Trametinib (GSK1120212)

For research use only.

Catalog No.S2673 Synonyms: JTP-74057, Mekinist

936 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 936 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 NI\3O4xHfW6ldHnvckBie3OjeR?= NEjySXMyODEkgJnuUS=> NH\JOWszPCCq NFzBd5F1emGvZYTpcoljKGOxdXzkJIRm[3KnYYPlJHlCWCCuZY\lcJMh[W6mIHnubIljcXRiTF3CMYlv\HWlZXSgXWFRKHWycnXneYxifGmxbjDpckBOTEFvTVKtNlMyNCCVV{GxNVYh[W6mIGPXOFgxKGOnbHzz NGfTV4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEizN|Y3PSd-M{C4N|M3PjV:L3G+
RG7388-resistant U87MG cells NWO5XJBITnWwY4Tpc44h[XO|YYm= MmPjNVAhdk1? NETPWGkzPCCq NGTjemZFVVOR MnvVWJJidWW2aX7pZkB1emWjdH3lcpQhemWmdXPl[EB1cGViaX72ZZNqfmVicHjlco91gXCnIH;mJHJIPzN6ODDy[ZNqe3SjboSgZ4VtdHNw MlTmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{N{S5PFQoRjNyMke0PVg1RC:jPh?=
BJAB cells NETCd4VHfW6ldHnvckBie3OjeR?= MoXHNE4xOc7:TR?= NYmzbY5FOjRiaB?= M3XGe|AvODFizszNJJRz[W2ndHnubYIh\W[oZXP0bZZmdHlic4XwdJJme3OnZDD0bIUhTVKNIHj5dIVz[WO2aY\heIlwdiCrbjDCTmFDKGOnbHzzJINifXOnZDDifUB1cGViY3;tZolv\WRidILlZZRu\W62IH;mJGJMVTF{MDDhcoQhTGGwdYPldpRq[i5? MofLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB7NEe1O|YoRjNyOUS3OVc3RC:jPh?=
Human PDAC cell lines (MIA-PACA, PANC-1, CFPAC-1, PL45, CAPAN-2 and HPAF-II) M{LySmZ2dmO2aX;uJIF{e2G7 NGfVfosyOCCwTTDvdkAyODBibl2= NHi5fnA{NWSjeYOgc5IhPi2mYYnz MUHUbIUh[2:wY3XueJJifGmxbjDv[kAyOCCwTTD0doFu\XSrbnniJINwdnOrc4TlcpRtgSCycn;keYNm\CC|aXfubYZq[2GwdDDkbYZn\XKnbnPld{Bj\XS5ZXXuJIdm\mm2aX7pZkBidmRidILhcYV1cW6rYjDhcI9v\SClb33wZZJm\CC2bzDjc41jcW6jdHnvckBo\W[rdHnubYIh[W6mIITyZY1mfGmwaXKgbY4h[WyuIH\veZIhe2Wwc3n0bZZmKGOnbHygcIlv\XNiKFPGVGFENTFuIIDsOFUtKEODUFHOMVIh[W6mIFjQRWYuUUlrLjDOc{Bi\GSrdHn2[UBm\m[nY4Sge4F{KG:kc3XyeoVlKGmwIITo[UBo\W[rdHnubYIhcW6|ZX7zbZRqfmVib4Kg[ZhkcXSjdH;yfUBk\WyuIHzpcoV{KCiPSVGtVIFk[SCjbnSgVGFPSy1zKR?= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl{MUO1NUc,OzB7MkGzOVE9N2F-
Transitional cell carcinoma (TCC) cell lines M2\qfGZ2dmO2aX;uJIF{e2G7 NGrYZ5UzPSCwTR?= MYm2MVI1KGh? M1\QWmNidmmwZTDUR2Mh[2WubDDsbY5meyCjcnWgd4Vve2m2aY\lJJRwKE2HSzDpcohq[mm2aX;u NUjvNlIyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GwOFg2PDhpPkOxNFQ5PTR6PD;hQi=>
COLO205 Mo\DS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH22fFI4OiCq MljsTWM2OCB;IECuNFAyKM7:TR?= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
HT-29 NV;ndINZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEPlfYQ4OiCq M1XpZmlEPTBiPTCwMlAxOSEQvF2= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
COLO205 NInBWYdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{noc|czKGh? MmHnTWM2OCB;IECuNFAyKM7:TR?= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
MV522 MojwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXnHZYh{PzJiaB?= Mn7mTWM2OCB;IECuNFAyKM7:TR?= NGi2fXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
HT-29 M4H4Nmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUG2bWt1PzJiaB?= MYPJR|UxKD1iMD6wNFIh|ryP MnLSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
MV522 MlzwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGC0OXQ4OiCq NGDqWnNKSzVyIE2gNE4xODJizszN M2\Mc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H727 MnnMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXO3NkBp MWTJR|UxKD1iMD6wNFIh|ryP M1HjO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H727 MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MknjO|IhcA>? Mm[wTWM2OCB;IECuNFAzKM7:TR?= NHjjcoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW1417 M2PVbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUj3ZnZMPzJiaB?= NEW2cFlKSzVyIE2gNE4xODNizszN M3:5RVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
SW1417 NF\uRmtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGW0bFA4OiCq NFrqWXZKSzVyIE2gNE4xODNizszN NIfvNXg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
Calu6 NFjzUmNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3vL[|czKGh? M{nJVWlEPTBiPTCwMlAxOyEQvF2= MoXxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
LS1034 MkDOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVi3NkBp NWjo[Yl{UUN3MDC9JFAvODB2IN88US=> NYnFcINGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
SW1463 Mor4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlnhO|IhcA>? NGXPWnlKSzVyIE2gNE4xODRizszN MmDzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
SW1463 Mo\JS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3XFWlczKGh? NVHDR5RlUUN3MDC9JFAvODB2IN88US=> Ml64QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
Calu6 MlzVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{H5PVczKGh? MWrJR|UxKD1iMD6wNFQh|ryP NYjQN|lZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
LS1034 NHe2cmlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3\oW|czKGh? Ml;tTWM2OCB;IECuNFA2KM7:TR?= M3fsZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
RKO NXW2eXdHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYflOXFxPzJiaB?= NHvrbJNKSzVyIE2gNE4xODVizszN M3rnVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H508 NVzNbY45T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEiyenI4OiCq NXfVR2pZUUN3MDC9JFAvODB6IN88US=> NVXzO411RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
KM12 M3;Hc2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUfGT4ZrPzJiaB?= MmTPTWM2OCB;IECuNFEh|ryP MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
A427 M1HRcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4PieVczKGh? Ml\pTWM2OCB;IECuNFEh|ryP NELXOpo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
NCI-H1155 NFL0UINIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXG3NkBp NFPB[4VKSzVyIE2gNE4xOSEQvF2= M2fXRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
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MDA-MB-175-VII NWDofVFuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{i3W|czKGh? MlPOTWM2OCB;IECuNFE3KM7:TR?= MVG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
A549 Mli4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NX;TdFFvPzJiaB?= NYrRfHVuUUN3MDC9JFAvODF4IN88US=> MnTJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
RKO NXnISJBlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGHCcHc4OiCq NInQcFhKSzVyIE2gNE4xOThizszN Mn64QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
NCI-H23 MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUi3NkBp NVfhN|hVUUN3MDC9JFAvODJizszN M{jpT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
A427 Mn;uS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXWwR5ByPzJiaB?= NX6yZVY{UUN3MDC9JFAvODJ{IN88US=> NVW1VGtNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
KM12 NXrSW41PT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVHNU5hlPzJiaB?= MlXtTWM2OCB;IECuNFI{KM7:TR?= MmjyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
NCI-H508 MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXHnNXRnPzJiaB?= NVTEVJZNUUN3MDC9JFAvODJ|IN88US=> NVLHRVVHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
MDA-MB-231 NVHDS4VNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEnkUZA{KGSjeYO= MnLxS2k2OCB;IECuNFI2KM7:TR?= NV;jUJRtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
SW837 NX3wbFJyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYG3NkBp MVjJR|UxKD1iMD6wNlUh|ryP MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
SW480 MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHPY[ZA4OiCq NFziXYJKSzVyIE2gNE4xOjZizszN MlyzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
NCI-H1355 MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFLtbIg4OiCq MmXwTWM2OCB;IECuNFI4KM7:TR?= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
NCI-H23 M3O4dGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXTWeFhJPzJiaB?= NFjaXppKSzVyIE2gNE4xOjlizszN M1P5blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
EFM19 M{Pk[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4ribVczKGh? MmTvTWM2OCB;IECuNFMh|ryP NWL6UZZsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
T84 M1\nSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnK5O|IhcA>? MoW2TWM2OCB;IECuNFMh|ryP MmTIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
A549 MnjZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{jndlczKGh? NHj4XGRKSzVyIE2gNE4xOzRizszN M4rFelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H1792 MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVS2TYhjPzJiaB?= M2HOcWlEPTBiPTCwMlA{PSEQvF2= NEP3[HY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW480 NUL0bIpYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVW3NkBp NFiycmRKSzVyIE2gNE4xOzdizszN M4[zclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
COR-L23 NUTFSXZMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnL3O|IhcA>? MlvrTWM2OCB;IECuNFM4KM7:TR?= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
SW1573 NVXqWm9QT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MknzO|IhcA>? M4myPWlEPTBiPTCwMlA{QCEQvF2= NYK0XlhKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
Calu3 MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2[0[|czKGh? M4jwdGlEPTBiPTCwMlA{QSEQvF2= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
HCC827 NUO1bW5{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUTpOWtJPzJiaB?= Mnu2TWM2OCB;IECuNFQh|ryP M3faRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
HOP62 M2X5VGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXW4PZVDPzJiaB?= NH;mR|BKSzVyIE2gNE4xPSEQvF2= M{X5TFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H1355 M3X2TWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV;ON2NFPzJiaB?= NIW5ZWJKSzVyIE2gNE4xPTJizszN MkDzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
NCI-H1792 NVPIbHl[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYXiVpkxPzJiaB?= NGfVfVhKSzVyIE2gNE4xPTNizszN MkK5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
HCT8 MnPxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUjXTW9WPzJiaB?= M3PYbGlEPTBiPTCwMlA2PSEQvF2= NVzHb4VXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
T84 M1f4R2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MU[3NkBp Moj1TWM2OCB;IECuNFYyKM7:TR?= NFXoTlU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW900 NHf1VGZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXW3NkBp NWHxfVQ2UUN3MDC9JFAvODd{IN88US=> M1WwNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
SW837 NFHUXIFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFnz[4Y4OiCq MULJR|UxKD1iMD6wO|Qh|ryP NVHyRYgzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
DLD1 MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYLkU21XPzJiaB?= NYrqZ2s4UUN3MDC9JFAvODl|IN88US=> M4\B[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
MDA-MB-175-VII MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV63NkBp NXvwbVFEUUN3MDC9JFAvODl4IN88US=> NWHKb5M4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
SW900 NVzGV49KT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1zEZ|czKGh? MlO2TWM2OCB;IECuNVI4KM7:TR?= MmX6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
Calu3 NH3Ce41Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEXBdWM4OiCq M{fDR2lEPTBiPTCwMlE2QCEQvF2= NUHUPHFmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
COR-L23 NWe2NHlGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3vURlczKGh? NYTFWVQ4UUN3MDC9JFAvOzJ7IN88US=> NV;SbmNpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
DLD1 MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M33QPFczKGh? MYnJR|UxKD1iMD62N|Ih|ryP MnOzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>

... 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]
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  • 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
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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)

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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
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    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 January 29 2021 --
NCT04566133 Not yet 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 5 2021 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 2021 Phase 1
NCT04485559 Recruiting Drug: Everolimus|Drug: Trametinib Recurrent World Health Organization (WHO) Grade II Glioma University of California San Francisco|Novartis Pharmaceuticals|Pediatric Brain Tumor Foundation|The Lilabean Foundation for Pediatric Brain Cancer Research December 9 2020 Phase 1
NCT04666272 Not yet recruiting Drug: dabrafenib|Drug: trametinib Melanoma Novartis Pharmaceuticals|Novartis December 22 2020 --

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