Trametinib (GSK1120212)

Catalog No.S2673 Synonyms: JTP-74057, Mekinist

For research use only.

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.

Trametinib (GSK1120212) Chemical Structure

CAS No. 871700-17-3

Selleck's Trametinib (GSK1120212) has been cited by 1072 publications

Purity & Quality Control

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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 NHvlS|JHfW6ldHnvckBie3OjeR?= MkfsNVAx6oDLbl2= NFHhbXIzPCCq NHS3Z5F1emGvZYTpcoljKGOxdXzkJIRm[3KnYYPlJHlCWCCuZY\lcJMh[W6mIHnubIljcXRiTF3CMYlv\HWlZXSgXWFRKHWycnXneYxifGmxbjDpckBOTEFvTVKtNlMyNCCVV{GxNVYh[W6mIGPXOFgxKGOnbHzz M17JNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOEOzOlY2Lz5|MEizN|Y3PTxxYU6=
RG7388-resistant U87MG cells NUToeWdFTnWwY4Tpc44h[XO|YYm= NF7IWJMyOCCwTR?= NHrEcIEzPCCq NEHXOlBFVVOR NF7RU|NVemGvZYTpcoljKHS{ZXH0cYVvfCC{ZXT1Z4VlKHSqZTDpcpZie2m4ZTDwbIVvd3S7cHWgc4YhWkd5M{i4JJJme2m|dHHueEBk\Wyucz6= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ5NEm4OEc,OzB{N{S5PFQ9N2F-
BJAB cells MV;GeY5kfGmxbjDhd5NigQ>? MUewMlAy|ryP M2XDc|I1KGh? NE\nZm0xNjBzIN88UUB1emGvZYTpcoljKGWoZnXjeIl3\Wy7IIP1dJBz\XO|ZXSgeIhmKEWUSzDofZBmemGldHn2ZZRqd25iaX6gRmpCSiClZXzsd{Bk[XW|ZXSgZpkhfGinIHPvcYJqdmWmIITy[YF1dWWwdDDv[kBDU01zMkCgZY5lKESjboXz[ZJ1cWJw MlnUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB7NEe1O|YoRjNyOUS3OVc3RC:jPh?=
Human PDAC cell lines (MIA-PACA, PANC-1, CFPAC-1, PL45, CAPAN-2 and HPAF-II) NFntU3JHfW6ldHnvckBie3OjeR?= NUHhR|JVOTBibl2gc5IhOTByIH7N MVezMYRigXNib4KgOk1l[Xm| NGHuPYFVcGViY3;uZ4VvfHKjdHnvckBw\iBzMDDuUUB1emGvZYTpcoljKGOxboPpd5RmdnSueTDwdo9lfWOnZDDzbYdvcW[rY3HueEBlcW[oZYLlcoNmeyCkZYT3[YVvKGenZnn0bY5q[iCjbnSgeJJidWW2aX7pZkBidG:wZTDjc41x[XKnZDD0c{Bkd22kaX7heIlwdiCpZX\peIlvcWJiYX7kJJRz[W2ndHnubYIhcW5iYXzsJIZwfXJic3Xud4l1cX[nIHPlcIwhdGmwZYOgLGNHWEGFLUGsJJBtPDVuIFPBVGFPNTJiYX7kJGhRSUZvSVmpMkBPdyCjZHTpeIl3\SCnZn\lZ5Qhf2G|IH;id4VzfmWmIHnuJJRp\SCpZX\peIlvcWJiaX7z[Y5{cXSrdnWgc5Ih\XilaYTheI9zgSClZXzsJIxqdmW|IDjNTWEuWGGlYTDhcoQhWEGQQz2xLS=> MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl{MUO1NUc,OzB7MkGzOVE9N2F-
Transitional cell carcinoma (TCC) cell lines M3HFdWZ2dmO2aX;uJIF{e2G7 NUnKNYN1OjVibl2= M1LsR|YuOjRiaB?= NHTneFhE[W6rbnWgWGNEKGOnbHygcIlv\XNiYYLlJJNmdnOrdHn2[UB1dyCPRVugbY5pcWKrdHnvci=> M1mwZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzMES4OVQ5Lz5|MUC0PFU1QDxxYU6=
COLO205 NFnTPFZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXm3NkBp M{PrcGlEPTBiPTCwMlAxOSEQvF2= MmHzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
HT-29 M4\uWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4e4c|czKGh? M3G3XmlEPTBiPTCwMlAxOSEQvF2= MmHLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
COLO205 NX3TeII2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWG3NkBp M1zyemlEPTBiPTCwMlAxOSEQvF2= MmjpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
MV522 MlLsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUG3NkBp MVTJR|UxKD1iMD6wNFEh|ryP NUP5PIsxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
HT-29 M1n6[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWDxUppwPzJiaB?= MXzJR|UxKD1iMD6wNFIh|ryP MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
MV522 Mnn5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnrEO|IhcA>? NFL5[WJKSzVyIE2gNE4xODJizszN NI\sW5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
NCI-H727 Mn7wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3zUZlczKGh? NE\HT25KSzVyIE2gNE4xODJizszN MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
NCI-H727 MorMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1\nclczKGh? NWKzZ3NPUUN3MDC9JFAvODB{IN88US=> NWD4SJg6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
SW1417 NHXofVRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MU[3NkBp NFOwbZFKSzVyIE2gNE4xODNizszN MmH2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
SW1417 M3z2cmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlHjO|IhcA>? M{TtTmlEPTBiPTCwMlAxOyEQvF2= MnPaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
Calu6 MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MljCO|IhcA>? NX7WRYMxUUN3MDC9JFAvODB|IN88US=> NEXJdJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
LS1034 NGGzO5hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYq3NkBp M3HvUGlEPTBiPTCwMlAxPCEQvF2= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
SW1463 M3PPcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF\LTVA4OiCq MU\JR|UxKD1iMD6wNFQh|ryP M{HqN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
SW1463 MojES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWi3NkBp MnOzTWM2OCB;IECuNFA1KM7:TR?= MkjnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
Calu6 NGf5fmxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmC1O|IhcA>? M3K3XWlEPTBiPTCwMlAxPCEQvF2= M3zhfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
LS1034 NEHGUlVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV63NkBp MkfHTWM2OCB;IECuNFA2KM7:TR?= M2fjOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
RKO M3vUS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXrrWXdTPzJiaB?= NGPyfoRKSzVyIE2gNE4xODVizszN MnLYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
NCI-H508 MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnXYO|IhcA>? M1znN2lEPTBiPTCwMlAxQCEQvF2= NVXwRmFuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
KM12 NFHZPWlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHTFSpc4OiCq NVvH[oc6UUN3MDC9JFAvODFizszN NYrERZo2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
A427 MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGq2XZk4OiCq MlGzTWM2OCB;IECuNFEh|ryP MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
NCI-H1155 NXrqV2JkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnfEO|IhcA>? NE[zV|JKSzVyIE2gNE4xOSEQvF2= M{DZTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
HCT8 MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV[z[HBZPzJiaB?= M1jaTGlEPTBiPTCwMlAyPCEQvF2= MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
MDA-MB-175-VII MnvuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWPSdFFMPzJiaB?= NHLEXZJKSzVyIE2gNE4xOTZizszN MlnqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
A549 NU\rS2w{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUiyWoV5PzJiaB?= NWCyRpBIUUN3MDC9JFAvODF4IN88US=> NEPwOIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
RKO MmLHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkLpO|IhcA>? MljuTWM2OCB;IECuNFE5KM7:TR?= MnzjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
NCI-H23 NX;Bd3Y4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV7zenBrPzJiaB?= Mn\CTWM2OCB;IECuNFIh|ryP MorEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
A427 MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUHZNY9jPzJiaB?= MVrJR|UxKD1iMD6wNlIh|ryP NHXveIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
KM12 MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3eyfFczKGh? MYnJR|UxKD1iMD6wNlMh|ryP NEX6bVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
NCI-H508 NYPlNmxqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGTWNXU4OiCq MXPJR|UxKD1iMD6wNlMh|ryP NGfDOYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
MDA-MB-231 MlHIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{fwWlMh\GG7cx?= M3v3T2dKPTBiPTCwMlAzPSEQvF2= M1G0[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
SW837 NUjpZYx[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmfGO|IhcA>? M1XkPWlEPTBiPTCwMlAzPSEQvF2= MlLwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
SW480 M1\sdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVzSeIRLPzJiaB?= NWSzNXpxUUN3MDC9JFAvODJ4IN88US=> M3X4TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H1355 NWriTlJ6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGG0RZU4OiCq MkC3TWM2OCB;IECuNFI4KM7:TR?= M1rG[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H23 MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFLCUYg4OiCq MY\JR|UxKD1iMD6wNlkh|ryP NVrQeHB3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
EFM19 NYXhdFk1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWe3NkBp M1HGUGlEPTBiPTCwMlA{KM7:TR?= Mn3QQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
T84 MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnHtO|IhcA>? M2D5NWlEPTBiPTCwMlA{KM7:TR?= NFzYOGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
A549 M4POVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUHlfpFwPzJiaB?= NEfVNohKSzVyIE2gNE4xOzRizszN MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
NCI-H1792 NVfkdFhTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGTofpY4OiCq M1m1Z2lEPTBiPTCwMlA{PSEQvF2= Mo\ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
SW480 NHXFUYNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{X2NFczKGh? NYLVd2wzUUN3MDC9JFAvODN5IN88US=> MnXGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
COR-L23 NHu3VFBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MljlO|IhcA>? NHq2UW9KSzVyIE2gNE4xOzdizszN NE\IO2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW1573 NXn0WJRvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEDLNng4OiCq M4j2W2lEPTBiPTCwMlA{QCEQvF2= Mof1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
Calu3 NF21U2NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUWwU4doPzJiaB?= MVrJR|UxKD1iMD6wN|kh|ryP M{DMOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
HCC827 MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnfrO|IhcA>? MkfCTWM2OCB;IECuNFQh|ryP NF\xfWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
HOP62 MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXPnTZJtPzJiaB?= NH\O[YZKSzVyIE2gNE4xPSEQvF2= NWfGcVRZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
NCI-H1355 Mn\FS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXq3NkBp M{TRUmlEPTBiPTCwMlA2OiEQvF2= M2jtfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H1792 MnXNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGmyTJM4OiCq MXXJR|UxKD1iMD6wOVMh|ryP M{C4XFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
HCT8 MofFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXSzfW9oPzJiaB?= MXXJR|UxKD1iMD6wOVUh|ryP MlfjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
T84 M2PWTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkXPO|IhcA>? NIDOS4pKSzVyIE2gNE4xPjFizszN M{jiT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
SW900 NYT1eZFqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkHaO|IhcA>? MlfFTWM2OCB;IECuNFczKM7:TR?= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
SW837 MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXy3NkBp NUO4UnFWUUN3MDC9JFAvODd2IN88US=> NWjGWHlSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
DLD1 MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUm3NkBp MnnWTWM2OCB;IECuNFk{KM7:TR?= NYPQO|M6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
MDA-MB-175-VII M2rEfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlroO|IhcA>? Mm[4TWM2OCB;IECuNFk3KM7:TR?= M2nY[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
SW900 M{DIOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXvPVHByPzJiaB?= M{nVT2lEPTBiPTCwMlEzPyEQvF2= NVHBWGFXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
Calu3 NGSwfIJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlzDO|IhcA>? NIradJJKSzVyIE2gNE4yPThizszN M3rubFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
COR-L23 MoDZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVj1U4doPzJiaB?= NVTncpNUUUN3MDC9JFAvOzJ7IN88US=> NYHPS3FURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
DLD1 MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVW3NkBp MWnJR|UxKD1iMD62N|Ih|ryP NWfrfJNYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
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
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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[1]
  • Animal Models: Female BALB/c-nu/nu mice inoculated subcutaneously with HT-29 or COLO205 cells
  • Dosages: ~1 mg/kg/day
  • Administration: Orally

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 615.39
Formula

C26H23FIN5O4

CAS No. 871700-17-3
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04961619 Not yet recruiting Drug: dabrafenib|Drug: trametinib Melanoma Novartis Pharmaceuticals|Novartis February 1 2022 --
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) January 18 2022 Phase 2
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) January 2022 Phase 1
NCT04547946 Recruiting Drug: dabrafenib + trametinib Malignant Melanoma Novartis Pharmaceuticals|Novartis October 15 2021 --
NCT05071183 Recruiting Drug: TPX-0005|Drug: Trametinib KRAS Mutation-Related Tumors|Metastatic Solid Tumor|Advanced Solid Tumor Turning Point Therapeutics Inc. September 23 2021 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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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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