PD0325901(Mirdametinib)

For research use only.

Licensed by Pfizer Catalog No.S1036

537 publications

PD0325901(Mirdametinib) Chemical Structure

Molecular Weight(MW): 482.19

PD0325901 is a selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM in cell-free assays, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. Phase 2.

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Selleck's PD0325901(Mirdametinib) has been cited by 537 publications

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Biological Activity

Description PD0325901 is a selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM in cell-free assays, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. Phase 2.
Targets
MEK [1]
(Cell-free assay)
0.33 nM
In vitro

PD0325901 shows higher permeability than CI-1040, another MEK inhibitor. PD0325901 should be able to achieve higher systemic exposures than CI-1040. [1] PD0325901 is exquisitely specific and highly potent against purified MEK, revealing a Kiapp of 1 nM against activated MEK1 and MEK2. [2] PD0325901 is roughly 500-fold more potent than CI-1040 with respect to its cellular effects on phosphorylation of ERK1 and ERK2, displaying subnanomolar activity. [2] PD0325901 prevents the growth of melanoma cell lines. PD0325901 inhibits the growth of TPC-1 cells and K2 cells with GI50 of 11 nM and 6.3 nM, respectively. [3] PD0325901 significantly prevents the the growth of PTC cells harboring a BRAF mutation at very low concentration (10 nM) and only moderately increases the growth of the PTC cells carrying the RET/PTC1 rearrangement at the same concentration. PD0325901 effectively inhibits the phosphorylation of ERK1/2 in multiple PTC cell lines. [3]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human CHP-212 cell M{jNd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGjXUlJKdmirYnn0bY9vKG:oIHj1cYFvKEOKUD2yNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjV{NzDuUU4> MYHTRW5ITVJ?
human M14 cell MonyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn;mTY5pcWKrdHnvckBw\iCqdX3hckBOOTRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkS1JI5ONg>? M3\LRnNCVkeHUh?=
human SK-MEL-28 cell MmD6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NInKdG9KdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0zQCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNUKgcm0v NFLyb|NUSU6JRWK=
human NOMO-1 cell Mlj0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1PVdWlvcGmkaYTpc44hd2ZiaIXtZY4hVk:PTz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4xPyCwTT6= M4\tUnNCVkeHUh?=
human A375 cell NHTu[2hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHztRlNKdmirYnn0bY9vKG:oIHj1cYFvKEF|N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlY6KG6PLh?= NUG0fFU6W0GQR1XS
human DU-4475 cell MmPpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkHSTY5pcWKrdHnvckBw\iCqdX3hckBFXS12NEe1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{42PyCwTT6= M4HhNXNCVkeHUh?=
human C32 cell MlqxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmnuTY5pcWKrdHnvckBw\iCqdX3hckBEOzJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Lk[3JI5ONg>? M1v5VHNCVkeHUh?=
human BPH-1 cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MofoTY5pcWKrdHnvckBw\iCqdX3hckBDWEhvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVUhdk1w NHviZYdUSU6JRWK=
human CP50-MEL-B cell M{HaSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoTRTY5pcWKrdHnvckBw\iCqdX3hckBEWDVyLV3FUE1DKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC53ODDuUU4> Mn3ZV2FPT0WU
human H9 cell MmnOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4PLTGlvcGmkaYTpc44hd2ZiaIXtZY4hUDliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13Lke3JI5ONg>? MULTRW5ITVJ?
human HTC-C3 cell NHjadGRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlzCTY5pcWKrdHnvckBw\iCqdX3hckBJXENvQ{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlg6KG6PLh?= MmG2V2FPT0WU
human BHT-101 cell MoiwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWrHSIhsUW6qaXLpeIlwdiCxZjDoeY1idiCESGStNVAyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi55IH7NMi=> NEP3d21USU6JRWK=
human COLO-741 cell M2jLTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MknLTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLUe0NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvOSCwTT6= M4DTNHNCVkeHUh?=
human OVCAR-5 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUHvN41EUW6qaXLpeIlwdiCxZjDoeY1idiCRVlPBVk02KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Py56MjDuUU4> NFLERYdUSU6JRWK=
