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 1090 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 MmrsSpVv[3Srb36gZZN{[Xl? NGPHdGEyODEkgJnuUS=> M4f1[lI1KGh? MoDveJJidWW2aX7pZkBkd3WuZDDk[YNz\WG|ZTDZRXAhdGW4ZXzzJIFv\CCrbnjpZol1KEyPQj3pcoR2[2WmIGnBVEB2eHKnZ4XsZZRqd25iaX6gUWRCNU2ELUKzNUwhW1dzMUG2JIFv\CCVV{S4NEBk\Wyucx?= Ml\YQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB6M{O2OlUoRjNyOEOzOlY2RC:jPh?=
RG7388-resistant U87MG cells MmXZSpVv[3Srb36gZZN{[Xl? MWexNEBvVQ>? MWCyOEBp MkTVSG1UVw>? MmHWWJJidWW2aX7pZkB1emWjdH3lcpQhemWmdXPl[EB1cGViaX72ZZNqfmVicHjlco91gXCnIH;mJHJIPzN6ODDy[ZNqe3SjboSgZ4VtdHNw NH\ROXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEK3OFk5PCd-M{CyO|Q6QDR:L3G+
BJAB cells M4XWWWZ2dmO2aX;uJIF{e2G7 NXq1TFZvOC5yMd88US=> Ml3JNlQhcA>? M1PZZVAvODFizszNJJRz[W2ndHnubYIh\W[oZXP0bZZmdHlic4XwdJJme3OnZDD0bIUhTVKNIHj5dIVz[WO2aY\heIlwdiCrbjDCTmFDKGOnbHzzJINifXOnZDDifUB1cGViY3;tZolv\WRidILlZZRu\W62IH;mJGJMVTF{MDDhcoQhTGGwdYPldpRq[i5? MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl2N{W3Okc,OzB7NEe1O|Y9N2F-
Human PDAC cell lines (MIA-PACA, PANC-1, CFPAC-1, PL45, CAPAN-2 and HPAF-II) MU\GeY5kfGmxbjDhd5NigQ>? NXT5eFdsOTBibl2gc5IhOTByIH7N M17IPVMu\GG7czDvdkA3NWSjeYO= M3XWc3Rp\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 NWq1WWlrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5NlE{PTFpPkOwPVIyOzVzPD;hQi=>
Transitional cell carcinoma (TCC) cell lines MYDGeY5kfGmxbjDhd5NigQ>? NHr6[5YzPSCwTR?= NWrEfVZUPi1{NDDo Mn;pR4FvcW6nIGTDR{Bk\WyuIHzpcoV{KGG{ZTDz[Y5{cXSrdnWgeI8hVUWNIHnubIljcXSrb36= NFfhWIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUC0PFU1QCd-M{GwOFg2PDh:L3G+
COLO205 M4PkZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4XrbFczKGh? NYfzUYtsUUN3MDC9JFAvODBzIN88US=> NECwd2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
HT-29 NYr2R|VmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIXiZlU4OiCq NFHBU2NKSzVyIE2gNE4xODFizszN M4\JNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
COLO205 M2HPZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUjmTpNIPzJiaB?= NWTMdWtiUUN3MDC9JFAvODBzIN88US=> NGXWSmk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
MV522 MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYC3NkBp M4fqOmlEPTBiPTCwMlAxOSEQvF2= NEnUUmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
HT-29 M3X4NWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVHVRXFJPzJiaB?= MULJR|UxKD1iMD6wNFIh|ryP MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
MV522 MonzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3HaeFczKGh? NIHZXppKSzVyIE2gNE4xODJizszN M3vSflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H727 M3;oW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mlv5O|IhcA>? M4[0SWlEPTBiPTCwMlAxOiEQvF2= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
NCI-H727 MnX2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXL1TYhQPzJiaB?= M2nCS2lEPTBiPTCwMlAxOiEQvF2= NVLQ[m81RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
SW1417 Mlq3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGDyNnI4OiCq NU\VO4xxUUN3MDC9JFAvODB|IN88US=> Ml\LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
SW1417 NGTV[INIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXy3NkBp M2rteGlEPTBiPTCwMlAxOyEQvF2= NI\zeGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
Calu6 M4HWc2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXG3NkBp NVLGUIk1UUN3MDC9JFAvODB|IN88US=> NWDa[2t2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
LS1034 M{XvNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVm3NkBp NXrT[|ZNUUN3MDC9JFAvODB2IN88US=> NWfQ[lQ2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
SW1463 MmPvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGHvXGk4OiCq NI\PXXBKSzVyIE2gNE4xODRizszN NIm4UJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW1463 NFy5bGNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2jNOlczKGh? MULJR|UxKD1iMD6wNFQh|ryP NX\tcYJrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
Calu6 NHXPUGRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NITFT5g4OiCq M3zPSWlEPTBiPTCwMlAxPCEQvF2= NE[5bII9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
LS1034 MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXq3NkBp NWi5[VFDUUN3MDC9JFAvODB3IN88US=> M2\pfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
RKO M2DrOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2jq[lczKGh? M3nz[GlEPTBiPTCwMlAxPSEQvF2= M2\TXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H508 M13qXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV3PW|ZSPzJiaB?= MUnJR|UxKD1iMD6wNFgh|ryP NI\0eY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
KM12 NX7We2prT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVT2W5RVPzJiaB?= NHLUWpNKSzVyIE2gNE4xOSEQvF2= Ml3WQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
A427 MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYj0eHlXPzJiaB?= MknSTWM2OCB;IECuNFEh|ryP NVnCWJVORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
NCI-H1155 MnXVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXnFeHRGPzJiaB?= MnHCTWM2OCB;IECuNFEh|ryP NVm0enhrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
HCT8 M4jacWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn\PO|IhcA>? MnXnTWM2OCB;IECuNFE1KM7:TR?= NGTVRow9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
MDA-MB-175-VII NHXCcpBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVuwVppnPzJiaB?= NELoVHVKSzVyIE2gNE4xOTZizszN M3;sUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
