Lz[ZJ3\WRiaX6geIhmKGenZnn0bY5q[iCrboPlcpNqfGm4ZTDvdkBmgGOrdHH0c5J6KGOnbHygcIlv\XNiKF3JRU1R[WOjIHHu[EBRSU6FLUGp NXrMRYFkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5NlE{PTFpPkOwPVIyOzVzPD;hQi=>
Transitional cell carcinoma (TCC) cell lines M1qxcGZ2dmO2aX;uJIF{e2G7 M1LSZlI2KG6P MkLlOk0zPCCq Mn3OR4FvcW6nIGTDR{Bk\WyuIHzpcoV{KGG{ZTDz[Y5{cXSrdnWgeI8hVUWNIHnubIljcXSrb36= NYS2dFhDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GwOFg2PDhpPkOxNFQ5PTR6PD;hQi=>
COLO205 MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEPlcVE4OiCq Mo\JTWM2OCB;IECuNFAyKM7:TR?= MoD2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
HT-29 MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4XidVczKGh? NIrTWFFKSzVyIE2gNE4xODFizszN NHS3OoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
COLO205 NHzNdm9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV3lfJl7PzJiaB?= MojMTWM2OCB;IECuNFAyKM7:TR?= NG\wUYQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
MV522 MornS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHj0Sm44OiCq M1rnTWlEPTBiPTCwMlAxOSEQvF2= NXzsNXFLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
HT-29 MorzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWC3NkBp Mn6yTWM2OCB;IECuNFAzKM7:TR?= MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
MV522 NVPiS4JvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlzNO|IhcA>? NIHhellKSzVyIE2gNE4xODJizszN MoLFQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
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NCI-H727 M2DPXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml7rO|IhcA>? Mm\ETWM2OCB;IECuNFAzKM7:TR?= NEnoXGE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW1417 NGDtOYlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{SxV|czKGh? M{H2WmlEPTBiPTCwMlAxOyEQvF2= M{fINVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
SW1417 NX7oPIJ[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUK3NkBp NITM[XhKSzVyIE2gNE4xODNizszN MlOwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
Calu6 NXnKVllDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUnDcZpFPzJiaB?= MWDJR|UxKD1iMD6wNFMh|ryP NGjNXGk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
LS1034 MkXqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1[0PFczKGh? M1PJZ2lEPTBiPTCwMlAxPCEQvF2= NVyyVHZ[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
SW1463 MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mo\tO|IhcA>? M{HJeWlEPTBiPTCwMlAxPCEQvF2= M4PmdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
SW1463 MlHPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlLGO|IhcA>? NFXjSItKSzVyIE2gNE4xODRizszN Mm\PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
Calu6 NGDtVWFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4Lnc|czKGh? M{TTd2lEPTBiPTCwMlAxPCEQvF2= M3KxTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
LS1034 NIrm[|hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVfjPYE1PzJiaB?= Mlz0TWM2OCB;IECuNFA2KM7:TR?= NV\TbmdIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
RKO M3HzUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEOzWHI4OiCq MY\JR|UxKD1iMD6wNFUh|ryP NGH5dpc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
NCI-H508 MnvUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXq3NkBp MnvmTWM2OCB;IECuNFA5KM7:TR?= NVm5TZZxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
KM12 NF3LW5JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M37TSlczKGh? M2TOVGlEPTBiPTCwMlAyKM7:TR?= MkLHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
A427 MkTwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NY[w[20zPzJiaB?= MVnJR|UxKD1iMD6wNUDPxE1? MojZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
NCI-H1155 NGfSXpVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXLkN3ZDPzJiaB?= MkfaTWM2OCB;IECuNFEh|ryP M4nrfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
HCT8 MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1\sXlczKGh? NVuzcXV5UUN3MDC9JFAvODF2IN88US=> NGTFSoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
MDA-MB-175-VII NH7lT2JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFHFN4o4OiCq M2C5dmlEPTBiPTCwMlAyPiEQvF2= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
A549 NHfZUWFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnjTO|IhcA>? NH;LW2NKSzVyIE2gNE4xOTZizszN MnvDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
RKO MoCxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV3hTGljPzJiaB?= MY\JR|UxKD1iMD6wNVgh|ryP NYGzVXBJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
NCI-H23 MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXL3OpJmPzJiaB?= NEXZZlNKSzVyIE2gNE4xOiEQvF2= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
A427 MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1TGVFczKGh? MVrJR|UxKD1iMD6wNlIh|ryP MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
KM12 NEHtUFlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUm3NkBp NUDsXJFEUUN3MDC9JFAvODJ|IN88US=> NGPiV|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
NCI-H508 M2X1e2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4LWZVczKGh? MVTJR|UxKD1iMD6wNlMh|ryP MlTQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
MDA-MB-231 MlTzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3fxelMh\GG7cx?= M3jGWmdKPTBiPTCwMlAzPSEQvF2= MoHrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
SW837 NYiwfWJXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnKyO|IhcA>? MkS4TWM2OCB;IECuNFI2KM7:TR?= NXHxfXRCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
SW480 M1LEdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHfEbnU4OiCq NYLodogyUUN3MDC9JFAvODJ4IN88US=> M2Hnb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H1355 NWrwPIFuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NW[0Z|QxPzJiaB?= NH;FOoJKSzVyIE2gNE4xOjdizszN MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
NCI-H23 MmLyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEPIb3Q4OiCq MYfJR|UxKD1iMD6wNlkh|ryP MnjoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
EFM19 M2Tyemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{H3c|czKGh? MVLJR|UxKD1iMD6wN{DPxE1? MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
T84 NHX4S|RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFWxOVU4OiCq M2DybmlEPTBiPTCwMlA{KM7:TR?= NIraXZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
A549 NFLZcVlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkfmO|IhcA>? NEn4em9KSzVyIE2gNE4xOzRizszN MnHBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
NCI-H1792 Ml:4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmDyO|IhcA>? MmLCTWM2OCB;IECuNFM2KM7:TR?= MnziQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
SW480 NV3mNWUzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUewRnFlPzJiaB?= M{nmbGlEPTBiPTCwMlA{PyEQvF2= Mlm3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
COR-L23 MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M13BSlczKGh? MYrJR|UxKD1iMD6wN|ch|ryP MlPPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
SW1573 M3HlRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYe3NkBp NHK5NmJKSzVyIE2gNE4xOzhizszN NWXid|kzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
Calu3 NGjxZlRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUfwVIM5PzJiaB?= MXnJR|UxKD1iMD6wN|kh|ryP M3\HTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
HCC827 MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHLNc204OiCq MXvJR|UxKD1iMD6wOEDPxE1? NGXDNmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
HOP62 MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXq3NkBp NGDFTXVKSzVyIE2gNE4xPSEQvF2= MlvOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
NCI-H1355 M4T1U2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHLlXnU4OiCq NXTje4l{UUN3MDC9JFAvODV{IN88US=> NFXZWZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
NCI-H1792 M{PoU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYHGcGdqPzJiaB?= MmPMTWM2OCB;IECuNFU{KM7:TR?= NFO0cWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
HCT8 MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXrmfotpPzJiaB?= NFHUbXBKSzVyIE2gNE4xPTVizszN M{\We|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
T84 NVnVdYZDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF;4O2E4OiCq NUP0SnJIUUN3MDC9JFAvODZzIN88US=> NFnyfY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW900 NYr0[nlCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkfGO|IhcA>? NFzE[2pKSzVyIE2gNE4xPzJizszN NULaVZJzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
SW837 Mn3ES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVTJV29IPzJiaB?= NFnoXoZKSzVyIE2gNE4xPzRizszN NWH1VHQzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
DLD1 MnfLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2r5cVczKGh? M2HRfWlEPTBiPTCwMlA6OyEQvF2= NXfENmRiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
MDA-MB-175-VII MmOyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUToU4k2PzJiaB?= NFHhd5VKSzVyIE2gNE4xQTZizszN NInDVlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW900 MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIj6SVY4OiCq MYjJR|UxKD1iMD6xNlch|ryP NFu4c3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
Calu3 NIDXb3lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHjGc204OiCq NXTHeHM6UUN3MDC9JFAvOTV6IN88US=> MnGzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
COR-L23 NFL6c2lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX[3NkBp MV\JR|UxKD1iMD6zNlkh|ryP NF;Oeog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
DLD1 M4G4V2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3;DUlczKGh? MXTJR|UxKD1iMD62N|Ih|ryP NVf0TGVlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
ERRα / IDH3 / c-Myc / Cyclin D1; 

PubMed: 30185207     


WB for ERRα, IDH3A, c-Myc and Cyclin D1 in the HCT116 and SW480 cells treated with the indicated concentrations of trametinib (0–100 nM) or DMSO for 48 h. 

pERK /ERK / pS6 / S6 ; 

PubMed: 29133622     


BRAF/NRAS-WT cell lines were treated with vehicle, ceritinib, trametinib or ceritinib-trametinib for 24h before extraction of protein and Western blot for pERK or pS6. Numbers above pS6 indicate the densitometry measurements expressed as a proportion of total S6. 

β-catenin; 

PubMed: 28422736     


The antibodies against phospho-ERK (p-ERK), total ERK (t-ERK) and β-catenin were used to determine the effect of trametinib on the levels of p-ERK and β-catenin in the indicated cells. GAPDH was used as a loading control.

30185207 29133622 28422736
Growth inhibition assay
Cell proliferation; 

PubMed: 30185207     


Cell proliferation was measured using the Cell Counting Kit-8 (CCK-8) assay in the HCT116 and SW480 cells treated with trametinib at 25 nm, 50 nM and 100 nM for 3 d.

MTT assay; 

PubMed: 26832408     


Percent viability of A549 cells determined by MTT assay plotted on a logarithmic molar dose curve scale. Shown are trametinib and fluvastatin single drug dose curves and fluvastatin dose curve with fixed trametinib dosing.

30185207 26832408
Immunofluorescence
phospho-PR(S345); 

PubMed: 29237804     


IF of the nuclear phospho-PR (S345) in ISHIKAWA cells treated with 10 μM onapristone, 100nM trametinib, or a combination for 24 hours.

β-catenin; 

PubMed: 28422736     


Immunofluorescence assay was used to investigate the effect of trametinib on subcellular localization of β-catenin in NOZ and GBC-SD cells. Red color represents nuclear and cytoplasmic staining of β-catenin, and blue color represents Hoeschst 33342 staining for nuclei. Scale bars, 200 μm.

29237804 28422736
In vivo Oral administration of GSK1120212 at 0.3 mg/kg or 1 mg/kg once daily for 14 days is effective in inhibiting the HT-29 xenograft growth, and 1 mg/kg of GSK1120212 almost completely blocks the tumor increase. The phosphorylation of ERK1/2 is completely inhibited in the established tumor tissues by single oral dose of 1 mg/kg GSK1120212, and both p15INK4b and p27KIP1 protein levels are upregulated after 14 days of treatment with GSK1120212. In the COLO205 xenograft model, tumor regression is observed even at a dose of 0.3 mg/kg. At a dose of 1 mg/kg, a complete regression is obtained in 4 out of 6 mice in which the tumor degenerates to the point that tumor volume is not measurable. [1] Administration of GSK1120212 at 0.1 mg/kg almost completely suppresses adjuvant-induced arthritis (AIA) and type II collagen-induced arthritis (CIA) in Lewis rats or DBA1/J mice, respectively. [2]

Protocol

Kinase Assay:[1]
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Raf-MEK-ERK cascade kinase assay:

Non-phosphorylated myelin basic protein (MBP) is coated onto an ELISA plate, and the active form of B-Raf/c-Raf is mixed with unphosphorylated MEK1/MEK2 and ERERK2 in 10 μM ATP and 12.5 mM MgCl2 containing MOPS buffer in the presence of various concentrations of GSK1120212. The phosphorylation of MBP is detected by the anti-phospho-MBP antibody.
Cell Research:[1]
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  • Cell lines: HT-29, HCT-15, HCT116, COLO205, LS-174T, SW480, SW620, T84, LoVo and COLO320
  • Concentrations: Dissolved in DMSO, final concentrations ~10 μM
  • Incubation Time: 3 or 4 days
  • Method: Exponentially growing cells are precultured in 96-well tissue culture plates for 24 hours and then exposed to GSK1120212. Cell growth is determined by an in vitro toxicology assay kit, sulforhodamine B based. For apoptosis assay, both floating and adherent cells are collected and fixed with 70% ethanol. After washing with PBS, the cells are suspended in 100 μg/mL RNase and 25 μg/mL propidium iodide (PI) and incubated at 37 °C for 30 minutes in the dark. The DNA content of each single cell is determined using the flow cytometer Cytomics FC500 or Guava EasyCyte plus.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: Female BALB/c-nu/nu mice inoculated subcutaneously with HT-29 or COLO205 cells
  • Dosages: ~1 mg/kg/day
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 22 mg/mL warmed (35.74 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+corn oil
For best results, use promptly after mixing.
3mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 615.39
Formula

C26H23FIN5O4

CAS No. 871700-17-3
Storage powder
in solvent
Synonyms JTP-74057, Mekinist
Smiles CC1=C2C(=C(N(C1=O)C)NC3=C(C=C(C=C3)I)F)C(=O)N(C(=O)N2C4=CC=CC(=C4)NC(=O)C)C5CC5

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • 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):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04547946 Not yet recruiting Drug: dabrafenib + trametinib Malignant Melanoma Novartis Pharmaceuticals|Novartis April 30 2021 --
NCT04059224 Recruiting Drug: Trametinib|Drug: Dabrafenib Stage IV Melanoma|Stage III Melanoma Universitair Ziekenhuis Brussel January 28 2019 Phase 2
NCT03668431 Unknown status Drug: Dabrafenib|Drug: Trametinib|Drug: PDR001 Metastatic Colorectal Cancer Massachusetts General Hospital|Novartis|Stand Up To Cancer October 15 2018 Phase 2
NCT03363217 Recruiting Drug: Trametinib Low-grade Glioma|Plexiform Neurofibroma|Central Nervous System Glioma St. Justine''s Hospital|Montreal Children''s Hospital of the MUHC|CHU de Quebec-Universite Laval August 16 2018 Phase 2
NCT03516214 Recruiting Drug: EGF816|Drug: Trametinib Bronchial Neoplasms University of Cologne April 25 2018 Phase 1
NCT03428126 Active not recruiting Drug: Durvalumab|Drug: Trametinib Malignant Neoplasms of Digestive Organs|Colorectal Cancer|Colon Cancer M.D. Anderson Cancer Center|MedImmune LLC|AstraZeneca|Novartis March 21 2018 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

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

  • Answer:

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

  • Question 2:

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

  • Answer:

    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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID