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 1026 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 NI\R[nlHfW6ldHnvckBie3OjeR?= MkHWNVAx6oDLbl2= M1LNNFI1KGh? MojPeJJidWW2aX7pZkBkd3WuZDDk[YNz\WG|ZTDZRXAhdGW4ZXzzJIFv\CCrbnjpZol1KEyPQj3pcoR2[2WmIGnBVEB2eHKnZ4XsZZRqd25iaX6gUWRCNU2ELUKzNUwhW1dzMUG2JIFv\CCVV{S4NEBk\Wyucx?= NEPQWYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEizN|Y3PSd-M{C4N|M3PjV:L3G+
RG7388-resistant U87MG cells NYfnZ3hNTnWwY4Tpc44h[XO|YYm= MXyxNEBvVQ>? NEf4b4wzPCCq NHjXXVJFVVOR MYTUdoFu\XSrbnniJJRz\WG2bXXueEBz\WS3Y3XkJJRp\SCrbo\hd4l3\SCyaHXuc5R6eGVib3[gVmc4Ozh6IILld4l{fGGwdDDj[Yxtey5? MnXUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB{N{S5PFQoRjNyMke0PVg1RC:jPh?=
BJAB cells NXK0RW9VTnWwY4Tpc44h[XO|YYm= Ml\DNE4xOc7:TR?= MmnJNlQhcA>? M3rsR|AvODFizszNJJRz[W2ndHnubYIh\W[oZXP0bZZmdHlic4XwdJJme3OnZDD0bIUhTVKNIHj5dIVz[WO2aY\heIlwdiCrbjDCTmFDKGOnbHzzJINifXOnZDDifUB1cGViY3;tZolv\WRidILlZZRu\W62IH;mJGJMVTF{MDDhcoQhTGGwdYPldpRq[i5? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODl2N{W3Okc,OzB7NEe1O|Y9N2F-
Human PDAC cell lines (MIA-PACA, PANC-1, CFPAC-1, PL45, CAPAN-2 and HPAF-II) NEfLVVhHfW6ldHnvckBie3OjeR?= NVTKZpZ7OTBibl2gc5IhOTByIH7N M4DrWlMu\GG7czDvdkA3NWSjeYO= MXTUbIUh[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?= NV\2Z5F5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C5NlE{PTFpPkOwPVIyOzVzPD;hQi=>
Transitional cell carcinoma (TCC) cell lines M4TnZWZ2dmO2aX;uJIF{e2G7 NGO2PZUzPSCwTR?= MlnIOk0zPCCq NV\zZWZMS2GwaX7lJHRESyClZXzsJIxqdmW|IHHy[UB{\W6|aYTpeoUhfG9iTVXLJIlvcGmkaYTpc44> M2PINlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzMES4OVQ5Lz5|MUC0PFU1QDxxYU6=
COLO205 NF3yVnFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUK3NkBp NX;IWoJPUUN3MDC9JFAvODBzIN88US=> NH7XVog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
HT-29 M1H4fGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV[3NkBp NUnFeHZTUUN3MDC9JFAvODBzIN88US=> NI[wUHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
COLO205 NVG0fpJ7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4rsOVczKGh? M2DIb2lEPTBiPTCwMlAxOSEQvF2= Ml;CQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
MV522 MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVS3NkBp M4rie2lEPTBiPTCwMlAxOSEQvF2= NVLsdIVPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
HT-29 MmL5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGL2ZnY4OiCq M{\MTGlEPTBiPTCwMlAxOiEQvF2= NFS2WHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
MV522 M4rTR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYG3NkBp Mm\jTWM2OCB;IECuNFAzKM7:TR?= MlLIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
NCI-H727 Mof6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MU[3NkBp M4PEdmlEPTBiPTCwMlAxOiEQvF2= MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
NCI-H727 NUDBXpdFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYLEeWt4PzJiaB?= MVnJR|UxKD1iMD6wNFIh|ryP MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
SW1417 MoG3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoXzO|IhcA>? NHLKVJlKSzVyIE2gNE4xODNizszN NEP2SVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW1417 NUnoWmZGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mln3O|IhcA>? NYHUenpJUUN3MDC9JFAvODB|IN88US=> NVW1WHRVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
Calu6 M{XY[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M13xOFczKGh? NFfI[mhKSzVyIE2gNE4xODNizszN NH3CNIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
LS1034 M3fOV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIXHXm84OiCq MkHPTWM2OCB;IECuNFA1KM7:TR?= NE\mUpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW1463 M3HmXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEDoT|M4OiCq NH60ZpNKSzVyIE2gNE4xODRizszN M1TrcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
SW1463 NHLVV4NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYjRbVF2PzJiaB?= MXrJR|UxKD1iMD6wNFQh|ryP Mn7IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
Calu6 MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXq4WYFLPzJiaB?= MXTJR|UxKD1iMD6wNFQh|ryP MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
LS1034 NV:yWpFOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2iwWlczKGh? MYLJR|UxKD1iMD6wNFUh|ryP NY\DWYI2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
RKO MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoWxO|IhcA>? M2j1TGlEPTBiPTCwMlAxPSEQvF2= MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
NCI-H508 NHjlZo9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWG3NkBp Mo\iTWM2OCB;IECuNFA5KM7:TR?= MoTXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
KM12 NFXKSGlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{HWOFczKGh? MV\JR|UxKD1iMD6wNUDPxE1? NV[4PFB[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
A427 MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYqxeFBjPzJiaB?= NGLCb3JKSzVyIE2gNE4xOSEQvF2= M1nrW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H1155 M2nmRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV;BUlhXPzJiaB?= MUDJR|UxKD1iMD6wNUDPxE1? Mk\FQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
HCT8 MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFLB[2s4OiCq MXfJR|UxKD1iMD6wNVQh|ryP NV3LUYI{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
MDA-MB-175-VII MlXES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mny2O|IhcA>? NH3JZnRKSzVyIE2gNE4xOTZizszN MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
A549 MlTxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYfxTZpVPzJiaB?= M2HkTWlEPTBiPTCwMlAyPiEQvF2= NWH5WII2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
RKO NGjRV2dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVq3NkBp NHrtTohKSzVyIE2gNE4xOThizszN NFvSVIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
NCI-H23 M3G1bmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4r3S|czKGh? NYXuVZVxUUN3MDC9JFAvODJizszN M1\SU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
A427 MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXzSSoc1PzJiaB?= MVvJR|UxKD1iMD6wNlIh|ryP NF[3PGw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
KM12 NGPJNoRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1fZW|czKGh? M4fRUGlEPTBiPTCwMlAzOyEQvF2= MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
NCI-H508 NFvhdopIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M17GNVczKGh? MlXrTWM2OCB;IECuNFI{KM7:TR?= MoTvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
MDA-MB-231 NYTOeGZCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWGzJIRigXN? NVLT[I1IT0l3MDC9JFAvODJ3IN88US=> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
SW837 M3X2Wmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmTyO|IhcA>? NVzON2l4UUN3MDC9JFAvODJ3IN88US=> MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
SW480 NGjveFVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmHGO|IhcA>? NWrIelVFUUN3MDC9JFAvODJ4IN88US=> M2TUdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H1355 MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYi0W2lRPzJiaB?= M{HFWmlEPTBiPTCwMlAzPyEQvF2= M3;ybFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H23 NIjKSJZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlriO|IhcA>? MWDJR|UxKD1iMD6wNlkh|ryP NYD0R45ERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
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T84 M1GzUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXPIXJhkPzJiaB?= NEPk[FBKSzVyIE2gNE4xOyEQvF2= MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
A549 M{[xPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{\j[|czKGh? MmG3TWM2OCB;IECuNFM1KM7:TR?= MofEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
NCI-H1792 NEj6eY1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlPYO|IhcA>? Ml[1TWM2OCB;IECuNFM2KM7:TR?= NEj2VJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW480 MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHnJTGw4OiCq M{LTSmlEPTBiPTCwMlA{PyEQvF2= MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
COR-L23 MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHrWcoc4OiCq NIrUNINKSzVyIE2gNE4xOzdizszN MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
SW1573 MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlT1O|IhcA>? NU\YWYtoUUN3MDC9JFAvODN6IN88US=> Mme3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
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HCC827 NU\BRotqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3j6SlczKGh? NV;lZVdUUUN3MDC9JFAvODRizszN M{\kPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
HOP62 MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXq3NkBp NF;2SnJKSzVyIE2gNE4xPSEQvF2= M2\hRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H1355 MnS0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFj6NHM4OiCq NGrT[otKSzVyIE2gNE4xPTJizszN NW\FNlByRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
NCI-H1792 M1XUXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1fubVczKGh? NUmxUnF4UUN3MDC9JFAvODV|IN88US=> NFzQdGg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
HCT8 M4ftfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml3nO|IhcA>? NWLw[IhiUUN3MDC9JFAvODV3IN88US=> NIrxS|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
T84 M1HQO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXHCUWx4PzJiaB?= NXOwR49kUUN3MDC9JFAvODZzIN88US=> NH;qSWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW900 MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWTOTGVNPzJiaB?= NGD4cG5KSzVyIE2gNE4xPzJizszN MmL6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
SW837 Mny5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXy3NkBp NH\qV3pKSzVyIE2gNE4xPzRizszN NVLSOlNDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
DLD1 MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmPUO|IhcA>? NH;QWXpKSzVyIE2gNE4xQTNizszN MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
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SW900 Mk[zS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVy0V4k1PzJiaB?= M2XyR2lEPTBiPTCwMlEzPyEQvF2= M2PZe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
Calu3 M2DVZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWm3NkBp NXzBXHhsUUN3MDC9JFAvOTV6IN88US=> MkfKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
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DLD1 MkDyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlLWO|IhcA>? MmDHTWM2OCB;IECuOlMzKM7:TR?= M1njVlxiKHSjcnfleF0oZ2KuYX7rK{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.
  • (Only for Reference)
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
  • (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 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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