A549 M4nuZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M13rNVczKGh? Mn3ETWM2OCB;IECuNFE3KM7:TR?= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
RKO NXjqTGx7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFTtRVY4OiCq NXrKVnFDUUN3MDC9JFAvODF6IN88US=> NUn2PGJbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
NCI-H23 M{XKfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUDwXZp3PzJiaB?= MXXJR|UxKD1iMD6wNkDPxE1? M4\nRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
A427 M3zNXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH7GSHI4OiCq M1zKWGlEPTBiPTCwMlAzOiEQvF2= NH;pTok9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
KM12 NIfwTZhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVS3NkBp M3zObGlEPTBiPTCwMlAzOyEQvF2= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
NCI-H508 NF3sWmJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH\IbmE4OiCq NVzZe3NVUUN3MDC9JFAvODJ|IN88US=> NIrJeGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
MDA-MB-231 MnnSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXv0[mpoOyCmYYnz NXPQXJN2T0l3MDC9JFAvODJ3IN88US=> NWHES|hkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
SW837 NWqzNG8xT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1fEVVczKGh? NGjF[nhKSzVyIE2gNE4xOjVizszN NUPSNIdnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
SW480 M1LyVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFTZSI84OiCq NI\XU|dKSzVyIE2gNE4xOjZizszN MlnaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
NCI-H1355 M3S5W2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGfCRWc4OiCq NVnvdXB4UUN3MDC9JFAvODJ5IN88US=> MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
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A549 NYXiWVM6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M13DbVczKGh? NXHSd|JmUUN3MDC9JFAvODN2IN88US=> MnPnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
NCI-H1792 M2\vZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4npcVczKGh? M4rvZWlEPTBiPTCwMlA{PSEQvF2= MXq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
SW480 NHHmSIFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYK3NkBp MlfITWM2OCB;IECuNFM4KM7:TR?= NH7Ncoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
COR-L23 NXXlVXBrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUW3NkBp MlntTWM2OCB;IECuNFM4KM7:TR?= NVXQfpk5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
SW1573 NIfWZ2JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4HaSFczKGh? NYHRZ2tlUUN3MDC9JFAvODN6IN88US=> NWHucFhHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
Calu3 MnnCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIP5SHY4OiCq NWXtPWw4UUN3MDC9JFAvODN7IN88US=> M1HsUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
HCC827 NV[3SY1[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{nhWVczKGh? MoHLTWM2OCB;IECuNFQh|ryP NETDcG09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
HOP62 NHjwb|RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M37YOFczKGh? M1T1dmlEPTBiPTCwMlA2KM7:TR?= MlezQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
NCI-H1355 MmfBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWe3NkBp NVHFS4RRUUN3MDC9JFAvODV{IN88US=> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
NCI-H1792 NFPnN|NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGjlcmM4OiCq MXfJR|UxKD1iMD6wOVMh|ryP NYCzRZEzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
HCT8 MlXoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3W4c|czKGh? NU\EUpVYUUN3MDC9JFAvODV3IN88US=> M3HUXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
T84 NV31fGJ6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX7UTlQ{PzJiaB?= NIewOHhKSzVyIE2gNE4xPjFizszN NG\GWJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW900 M4qxSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mnu4O|IhcA>? M4\q[2lEPTBiPTCwMlA4OiEQvF2= NIPVXY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW837 NH;LRWdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYrnfI04PzJiaB?= NVPSeYdiUUN3MDC9JFAvODd2IN88US=> NGTadG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
DLD1 MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlzUO|IhcA>? M2XaZWlEPTBiPTCwMlA6OyEQvF2= MnvJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
MDA-MB-175-VII NFzBWFBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NU\DNoJ2PzJiaB?= NUnjcoVkUUN3MDC9JFAvODl4IN88US=> NIGzV5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW900 NF\NZotIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX23NkBp MX3JR|UxKD1iMD6xNlch|ryP M{n5VlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
Calu3 NGqxXFdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXXuXWQ1PzJiaB?= MULJR|UxKD1iMD6xOVgh|ryP NUfLN29rRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
COR-L23 M2HMVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NU\0WXFGPzJiaB?= MofITWM2OCB;IECuN|I6KM7:TR?= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
DLD1 MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUe3NkBp NEfiZ2pKSzVyIE2gNE43OzJizszN M336WVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
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
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. December 2022 Phase 1|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) December 2022 Phase 1
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 2022-11-29)

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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