Mirdametinib (PD0325901)

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Licensed by Pfizer Catalog No.S1036

567 publications

Mirdametinib (PD0325901) Chemical Structure

CAS No. 391210-10-9

Mirdametinib (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 Mirdametinib (PD0325901) has been cited by 567 publications

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Biological Activity

Description Mirdametinib (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 MmnUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmHwTY5pcWKrdHnvckBw\iCqdX3hckBEUFBvMkGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42Ojdibl2u NEG3WYxUSU6JRWK=
human M14 cell M2\POmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV3Jcohq[mm2aX;uJI9nKGi3bXHuJG0yPCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEWgcm0v NFmyNVFUSU6JRWK=
human SK-MEL-28 cell MlqzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHzkcoxKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0zQCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNUKgcm0v MVnTRW5ITVJ?
human NOMO-1 cell MnjUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmXWTY5pcWKrdHnvckBw\iCqdX3hckBPV02RLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlA4KG6PLh?= MWXTRW5ITVJ?
human A375 cell M1\sS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnfXTY5pcWKrdHnvckBw\iCqdX3hckBCOzd3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj62PUBvVS5? M1[yU3NCVkeHUh?=
human DU-4475 cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1Tm[2lvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPTdibl2u MVjTRW5ITVJ?
human C32 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFmzdGNKdmirYnn0bY9vKG:oIHj1cYFvKEN|MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuOlchdk1w NXT3[md2W0GQR1XS
human BPH-1 cell NUjXTopzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnjtTY5pcWKrdHnvckBw\iCqdX3hckBDWEhvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVUhdk1w MV\TRW5ITVJ?
human CP50-MEL-B cell M2TWVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1z3bWlvcGmkaYTpc44hd2ZiaIXtZY4hS1B3MD3NSWwuSiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwNUigcm0v MkTHV2FPT0WU
human H9 cell NG\rVVlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEfTXFNKdmirYnn0bY9vKG:oIHj1cYFvKEh7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT63O{BvVS5? M32w[XNCVkeHUh?=
human HTC-C3 cell NEn2coZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmriTY5pcWKrdHnvckBw\iCqdX3hckBJXENvQ{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlg6KG6PLh?= NFvmZZFUSU6JRWK=
human BHT-101 cell NHjTNVRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUfJcohq[mm2aX;uJI9nKGi3bXHuJGJJXC1zMEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22Mlchdk1w M3fvRXNCVkeHUh?=
human COLO-741 cell MmTES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MojJTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLUe0NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvOSCwTT6= MlXUV2FPT0WU
human OVCAR-5 cell Mmr0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWPJcohq[mm2aX;uJI9nKGi3bXHuJG9XS0GULUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23MlgzKG6PLh?= NGTSbVZUSU6JRWK=
human A549 cell NF\lOpVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHHVdnFKdmirYnn0bY9vKG:oIHj1cYFvKEF3NEmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23Mlg6KG6PLh?= NF7CWYRUSU6JRWK=
human SH-4 cell growth M3LoXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX;Jcohq[mm2aX;uJI9nKGi3bXHuJHNJNTRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD16LkK2JI5ONg>? NGTWfFNUSU6JRWK=
human SK-N-AS cell MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGDvPIZKdmirYnn0bY9vKG:oIHj1cYFvKFONLV6tRXMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05NjR2IH7NMi=> M1\Sd3NCVkeHUh?=
human HT-144 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2i2emlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMUS0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PE46PyCwTT6= NGHCWpJUSU6JRWK=
human MEL-HO cell NUXRV5J2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVf3VIFCUW6qaXLpeIlwdiCxZjDoeY1idiCPRVytTG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjR7IH7NMi=> MnzpV2FPT0WU
human COLO-679 cell MnvvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MULJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vNke5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvODFibl2= NEjmU4VUSU6JRWK=
human HuP-T4 cell NVnm[4NRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkCxTY5pcWKrdHnvckBw\iCqdX3hckBJfVBvVESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE46QCCwTT6= M1PDOXNCVkeHUh?=
human H-EMC-SS cell NI\l[lBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{fIbWlvcGmkaYTpc44hd2ZiaIXtZY4hUC2HTVOtV3Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS5yMjDuUU4> MX3TRW5ITVJ?
human LB2518-MEL cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUPJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjVzOD3NSWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS5zMzDuUU4> NW\TZoJFW0GQR1XS
human HL-60 cell M2X3Xmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV6yb3V6UW6qaXLpeIlwdiCxZjDoeY1idiCKTD22NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjF3IH7NMi=> M1vvbnNCVkeHUh?=