human A549 cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHnOOJVKdmirYnn0bY9vKG:oIHj1cYFvKEF3NEmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23Mlg6KG6PLh?= M17yS3NCVkeHUh?=
human SH-4 cell growth M1PPfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX3JWmJDUW6qaXLpeIlwdiCxZjDoeY1idiCVSD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PE4zPiCwTT6= Mo\sV2FPT0WU
human SK-N-AS cell Mn7WS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml\iTY5pcWKrdHnvckBw\iCqdX3hckBUUy2QLVHTJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PE41PCCwTT6= NYPFTJNXW0GQR1XS
human HT-144 cell MoTiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MULJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTF2NDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUiuPVchdk1w MYTTRW5ITVJ?
human MEL-HO cell MmLaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH;LWZFKdmirYnn0bY9vKG:oIHj1cYFvKE2HTD3IU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvPDlibl2u NICyS5RUSU6JRWK=
human COLO-679 cell NXLMepRXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFvqXVlKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tOlc6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTBwMEGgcm0> NHfZUXFUSU6JRWK=
human HuP-T4 cell M3Hidmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4LRUmlvcGmkaYTpc44hd2ZiaIXtZY4hUHWSLWS0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvQThibl2u MkHUV2FPT0WU
human H-EMC-SS cell NIXvWXlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFm3NG5KdmirYnn0bY9vKG:oIHj1cYFvKEhvRV3DMXNUKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTFwMEKgcm0v MmLHV2FPT0WU
human LB2518-MEL cell NGDsSYZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUHJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjVzOD3NSWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS5zMzDuUU4> NVjK[3dVW0GQR1XS
human HL-60 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4nqN2lvcGmkaYTpc44hd2ZiaIXtZY4hUExvNkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNU4yPSCwTT6= M3;zbHNCVkeHUh?=
human NCI-H1666 cell M3G2SGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUL1cG1EUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PjZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMT6xO{BvVS5? Mm\DV2FPT0WU
human A101D cell MofzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEjtTZBKdmirYnn0bY9vKG:oIHj1cYFvKEFzMEHEJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVEvPDVibl2u NXm5fJJQW0GQR1XS
human RVH-421 cell Mnv5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHvITZRKdmirYnn0bY9vKG:oIHj1cYFvKFKYSD20NlEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi54NDDuUU4> MXvTRW5ITVJ?
human Hs-578-T cell M{XO[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWPJcohq[mm2aX;uJI9nKGi3bXHuJGh{NTV5OD3UJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvPzlibl2u NFniVnpUSU6JRWK=
human A375 cells Mn[xVJJwdGmoZYLheIlwdiCjc4PhfS=> NGHGc2M4OiCq MnXkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDM{e1JINmdGy|IHX4dJJme3OrbnegRnJCTiCYNkCwSUBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIwhfGm2ZYKt[4xwKGG|c3H5MEBKSzVyPUGzJI5ONg>? MY[yN|Q4PDN6OB?=
human DOK cell M4DEO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4nvU2lvcGmkaYTpc44hd2ZiaIXtZY4hTE:NIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuOEBvVS5? Mlm2V2FPT0WU
human Mewo cell M1;mbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWWwdpVHUW6qaXLpeIlwdiCxZjDoeY1idiCPZYfvJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPDVibl2u NVzsXY56W0GQR1XS
human ONS-76 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXPWTlRzUW6qaXLpeIlwdiCxZjDoeY1idiCRTmOtO|Yh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC53MTDuUU4> NF6y[IpUSU6JRWK=
human UACC-257 cell NHzvcZhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYfJcohq[mm2aX;uJI9nKGi3bXHuJHVCS0NvMkW3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPjJibl2u NWOxNJo6W0GQR1XS
human SW626 cell MmSyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3:yUGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4Mk[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE46OSCwTT6= MmPtV2FPT0WU
human SW620 cell NXjw[WFzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2TYeWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE46PSCwTT6= M3S0RnNCVkeHUh?=
human TYK-nu cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3jodWlvcGmkaYTpc44hd2ZiaIXtZY4hXFmNLX71JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvOTNibl2u M4DRUHNCVkeHUh?=
human ACN cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4LM[WlvcGmkaYTpc44hd2ZiaIXtZY4hSUOQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuO|Yhdk1w NYTISWZwW0GQR1XS
human MIAPaCa2 cells NYrPe|VGWHKxbHnm[ZJifGmxbjDhd5NigQ>? NXrvR5lzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNTWFR[UOjMjDj[YxteyxiSVO1NF0yPyCwTT6= MXOyN|Q4PDN6OB?=
human T-24 cell MofOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV3Jcohq[mm2aX;uJI9nKGi3bXHuJHQuOjRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zOT63NUBvVS5? NEXtNm9USU6JRWK=
human AGS cell MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1zCZWlvcGmkaYTpc44hd2ZiaIXtZY4hSUeVIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkCuOFEhdk1w NHzIeVZUSU6JRWK=
human SW872 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV3RRplZUW6qaXLpeIlwdiCxZjDoeY1idiCVV{i3NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI4Njl7IH7NMi=> Mmq4V2FPT0WU
human C2BBe1 cell NIfM[XNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH24NVhKdmirYnn0bY9vKG:oIHj1cYFvKEN{QlLlNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI5NjV2IH7NMi=> NWDjWmdPW0GQR1XS
human MZ7-mel cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlflTY5pcWKrdHnvckBw\iCqdX3hckBOYjdvbXXsJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlkvPDNibl2u NVTMRpc6W0GQR1XS
human HCC2998 cell M4DBXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2jkbWlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkm5PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM{NjZ4IH7NMi=> MUTTRW5ITVJ?
human HO-1-N-1 cell NIXSc|hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWLJcohq[mm2aX;uJI9nKGi3bXHuJGhQNTFvTj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|QvPDNibl2u NHjnU4JUSU6JRWK=
human SW756 cell NVfacIZGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Moe5TY5pcWKrdHnvckBw\iCqdX3hckBUXzd3NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO0MlQ2KG6PLh?= NUDNRnR1W0GQR1XS
human NCI-H1437 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXzHbVR4UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE1OzdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|ND60PUBvVS5? M{TWR3NCVkeHUh?=
human NCI-H747 cell M2nkbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3noOWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi3OFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{PC57ODDuUU4> NUDpR5dQW0GQR1XS
human SK-MEL-2 cell M{PvZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmjjTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM2NjJibl2u M17JXXNCVkeHUh?=
human MZ2-MEL cell NIjqTI9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWL2Xo5RUW6qaXLpeIlwdiCxZjDoeY1idiCPWkKtUWVNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzVwNkWgcm0v NX7DT2E6W0GQR1XS
human PSN1 cell NWP1S3U6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4HBbGlvcGmkaYTpc44hd2ZiaIXtZY4hWFOQMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO4MlQ2KG6P M1PU[HNCVkeHUh?=
human CAL-39 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXK3W2FNUW6qaXLpeIlwdiCxZjDoeY1idiCFQVytN|kh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{QS5yNDDuUU4> NX\iUY5pW0GQR1XS
human LOXIMVI cell Mni2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NW\lWVE4UW6qaXLpeIlwdiCxZjDoeY1idiCOT2jJUXZKKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzlwM{mgcm0v Ml7EV2FPT0WU
human COLO-792 cell Mn3rS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3jHU2lvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz23PVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Oy5zNTDuUU4> NILlRWVUSU6JRWK=
human CAL-27 cell MkDBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHTTPHlKdmirYnn0bY9vKG:oIHj1cYFvKEODTD2yO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ1NjlzIH7N M3zIdnNCVkeHUh?=
human AsPC-1 cell MknxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlvKTY5pcWKrdHnvckBw\iCqdX3hckBCe1CFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20OU4zQCCwTT6= NUXq[XlHW0GQR1XS
human NCI-H2291 cell NHqxdmZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmDoTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKyPVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Pi52NjDuUU4> MYDTRW5ITVJ?
human RCM-1 cell MoXaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmfGTY5pcWKrdHnvckBw\iCqdX3hckBTS01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS2Mlg2KG6PLh?= M4LxOHNCVkeHUh?=
human NCI-H292 cell MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkmyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFcvOzlibl2u NWDYc2ZkW0GQR1XS
human WM-115 cell NEW2fJFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnjTTY5pcWKrdHnvckBw\iCqdX3hckBYVS1zMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20PE42KG6PLh?= M4i1NHNCVkeHUh?=
human RT-112 cell NXfzVG12T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXjJcohq[mm2aX;uJI9nKGi3bXHuJHJVNTFzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS4Mlg1KG6PLh?= MVjTRW5ITVJ?
human HT-29 cell MkXyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml3tTY5pcWKrdHnvckBw\iCqdX3hckBJXC1{OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWwMlQ6KG6PLh?= NXHsW|J5W0GQR1XS
human RKO cell growth NEi0R|ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF3zbXdKdmirYnn0bY9vKG:oIHj1cYFvKFKNTzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWyMlAzKG6PLh?= MYfTRW5ITVJ?
human KY821 cell MmjvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHHqUYxKdmirYnn0bY9vKG:oIHj1cYFvKEu\OEKxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVMvOyCwTT6= MmnUV2FPT0WU
human LB1047-RCC cell M4PsXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVKy[olFUW6qaXLpeIlwdiCxZjDoeY1idiCOQkGwOFcuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUmuOlUhdk1w NIWy[WtUSU6JRWK=
human SW1116 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHPJZXJKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUGxOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYxNjR7IH7NMi=> MVfTRW5ITVJ?
human P12-ICHIKAWA cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NI\NWZZKdmirYnn0bY9vKG:oIHj1cYFvKFBzMj3JR2hKU0GZQTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[yMlI4KG6PLh?= M{jMNHNCVkeHUh?=
human HCC70 cell NEHzPYhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUfq[2lWUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1O3NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVY{NjBzIH7NMi=> MWPTRW5ITVJ?
human MIA-PaCa-2 cell MlLVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1rZfGlvcGmkaYTpc44hd2ZiaIXtZY4hVUmDLWDhR4EuOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZ|LkWzJI5ONg>? NVn0OFRYW0GQR1XS
human LoVo cell NFnJVm9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn3iTY5pcWKrdHnvckBw\iCqdX3hckBNd1[xIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NkWuNlkhdk1w MVfTRW5ITVJ?
human LB2241-RCC cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGexWIVKdmirYnn0bY9vKG:oIHj1cYFvKEyEMkK0NU1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14NT61NkBvVS5? NVPBPHRMW0GQR1XS
human GAK cell M4L6dmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX;qV4c{UW6qaXLpeIlwdiCxZjDoeY1idiCJQVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22Ok45PyCwTT6= MofIV2FPT0WU
human RD cell M{DYR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NELRWnpKdmirYnn0bY9vKG:oIHj1cYFvKFKGIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NkeuNUBvVS5? NHrHOJdUSU6JRWK=
human KNS-62 cell NUGxZ2pvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXm2O2lXUW6qaXLpeIlwdiCxZjDoeY1idiCNTmOtOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03QS57OTDuUU4> NUHUSll1W0GQR1XS
human HD-MY-Z cell M4fXO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MljsTY5pcWKrdHnvckBw\iCqdX3hckBJTC2PWT3aJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O|EvOTJibl2u MYrTRW5ITVJ?
human COR-L105 cell M{fuNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmTTTY5pcWKrdHnvckBw\iCqdX3hckBEV1JvTEGwOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcyNjdzIH7NMi=> MoPhV2FPT0WU
human IA-LM cell NVLtO3I4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVnBcmRjUW6qaXLpeIlwdiCxZjDoeY1idiCLQT3MUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVc{NjJ6IH7NMi=> M4TOTHNCVkeHUh?=
human EM-2 cell NXPxRZZ4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3fLSWlvcGmkaYTpc44hd2ZiaIXtZY4hTU1vMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUe0Mlchdk1w NGXucGJUSU6JRWK=
human NB69 cell M2TaUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnLKTY5pcWKrdHnvckBw\iCqdX3hckBPSjZ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYm= NVe4R4t1W0GQR1XS
human HuP-T3 cell MoG2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWXONmdvUW6qaXLpeIlwdiCxZjDoeY1idiCKdWCtWFMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05Oy57MzDuUU4> NXjJPWVQW0GQR1XS
human BB30-HNC cell NWnH[WM2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2L3cGlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ|MD3IUmMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05PS53MTDuUU4> M3TBTHNCVkeHUh?=
human HT-1080 cell MlfHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWTRdI9[UW6qaXLpeIlwdiCxZjDoeY1idiCKVD2xNFgxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QDVwOEigcm0v Mm\SV2FPT0WU
human RMG-I cell M3jicmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3;MOWlvcGmkaYTpc44hd2ZiaIXtZY4hWk2JLVmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24O{4{PCCwTT6= M12xV3NCVkeHUh?=
human HCC1419 cell MkHZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoHETY5pcWKrdHnvckBw\iCqdX3hckBJS0NzNEG5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVEvOzhibl2u Mly2V2FPT0WU
human SW780 cell M1j3bmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVXJcohq[mm2aX;uJI9nKGi3bXHuJHNYPzhyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OUKuN|Ihdk1w MV7TRW5ITVJ?
human SNU-387 cell M4GyXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXXJcohq[mm2aX;uJI9nKGi3bXHuJHNPXS1|OEegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25N{4{PiCwTR?= NIDsfnFUSU6JRWK=
human LAMA-84 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M33rWWlvcGmkaYTpc44hd2ZiaIXtZY4hVEGPQT24OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk1NjZ6IH7NMi=> NGfyNZRUSU6JRWK=
human MV-4-11 cell NVXjZm5lT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVfJcohq[mm2aX;uJI9nKGi3bXHuJG1XNTRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25OE44OyCwTT6= MX3TRW5ITVJ?
human EGI-1 cell M1v5Z2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFntRWRKdmirYnn0bY9vKG:oIHj1cYFvKEWJST2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVUvQDFibl2u NUXwbHRpW0GQR1XS
human NCI-SNU-1 cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoPBTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvU17VMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Pi55MzDuUU4> MnrTV2FPT0WU
human MEG-01 cell MlHZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnrZTY5pcWKrdHnvckBw\iCqdX3hckBOTUdvMEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25O{44PyCwTT6= MV;TRW5ITVJ?
human OMC-1 cell MnizS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mm[yTY5pcWKrdHnvckBw\iCqdX3hckBQVUNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwNE4zOyCwTT6= M3fLTHNCVkeHUh?=
human NB10 cell NG\0cmRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1vu[mlvcGmkaYTpc44hd2ZiaIXtZY4hVkJzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwNE41OiCwTT6= M2\iO3NCVkeHUh?=
human CAL-62 cell MmrnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUTJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC14MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwNE44QCCwTT6= M{P6XnNCVkeHUh?=
human NCI-H2087 cell M1nBOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{GwUGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFg4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTBzLkG0JI5ONg>? MkLJV2FPT0WU
human MDA-MB-175-VII cell NXLRdGFnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVjJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2xO|UuXkmLIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYm= Ml;TV2FPT0WU
human LS-513 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVjJcohq[mm2aX;uJI9nKGi3bXHuJGxUNTVzMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGxOE45OyCwTT6= MVLTRW5ITVJ?
human HN cell growth NIXIRopIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHTDWJJKdmirYnn0bY9vKG:oIHj1cYFvKEiQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKyMlU6KG6PLh?= M3zRfXNCVkeHUh?=
human ABC-1 cell M1L6WGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mm\hTY5pcWKrdHnvckBw\iCqdX3hckBCSkNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGyN{4xOiCwTT6= NF3hN2RUSU6JRWK=
human SJSA-1 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4n1OWlvcGmkaYTpc44hd2ZiaIXtZY4hW0qVQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVI{NjF7IH7NMi=> M4XUVnNCVkeHUh?=
human PANC1 cells MVTGeY5kfGmxbjDhd5NigQ>? MVGxNEDPxE1? NIfQdXoyKGh? M4X4[mlvcGmkaYTpc44hd2ZiTVXLNUBqdiCqdX3hckBRSU6FMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4heEW{a{GvNkBt\X[nbDDheEAyOCC3TTDh[pRmeiBzIHjyJIJ6KFenc4Tldo4h[myxdITpcoch[W6jbInzbZM> NH[yXnQzPTd4Nk[zNy=>
human MCF7 cells MkHMSpVv[3Srb36gZZN{[Xl? NGDvSog4PSCvaX7z NFfK[XJKdmirYnn0bY9vKG:oIF3Fb|EwOiCrbjDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKEWUSzDwbI9{eGixconsZZRqd25iYX\0[ZIhPzVibXnud{BjgSCZZYP0[ZJvKGKub4T0bY5oKGGwYXz5d4l{ MUSyN|M6QDR3Mx?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-ERK / p-AKT / Cyclin D1 / p27; 

PubMed: 22573716     


parental or MEK inhibitor-resistant clonal populations (1182, 1183, and 1187) were treated with increasing doses of PD0325901 for 24 hours and subjected to immunoblot analysis using the indicated antibodies.

p-p70S6K(T389) / p4EBP1(S65) / pS6(S235); 

PubMed: 27699948     


Sensitive (MKN-45, OKAJIMA, HSC-57, GUS, NUGC-4, OCUM-1, SNU-719, and IM95) and resistant (SH-10-TC, MKN-1, HSC-39, NCI-N87, H-111-TC, KE-97, SNU-484, and TMK-1) cell lines were treated with DMSO or PD0325901 (0.1 or 1 μM) for 24 h and then subjected to Western blotting using antibodies against pERK, pAKT, p-p70S6K, p4EBP1, pS6, and GAPDH.

cleaved PARP; 

PubMed: 22573716     


NF1-deficient U251 or LN229 GBM cells were treated with PD0325901 for 4 days and subjected to immunoblot analysis using the indicated antibodies.

DR5; 

PubMed: 25867065     


The indicated cancer cell lines were exposed to the given concentrations of the inhibitors as indicated for 16 h.

22573716 27699948 25867065
Immunofluorescence
Fibronectin / Actin / pFAK; 

PubMed: 28187762     


Representative immunofluorescence images of FNMA by GBM-3 cells treated either with DMSO (b) or PD0325901 (c). Fibronectin is depicted in green and DAPI (blue) was used as counterstain. PD0325901 did not appear to induce FNMA by GBM-3 cells. Rhodamine-phalloidin staining of actin in DMSO-treated (d) or PD0325901-treated GBM-3 cells (e). Note significant cell shape change and actin fiber organization. Scale bar in (e) is 5 μm. Triple stain for actin (red), p-FAK (green) and DAPI (blue) in DMSO-treated (f) and PD0325901-treated (g) GBM-3 cells. PD0325901 appears to induce the localization of p-FAK at sites of cell-ECM attachment. Thirty-micron thick z-stack of DMSO (h) and PD0325901-treated (i) collected by confocal microscopy of multicellular aggregates of GBM-3. Note marked change in actin organization from cortical to stress fibers. Scale bar in (i) is 30 μm.

ZO-1; 

PubMed: 25394671     


16HBE cells were fixed and stained for ZO-1 and DNA. Scale bar, 20 μm.

28187762 25394671
In vivo The improved potency of PD0325901 relative to CI-1040 is evident. A single oral dose of PD0325901 (25 mg/kg) inhibits phosphorylation of ERK by more than 50% at 24 hours post-dosing. In contrast, CI-1040 at a much higher dose (150 mg/kg) only inhibit pERK levels for roughly 8 hours, returning to control levels by 24 hours after treatment. [2] Therefore, the dose required to produce a 70% incidence of complete tumor responses (C26 model) is 25 mg/kg/day versus 900 mg/kg/day for PD0325901 and CI-1040, respectively. Anticancer activity of PD 0325901 has been demonstrated for a broad spectrum of human tumor xenografts. [2] After 1 week of oral administration of PD0325901 (20–25 mg/kg/day) in mice, no tumor growth is detected in mice inoculated with PTC cells bearing a BRAF mutation. [3] For PTC with the RET/PTC1 rearrangement, the average tumor volume of the orthotopic tumor is decreased by 58% as compared with controls. In conclusion, PTC cells carrying a BRAF mutation are more sensitive to PD0325901 than are PTC cells carrying the RET/PTC1 rearrangement. [3]

Protocol

Kinase Assay:

[1]
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In vitro cascade assay:

Incorporation of 32P into myelin basic protein (MBP) is assayed in the presence of a glutathione S-transferase fusion protein containing p44MAP kinase (GST-MAPK) and a glutathione S-transferase protein containing p45MEK (GST-MEK). The assay solution contained 20 mM HEPES, pH 7.4, 10 mM MgCl2, 1 mM MnCl2, 1 mM EGTA, 50 mM [gamma-32P]ATP, 10 mg GST-MEK, 0.5 mg GST-MAPK and 40 mg MBP in a final volume of 100 mL. Reactions are stopped after 20 minutes by addition of trichloroacetic acid and filtered through a GF/C filter mat. 32P retained on the filter mat is determined using a 1205 Betaplate. PD0325901 is assessed at various dose ranges in order to determine dose response curves.
Cell Research:

[3]
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  • Cell lines: PTC cells
  • Concentrations: 0.1 nM- 1 μM
  • Incubation Time: 48 hours
  • Method:

    PTC cells (1 × 104) are seeded in 24-well plates with 1 mL of medium for 4 days in a 37 °C incubator. MEK inhibitor PD0325901 at varying concentrations is added to the cells in triplicate on day 0. MTT dissolved in 0.8% NaCl solution at 5 mg/mL is added to each well (0.2 mL) on day 2 to test GI50 or every day for cell growth curves. The cells are incubated at 37 °C for 3 hours with MTT. The liquid is then aspirated from the wells and discarded. Stained cells are dissolved in 0.5 mL of DMSO and their absorption at 570 nm is measured using a Synergy HT multidetection microplate reader. For GI50, cell growth is calculated as 100 × (T − T0)/(C − T0), where T is the optical density of the wells treated with inhibitors after a 48-hour period, T0 is the optical density at time zero, and C is the control optical density with DMSO only.


    (Only for Reference)
Animal Research:

[3]
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  • Animal Models: Ncr-nu/nu mice bearing PTC cells
  • Dosages: 20-25 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 96 mg/mL (199.09 mM)
Ethanol 40 mg/mL (82.95 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
For best results, use promptly after mixing. 		5mg/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 482.19
Formula

C16H14F3IN2O4
CAS No. 391210-10-9
Storage powder
in solvent
Synonyms N/A
Smiles OCC(O)CONC(=O)C1=C(NC2=CC=C(I)C=C2F)C(=C(F)C=C1)F

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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
    V1
    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

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.

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Frequently Asked Questions

  • Question 1:

    Whether the inhibitor PD0325901 interacts with other targets other than MEK?

  • Answer:

    PD0325901 has very high selectivity to MEK. In addition, it can also inhibits VEGF activity according to the reference: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2713590/

selleck catalog

MEK Signaling Pathway Map

MEK Inhibitors with Unique Features

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  • Trametinib (GSK1120212)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID