Trametinib (GSK1120212)

别名: JTP-74057

Trametinib (GSK1120212, JTP-74057)是一种高特异性的,有效的MEK1/2抑制剂,无细胞试验中IC50为0.92 nM/1.8 nM,对c-Raf, B-Raf, ERK1/2没有抑制活性。Trametinib 可激活自噬并诱导凋亡。

Trametinib (GSK1120212) Chemical Structure

Trametinib (GSK1120212) Chemical Structure

CAS: 871700-17-3

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 794.43 现货
5mg RMB 647.01 现货
10mg RMB 1040.13 现货
50mg RMB 3104.01 现货
1g RMB 7944.3 现货
更大包装 有超大折扣

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info@selleck.cn

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常与Trametinib (GSK1120212)一起在实验中被使用的化合物

Gefitinib


Trametinib和Gefitinib联合有效抑制NRAS/KRAS/BRAF V600野生型结直肠癌(CRC)细胞增殖。


Georgiou A, et al. Mol Cancer Res. 2020 Jun;18(6):835-846.

Olaparib (AZD2281)


Trametinib和Olaparib在MESO-1/MSTO-211/H2452异种移植物和BE261T PDX模型中显示出明显更高的抗肿瘤效果。


Yang H, et al. Cell Death Discov. 2023 Feb 10;9(1):55.

Doxorubicin (Adriamycin) HCl


Trametinib与拓扑异构酶2 (Top2)抑制剂Doxorubicin联用对K562细胞的转录组具有拮抗作用。


Mathur L, et al. Nat Commun. 2022 Aug 1;13(1):4450.

Dabrafenib


Trametinib和Dabrafenib联合治疗是FDA批准的用于恶性黑色素瘤和非小细胞肺癌(NSCLC)患者的治疗。


Brown CN, et al. Cell Signal. 2020 Jul;71:109605.

Cisplatin


Trametinib和Cisplatin联合治疗在非小细胞肺癌(NSCLC)患者中具有应用潜力。


Brown CN, et al. Cell Signal. 2020 Jul;71:109605.

客户使用Selleck的Trametinib (GSK1120212)发表文献1071篇:

产品质控

批次: 纯度: 99.98%
99.98

MEK抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
MDA-MB-231, SW480 and SW1116 cells MkHISpVv[3Srb36gZZN{[Xl? MX[xNFDjiImwTR?= NVTCcoUyOjRiaB?= NHjnbmR1emGvZYTpcoljKGOxdXzkJIRm[3KnYYPlJHlCWCCuZY\lcJMh[W6mIHnubIljcXRiTF3CMYlv\HWlZXSgXWFRKHWycnXneYxifGmxbjDpckBOTEFvTVKtNlMyNCCVV{GxNVYh[W6mIGPXOFgxKGOnbHzz NIPrPFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEizN|Y3PSd-M{C4N|M3PjV:L3G+
RG7388-resistant U87MG cells M2q2UGZ2dmO2aX;uJIF{e2G7 MUixNEBvVQ>? MmjYNlQhcA>? MnLKWJJidWW2aX7pZkB1emWjdH3lcpQhemWmdXPl[EB1cGViaX72ZZNqfmVicHjlco91gXCnIH;mJHJIPzN6ODDy[ZNqe3SjboSgZ4VtdHNw MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODJ5NEm4OEc,OzB{N{S5PFQ9N2F-
BJAB cells M1nzdGZ2dmO2aX;uJIF{e2G7 MUiwMlAy|ryP NHrF[XQzPCCq MnrBNE4xOSEQvF2geJJidWW2aX7pZkBm\m[nY4TpeoVtgSC|dYDwdoV{e2WmIITo[UBGWktiaInw[ZJi[3SrdnH0bY9vKGmwIFLKRWIh[2WubIOgZ4F2e2WmIHL5JJRp\SClb33ibY5m\CC2cnXheI1mdnRib3[gRmtOOTJyIHHu[EBF[W63c3XyeIljNg>? MlnGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB7NEe1O|YoRjNyOUS3OVc3RC:jPh?=
Human PDAC cell lines (MIA-PACA, PANC-1, CFPAC-1, PL45, CAPAN-2 and HPAF-II) NXjXZXkyTnWwY4Tpc44h[XO|YYm= NXrvfVVZOTBibl2gc5IhOTByIH7N MkW5N{1l[Xm|IH;yJFYu\GG7cx?= MYDUbIUh[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?= M3fzOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyOUKxN|UyLz5|MEmyNVM2OTxxYU6=
Transitional cell carcinoma (TCC) cell lines NVz1cFNUTnWwY4Tpc44h[XO|YYm= NU[zVYt6OjVibl2= NEHNRWU3NTJ2IHi= NWDBfmpOS2GwaX7lJHRESyClZXzsJIxqdmW|IHHy[UB{\W6|aYTpeoUhfG9iTVXLJIlvcGmkaYTpc44> NIfqVYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MUC0PFU1QCd-M{GwOFg2PDh:L3G+
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MV522 M33aOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIDHe5o4OiCq MmP2TWM2OCB;IECuNFAyKM7:TR?= M2fVNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
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LS1034 NIKwcnJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2S3flczKGh? MmewTWM2OCB;IECuNFA2KM7:TR?= NXf0RlBHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
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NCI-H508 NXLmTmRCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2PsNlczKGh? MkXFTWM2OCB;IECuNFA5KM7:TR?= M4n3PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
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MDA-MB-175-VII NYrBT5oyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MY[3NkBp NYPRUXRzUUN3MDC9JFAvODF4IN88US=> NX32[VdLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
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MDA-MB-231 MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3y4XlMh\GG7cx?= MVrHTVUxKD1iMD6wNlUh|ryP Mor6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
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SW480 MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmnCO|IhcA>? M3\xVWlEPTBiPTCwMlAzPiEQvF2= NXHyOGQ4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
NCI-H1355 NF3DcGZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV:3NkBp M2X5[GlEPTBiPTCwMlAzPyEQvF2= Mn\oQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
NCI-H23 NUTKcoRDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoPWO|IhcA>? MoDkTWM2OCB;IECuNFI6KM7:TR?= NIPYSFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
EFM19 MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXjv[4tCPzJiaB?= NYTkNmdsUUN3MDC9JFAvODNizszN M4j5XFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
T84 M360c2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWXrUoJ[PzJiaB?= NYfVZnM5UUN3MDC9JFAvODNizszN MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
A549 NG\CN|BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmC5O|IhcA>? M1PheWlEPTBiPTCwMlA{PCEQvF2= NEL5[3k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
NCI-H1792 M3r2fWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWS3NkBp MmXmTWM2OCB;IECuNFM2KM7:TR?= NFziVWk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW480 NY\jWWhPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnzqO|IhcA>? M2rpPGlEPTBiPTCwMlA{PyEQvF2= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
COR-L23 NXPxdJZQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXe3NkBp M4n6WGlEPTBiPTCwMlA{PyEQvF2= NXTSXnNvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
SW1573 NFnSSXJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NE\vUo84OiCq M{XnZWlEPTBiPTCwMlA{QCEQvF2= M335[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
Calu3 NXXVUVcxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4rGN|czKGh? NH7STFRKSzVyIE2gNE4xOzlizszN MnXzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
HCC827 M1PF[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFH5NZI4OiCq MnO1TWM2OCB;IECuNFQh|ryP NGHlemk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
HOP62 NE[5SopIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXvncnM1PzJiaB?= Mk\pTWM2OCB;IECuNFUh|ryP M1XzNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
NCI-H1355 MkHvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH71VWI4OiCq NFTtbFdKSzVyIE2gNE4xPTJizszN MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyNVA{QDd3Lze+R4hGVUKOPD;hQi=>
NCI-H1792 M3j6b2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGHQVXI4OiCq NHvjd|FKSzVyIE2gNE4xPTNizszN NGrNS4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
HCT8 M1rKdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH7PU3o4OiCq NInpNWZKSzVyIE2gNE4xPTVizszN NUntRYk4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
T84 MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkDCO|IhcA>? MlW0TWM2OCB;IECuNFYyKM7:TR?= Mmf5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
SW900 NEXwTHlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGn4TWE4OiCq NH3p[o9KSzVyIE2gNE4xPzJizszN MoDRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
SW837 M4HT[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NE\QSXM4OiCq M2q5OmlEPTBiPTCwMlA4PCEQvF2= NV3NXZl7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyM{i3OU8oRkOqRV3CUFww[T5?
DLD1 NF6wWnRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{jCflczKGh? NWPPVnJTUUN3MDC9JFAvODl|IN88US=> NFfjeYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
MDA-MB-175-VII MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1nOWlczKGh? MVfJR|UxKD1iMD6wPVYh|ryP NFrUN249[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
SW900 MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoTIO|IhcA>? NV\NbXhzUUN3MDC9JFAvOTJ5IN88US=> NHXNdZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzOTB|OEe1M{c,S2iHTVLMQE9iRg>?
Calu3 M{e2T2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXe3NkBp M2rHfGlEPTBiPTCwMlE2QCEQvF2= Ml:wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
COR-L23 MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHfsVWw4OiCq M1GyRmlEPTBiPTCwMlMzQSEQvF2= MlvxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExOzh5NT:nQmNpTU2ETEyvZV4>
DLD1 MnK4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3uwbVczKGh? MWLJR|UxKD1iMD62N|Ih|ryP M4jU[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFIyODN6N{WvK|5EcEWPQly8M4E,
点击查看更多细胞系数据

生物活性

产品描述 Trametinib (GSK1120212, JTP-74057)是一种高特异性的,有效的MEK1/2抑制剂,无细胞试验中IC50为0.92 nM/1.8 nM,对c-Raf, B-Raf, ERK1/2没有抑制活性。Trametinib 可激活自噬并诱导凋亡。
特性 药效大于PD0325901或AZD6244
靶点
MEK1 [1]
(Cell-free assay)
MEK2 [1]
(Cell-free assay)
0.92 nM 1.8 nM
体外研究(In Vitro)
体外研究活性

GSK1120212抑制 MBP 的磷酸化,对于不同亚型的Raf和MEK 而言,IC50在0.92 nM-3.4 nM。GSK1120212对c-Raf, B-Raf, ERK1和ERK2的激酶活性没有抑制作用。另外,GSK1120212对于其它98种激酶没有很强的抑制作用。GSK1120212对于人结肠癌细胞系有很强的抑制作用,其中HT-29和COLO205细胞组成型表达有活性的B-Raf突变,这两种细胞对GSK1120212最为敏感,IC50分别是0.48 nM 和 0.52 nM。含有k-Raf突变的细胞系对GSK1120212的敏感性介于如下范围,IC50是2.2-174 nM. 相反地,COLO320 DM细胞中B-Raf 和K-Ras均为野生型,因而即便在10 μM都对GSK1120212有抗性。用GSK1120212处理24小时可以诱导所有敏感细胞的细胞周期停滞在G1期。与此一致,GSK1120212处理使得大部分人结肠癌细胞系中p15INK4b 和/或p27KIP1的表达量上升。GSK1120212能诱导HT-29和COLO205细胞的凋亡,COLO205细胞更为敏感。[1] GSK1120212抑制外周血单核细胞产生肿瘤坏死因子-α和白介素-6。 [2]

激酶实验 Raf-MEK-ERK级联激酶检测
非磷酸化的髓鞘碱性蛋白(MBP)涂覆到ELISA板上,B-Raf/c-Raf的活性形式与非磷酸化MEK1/MEK2和ERERK2混合在10 μM ATP和12.5 mM MgCl2,其MOPS缓冲液中含有不同浓度的GSK1120212。 MBP的磷酸化是由抗磷酸化的MBP抗体进行检测。
细胞实验 细胞系 HT-29, HCT-15, HCT116, COLO205, LS-174T, SW480, SW620, T84, LoVo和COLO320
浓度 溶解在DMSO中至终浓度约10 μM
孵育时间 3天或4天
方法

指数生长的细胞预培养在96孔组织培养板中24小时后用GSK1120212孵育。细胞生长是通过体外毒理学测定试剂盒(基于磺酰罗丹明B)检测。对于细胞凋亡测定,漂浮和贴壁细胞被收集并用70%乙醇固定。用PBS洗涤后,将细重胞悬在100微克/毫升RNA酶和25微克/毫升的碘化丙啶(PI)中,至于37℃黑暗中30分钟。每一个单细胞的DNA含量是用流式细胞仪Cytomics FC500或番石榴EasyCyte来确定。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot ERRα / IDH3 / c-Myc / Cyclin D1 pERK /ERK / pS6 / S6 β-catenin 30185207
Growth inhibition assay Cell proliferation MTT assay 30185207
Immunofluorescence phospho-PR(S345) β-catenin 29237804
体内研究(In Vivo)
体内研究活性

按0.3 mg/kg或1 mg/kg 的剂量口服GSK1120212(一天一次共14天)能有效抑制HT-29肿瘤,1 mg/kg 的剂量可完全抑制肿瘤生长。在癌症组织中,一次口服1 mg/kg GSK1120212能完全抑制ERK1/2的磷酸化,14天后能提高p15INK4b和p27KIP1的表达量。在COLO205肿瘤模型中,0.3 mg/kg剂量的GSK1120212就足以抑制肿瘤生长,1 mg/kg剂量的GSK1120212可以使2/3的老鼠的肿瘤消退至可检测水平之下。[1] 0.1 mg/kg剂量的GSK1120212完全抑制佐剂性关节炎(AIA)和II型胶原诱导的关节炎(CIA) Lewis大鼠或DBA1/J小鼠。[2]

动物实验 Animal Models 雌雄BALB/c-nu/nu小鼠皮下注射HT-29或COLO205细胞
Dosages 1 mg/kg/day
Administration 口服
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05275374 Not yet recruiting 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 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 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 Melanoma Novartis Pharmaceuticals|Novartis December 1 2021 --

化学信息&溶解度

分子量 615.39 分子式

C26H23FIN5O4

CAS号 871700-17-3 SDF Download Trametinib (GSK1120212) SDF
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
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 8 mg/mL ( 12.99 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

技术支持

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操作手册

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常见问题及建议解决方法

问题 1:
Could you help us with the best way to prepare Trametinib for in vivo i.p. injections?

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

问题 2:
How to solve the problem that this product didn't dissolve up to 10mM in DMSO at room temperature?

回答:
The solution can be heated up to 50 degree to help dissolve. Besides, sonication (with a probe sonicator) also helped greatly.

MEK相关信号通路图

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