human NCI-H1666 cell NFLObHRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVrNRnA6UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PjZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMT6xO{BvVS5? MorMV2FPT0WU
human A101D cell NVe5Xoo3T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4nlUWlvcGmkaYTpc44hd2ZiaIXtZY4hSTFyMVSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNU41PSCwTT6= M2DzZ3NCVkeHUh?=
human RVH-421 cell NWjNVW9kT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUOxNotvUW6qaXLpeIlwdiCxZjDoeY1idiCUVlitOFIyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwNkSgcm0v MVrTRW5ITVJ?
human Hs-578-T cell Ml3sS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYLJcohq[mm2aX;uJI9nKGi3bXHuJGh{NTV5OD3UJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVIvPzlibl2u NH3QOWJUSU6JRWK=
human A375 cells Moe4VJJwdGmoZYLheIlwdiCjc4PhfS=> NWPNRZdiPzJiaB?= M1LIN2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OUBk\WyuczDlfJBz\XO|aX7nJGJTSUZiVk[wNGUhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3ME2xN{BvVS5? NUWwd2FOOjN2N{SzPFg>
human DOK cell NHzpb|FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWTtRXV1UW6qaXLpeIlwdiCxZjDoeY1idiCGT1ugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{41KG6PLh?= NHX4fVdUSU6JRWK=
human Mewo cell M2XveWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXrJcohq[mm2aX;uJI9nKGi3bXHuJG1mf29iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zND60OUBvVS5? M{TnSHNCVkeHUh?=
human ONS-76 cell M1Gxfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX7Jcohq[mm2aX;uJI9nKGi3bXHuJG9PWy15NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlUyKG6PLh?= MlKzV2FPT0WU
human UACC-257 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXTJcohq[mm2aX;uJI9nKGi3bXHuJHVCS0NvMkW3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPjJibl2u MkPLV2FPT0WU
human SW626 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIrE[XZKdmirYnn0bY9vKG:oIHj1cYFvKFOZNkK2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvQTFibl2u NXG5R4p{W0GQR1XS
human SW620 cell M3Xx[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnTYTY5pcWKrdHnvckBw\iCqdX3hckBUXzZ{MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0Mlk2KG6PLh?= M33Zc3NCVkeHUh?=
human TYK-nu cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHnaSIZKdmirYnn0bY9vKG:oIHj1cYFvKFS\Sz3ueUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjF|IH7NMi=> M4LpfHNCVkeHUh?=
human ACN cell NX:0[nA2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYjhdmtXUW6qaXLpeIlwdiCxZjDoeY1idiCDQ16gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU44PiCwTT6= Mom0V2FPT0WU
human MIAPaCa2 cells MmDlVJJwdGmoZYLheIlwdiCjc4PhfS=> MVnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2LQWDhR4EzKGOnbHzzMEBKSzVyPUG3JI5ONg>? MV:yN|Q4PDN6OB?=
human T-24 cell MnPwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUfJcohq[mm2aX;uJI9nKGi3bXHuJHQuOjRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zOT63NUBvVS5? MVvTRW5ITVJ?
human AGS cell MonBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXHMTnlGUW6qaXLpeIlwdiCxZjDoeY1idiCDR2OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNE41OSCwTT6= MXTTRW5ITVJ?
human SW872 cell NGDCN5ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXXJcohq[mm2aX;uJI9nKGi3bXHuJHNYQDd{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkeuPVkhdk1w NF3rVI9USU6JRWK=
human C2BBe1 cell NFXlN5ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVXCXlBpUW6qaXLpeIlwdiCxZjDoeY1idiCFMlLC[VEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQC53NDDuUU4> NH;SfJlUSU6JRWK=
human MZ7-mel cell NHPIWYZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mlz2TY5pcWKrdHnvckBw\iCqdX3hckBOYjdvbXXsJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlkvPDNibl2u NUTy[WZEW0GQR1XS
human HCC2998 cell MnXGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3q5VWlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkm5PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM{NjZ4IH7NMi=> M3rQWXNCVkeHUh?=
human HO-1-N-1 cell NIfJcoVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1HtSGlvcGmkaYTpc44hd2ZiaIXtZY4hUE9vMT3OMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{PC52MzDuUU4> MX\TRW5ITVJ?
human SW756 cell NYq2PHZ7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVvJcohq[mm2aX;uJI9nKGi3bXHuJHNYPzV4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{SuOFUhdk1w NY\MeW9UW0GQR1XS
human NCI-H1437 cell Ml;RS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVrPNVF2UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE1OzdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|ND60PUBvVS5? M3uw[nNCVkeHUh?=
human NCI-H747 cell NWrFT3hvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn7ZTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEe0O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM1Njl6IH7NMi=> NVrqXZBMW0GQR1XS
human SK-MEL-2 cell NYPPXmczT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2fZPWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{PS5{IH7NMi=> NY\DdGtmW0GQR1XS
human MZ2-MEL cell NFrxbYRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3XrSmlvcGmkaYTpc44hd2ZiaIXtZY4hVVp{LV3FUEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM2NjZ3IH7NMi=> NHfHR2ZUSU6JRWK=
human PSN1 cell MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmK5TY5pcWKrdHnvckBw\iCqdX3hckBRW05zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{iuOFUhdk1? Mke5V2FPT0WU
human CAL-39 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWnJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC1|OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO5MlA1KG6PLh?= MoDMV2FPT0WU
human LOXIMVI cell NYOySXE2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYraWnZ6UW6qaXLpeIlwdiCxZjDoeY1idiCOT2jJUXZKKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzlwM{mgcm0v MULTRW5ITVJ?
human COLO-792 cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkfjTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLUe5NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ{NjF3IH7NMi=> NYDMbXY4W0GQR1XS
human CAL-27 cell MkLVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{D3c2lvcGmkaYTpc44hd2ZiaIXtZY4hS0GOLUK3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFQvQTFibl2= NG\oPFdUSU6JRWK=
human AsPC-1 cell M4LX[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmjRTY5pcWKrdHnvckBw\iCqdX3hckBCe1CFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20OU4zQCCwTT6= MmnjV2FPT0WU
human NCI-H2291 cell M{PIeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mk\hTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKyPVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Pi52NjDuUU4> M{XFdXNCVkeHUh?=
human RCM-1 cell NX\RcGhVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoPPTY5pcWKrdHnvckBw\iCqdX3hckBTS01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS2Mlg2KG6PLh?= NF7sWpNUSU6JRWK=
human NCI-H292 cell Mmn1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF;IbnNKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlkzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PDdwM{mgcm0v MYfTRW5ITVJ?
human WM-115 cell NUXnNFVkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVTJcohq[mm2aX;uJI9nKGi3bXHuJHdONTFzNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS4MlUhdk1w NWDwTlYxW0GQR1XS
human RT-112 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVjJcohq[mm2aX;uJI9nKGi3bXHuJHJVNTFzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS4Mlg1KG6PLh?= M{LVRXNCVkeHUh?=
human HT-29 cell M1fiXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGhVNTJ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUCuOFkhdk1w NWm1ZpRlW0GQR1XS
human RKO cell growth MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFvGN3NKdmirYnn0bY9vKG:oIHj1cYFvKFKNTzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWyMlAzKG6PLh?= MojrV2FPT0WU
human KY821 cell MojRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXXOSVN{UW6qaXLpeIlwdiCxZjDoeY1idiCNWUiyNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVU{NjNibl2u NWWxPY5vW0GQR1XS
human LB1047-RCC cell NYfwem9TT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUniSnNZUW6qaXLpeIlwdiCxZjDoeY1idiCOQkGwOFcuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUmuOlUhdk1w NHLVT49USU6JRWK=
human SW1116 cell NEO4XHNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUX2[XIyUW6qaXLpeIlwdiCxZjDoeY1idiCVV{GxNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03OC52OTDuUU4> NVXhTWg1W0GQR1XS
human P12-ICHIKAWA cell NGLvWYRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1TR[2lvcGmkaYTpc44hd2ZiaIXtZY4hWDF{LVnDTGlMSVeDIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NkKuNlchdk1w M2\kTnNCVkeHUh?=
human HCC70 cell M3XWc2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mm\0TY5pcWKrdHnvckBw\iCqdX3hckBJS0N5MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[zMlAyKG6PLh?= NUjx[|Z[W0GQR1XS
human MIA-PaCa-2 cell NFPhfpdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXL2[HdlUW6qaXLpeIlwdiCxZjDoeY1idiCPSVGtVIFE[S1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NkOuOVMhdk1w NGj5SoNUSU6JRWK=
human LoVo cell NVv3WXViT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGxwXm9iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14NT6yPUBvVS5? NGS5XItUSU6JRWK=
human LB2241-RCC cell NUf6[XoxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2K0OWlvcGmkaYTpc44hd2ZiaIXtZY4hVEJ{MkSxMXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZ3LkWyJI5ONg>? MUjTRW5ITVJ?
human GAK cell MlyzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVrJcohq[mm2aX;uJI9nKGi3bXHuJGdCUyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZ4Lki3JI5ONg>? MmLGV2FPT0WU
human RD cell NIfrZVlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYLJcohq[mm2aX;uJI9nKGi3bXHuJHJFKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PjdwMTDuUU4> NInmXZNUSU6JRWK=
human KNS-62 cell NYLqdpo4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX\lVW5[UW6qaXLpeIlwdiCxZjDoeY1idiCNTmOtOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03QS57OTDuUU4> MXzTRW5ITVJ?
human HD-MY-Z cell NWK2UZdFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXXJcohq[mm2aX;uJI9nKGi3bXHuJGhFNU2\LWqgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23NU4yOiCwTT6= NH3tNIJUSU6JRWK=
human COR-L105 cell M1zIb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHu4O|RKdmirYnn0bY9vKG:oIHj1cYFvKEORUj3MNVA2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PzFwN{Ggcm0v NEi0dZVUSU6JRWK=
human IA-LM cell NH7DPIdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{TyTWlvcGmkaYTpc44hd2ZiaIXtZY4hUUFvTF2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23N{4zQCCwTT6= MVPTRW5ITVJ?
human EM-2 cell M3\zZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmPzTY5pcWKrdHnvckBw\iCqdX3hckBGVS1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;N{SuO{BvVS5? NIq2Zm1USU6JRWK=
human NB69 cell M{XxeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV\Jcohq[mm2aX;uJI9nKGi3bXHuJG5DPjliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeR?= NV3QVnliW0GQR1XS
human HuP-T3 cell MnW1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4PpbWlvcGmkaYTpc44hd2ZiaIXtZY4hUHWSLWSzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFMvQTNibl2u Mn3nV2FPT0WU
human BB30-HNC cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEfIfGhKdmirYnn0bY9vKG:oIHj1cYFvKEKEM{CtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QDVwNUGgcm0v NIP0dldUSU6JRWK=
human HT-1080 cell M4KzT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYnHNFdCUW6qaXLpeIlwdiCxZjDoeY1idiCKVD2xNFgxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QDVwOEigcm0v MU\TRW5ITVJ?
human RMG-I cell NGDF[HFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVTnWIE1UW6qaXLpeIlwdiCxZjDoeY1idiCUTVetTUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVg4NjN2IH7NMi=> NHHudotUSU6JRWK=
human HCC1419 cell MmTxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3TTOGlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUSxPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkyNjN6IH7NMi=> NF7lVJJUSU6JRWK=
human SW780 cell NV;XfIx1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MonTTY5pcWKrdHnvckBw\iCqdX3hckBUXzd6MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmyMlMzKG6PLh?= MY\TRW5ITVJ?
human SNU-387 cell Mn7QS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEG0[HlKdmirYnn0bY9vKG:oIHj1cYFvKFOQVT2zPFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Oy5|NjDuUS=> NG\5NYxUSU6JRWK=
human LAMA-84 cell NH2wbnNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1n6UWlvcGmkaYTpc44hd2ZiaIXtZY4hVEGPQT24OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk1NjZ6IH7NMi=> NFXEUW5USU6JRWK=
human MV-4-11 cell NUizUVltT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2PIeGlvcGmkaYTpc44hd2ZiaIXtZY4hVVZvND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk1Njd|IH7NMi=> NWjoPVJzW0GQR1XS
human EGI-1 cell MmfNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2\Y[WlvcGmkaYTpc44hd2ZiaIXtZY4hTUeLLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25OU45OSCwTT6= MnTRV2FPT0WU
human NCI-SNU-1 cell NYD3VVJLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHLkeoVKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3TUnUuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTl4LkezJI5ONg>? NV3WZpU6W0GQR1XS
human MEG-01 cell MkXtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWfJcohq[mm2aX;uJI9nKGi3bXHuJG1GTy1yMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm3Mlc4KG6PLh?= M4TXTnNCVkeHUh?=
human OMC-1 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1rKRWlvcGmkaYTpc44hd2ZiaIXtZY4hV02FLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNFAvOjNibl2u MnnxV2FPT0WU
human NB10 cell MnTES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWfJcohq[mm2aX;uJI9nKGi3bXHuJG5DOTBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMECuOFIhdk1w NFrZXppUSU6JRWK=
human CAL-62 cell M{X6PGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MofRTY5pcWKrdHnvckBw\iCqdX3hckBESUxvNkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNFAvPzhibl2u Mk\zV2FPT0WU
human NCI-H2087 cell NETk[YtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mlf5TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwPFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yODFwMUSgcm0v MWLTRW5ITVJ?
human MDA-MB-175-VII cell M4ft[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NW\IbpZ6UW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuOTd3LW\JTUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6 NYDCXVNRW0GQR1XS
human LS-513 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoHMTY5pcWKrdHnvckBw\iCqdX3hckBNWy13MUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNVQvQDNibl2u MYrTRW5ITVJ?
human HN cell growth M{HBZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{HafmlvcGmkaYTpc44hd2ZiaIXtZY4hUE5iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMkKuOVkhdk1w M2PmVHNCVkeHUh?=
human ABC-1 cell NV7t[YpHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH7PWW1KdmirYnn0bY9vKG:oIHj1cYFvKEGEQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVI{NjB{IH7NMi=> M2jZVHNCVkeHUh?=
human SJSA-1 cell MlTFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2DtWWlvcGmkaYTpc44hd2ZiaIXtZY4hW0qVQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVI{NjF7IH7NMi=> M1fsUnNCVkeHUh?=
human PANC1 cells NET2OWhHfW6ldHnvckBie3OjeR?= NIfxOYIyOCEQvF2= NVjne5V[OSCq Mke4TY5pcWKrdHnvckBw\iCPRVuxJIlvKGi3bXHuJHBCVkNzIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBxTXKtMT:yJIxmfmWuIHH0JFExKHWPIHHmeIVzKDFiaIKgZpkhX2W|dHXyckBjdG:2dHnu[{BidmGueYPpdy=> M4rnRlI2PzZ4NkOz
human MCF7 cells MXjGeY5kfGmxbjDhd5NigQ>? NXHjS3NyPzVibXnudy=> NF7ZU4NKdmirYnn0bY9vKG:oIF3Fb|EwOiCrbjDoeY1idiCPQ1[3JINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKEWUSzDwbI9{eGixconsZZRqd25iYX\0[ZIhPzVibXnud{BjgSCZZYP0[ZJvKGKub4T0bY5oKGGwYXz5d4l{ NGW5ZnMzOzN7OES1Ny=>

... 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]
- Collapse
  • 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 C1=CC(=C(C=C1I)F)NC2=C(C=CC(=C2F)F)C(=O)NOCC(CO)O

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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

Related MEK Products

  • Cobimetinib (GDC-0973) New

    Cobimetinib (GDC-0973, RG7420) is a potent and highly selective MEK1 inhibitor with IC50 of 4.2 nM, showing more than 100-fold selectively for MEK1 over MEK2 and showed no significant inhibition when tested against a panel of more than 100 of serine-threonine and tyrosine kinases. Cobimetinib induces apoptosis. Phase 3.

  • BI-847325 New

    BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.

  • GDC-0623 New

    GDC-0623 (G-868) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.

  • Trametinib (GSK1120212)

    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.

  • Selumetinib (AZD6244)

    Selumetinib (AZD6244, ARRY-142886) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Selumetinib suppresses cell proliferation, migration and trigger apoptosis. Phase 3.

    Features:First MEK inhibitor being tested in Phase II clinical trials.

  • U0126-EtOH

    U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM in cell-free assays, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD98059. U0126 inhibits autophagy and mitophagy with antiviral activity.

    Features:A chemically synthesized and highly selective inhibitor of both MEK1 and MEK2.

  • PD98059

    PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR) and functions as an AHR antagonist.

    Features:Does not inhibit c-Raf phosphorylated MEK1.

  • PD184352 (CI-1040)

    PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. PD184352 (CI-1040) selectively induces apoptosis. Phase 2.

    Features:First MEK inhibitor to begin clinical development.

  • Binimetinib (MEK162)

    Binimetinib (MEK162, ARRY-162, ARRY-438162) is a potent inhibitor of MEK1/2 with IC50 of 12 nM in a cell-free assay. Binimetinib induces G1 cell cycle arrest and apoptosis in human NSCLC cell lines and induces autophagy. Phase 3.

  • Refametinib (RDEA119)

    Refametinib (RDEA119, Bay 86-9766) is a potent, ATP non-competitive and highly selective inhibitor of MEK1 and MEK2 with IC50 of 19 nM and 47 nM, respectively.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID