Mirdametinib (PD0325901)

For research use only.

Licensed by Pfizer Catalog No.S1036

509 publications

Mirdametinib (PD0325901) Chemical Structure

Molecular Weight(MW): 482.19

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 509 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 NX22UIdwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUjUe4s5UW6qaXLpeIlwdiCxZjDoeY1idiCFSGCtNlEzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC53Mkegcm0v M1zMU3NCVkeHUh?=
human M14 cell NHvBZo5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mnr3TY5pcWKrdHnvckBw\iCqdX3hckBOOTRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkS1JI5ONg>? MXzTRW5ITVJ?
human SK-MEL-28 cell M4P2XWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MULJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPTJibl2u NUXuToxUW0GQR1XS
human NOMO-1 cell Mm\IS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkGyTY5pcWKrdHnvckBw\iCqdX3hckBPV02RLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlA4KG6PLh?= NF64blZUSU6JRWK=
human A375 cell NHXJdoFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVH0W2xQUW6qaXLpeIlwdiCxZjDoeY1idiCDM{e1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk43QSCwTT6= MlOzV2FPT0WU
human DU-4475 cell M4jlT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mlf2TY5pcWKrdHnvckBw\iCqdX3hckBFXS12NEe1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{42PyCwTT6= M2r4RXNCVkeHUh?=
human C32 cell M4P4cmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXnJcohq[mm2aX;uJI9nKGi3bXHuJGM{OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNwNkegcm0v NGfMSIdUSU6JRWK=
human BPH-1 cell M3znbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYjJcohq[mm2aX;uJI9nKGi3bXHuJGJRUC1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz65OUBvVS5? M4LLOnNCVkeHUh?=
human CP50-MEL-B cell M4XTSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVnJcohq[mm2aX;uJI9nKGi3bXHuJGNRPTBvTVXMMWIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjV6IH7NMi=> MXjTRW5ITVJ?
human H9 cell NWHrbm5yT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWPJcohq[mm2aX;uJI9nKGi3bXHuJGg6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS55NzDuUU4> MkHLV2FPT0WU
human HTC-C3 cell NHXscnlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHTaN4hKdmirYnn0bY9vKG:oIHj1cYFvKEiWQz3DN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQDlibl2u M{\TUXNCVkeHUh?=
human BHT-101 cell M{\0TGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVXvSI5nUW6qaXLpeIlwdiCxZjDoeY1idiCESGStNVAyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi55IH7NMi=> MV\TRW5ITVJ?
human COLO-741 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoXyTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLUe0NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvOSCwTT6= NEH6eIRUSU6JRWK=
human OVCAR-5 cell M3XMdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1rKd2lvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvQDJibl2u MkX5V2FPT0WU
human A549 cell MmnVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXzJcohq[mm2aX;uJI9nKGi3bXHuJGE2PDliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD15Lki5JI5ONg>? NUnnZ3l6W0GQR1XS
human SH-4 cell growth MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnTiTY5pcWKrdHnvckBw\iCqdX3hckBUUC12IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OD6yOkBvVS5? NW\s[4NxW0GQR1XS
human SK-N-AS cell NFHZclNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHL0RW9KdmirYnn0bY9vKG:oIHj1cYFvKFONLV6tRXMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05NjR2IH7NMi=> NYGxeJZUW0GQR1XS
human HT-144 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHu1WllKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUG0OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVgvQTdibl2u NIDESXpUSU6JRWK=
human MEL-HO cell MonpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXizVopuUW6qaXLpeIlwdiCxZjDoeY1idiCPRVytTG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjR7IH7NMi=> MoC5V2FPT0WU
human COLO-679 cell MoezS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV3Jcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vNke5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvODFibl2= MmCyV2FPT0WU
human HuP-T4 cell NGLqZ|FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NU\GVpg4UW6qaXLpeIlwdiCxZjDoeY1idiCKdWCtWFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC57ODDuUU4> MoK5V2FPT0WU
human H-EMC-SS cell NFPiZo1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1LRPWlvcGmkaYTpc44hd2ZiaIXtZY4hUC2HTVOtV3Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS5yMjDuUU4> MVPTRW5ITVJ?
human LB2518-MEL cell M3\URmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGxDOjVzOD3NSWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS5zMzDuUU4> NUjpZYN[W0GQR1XS
human HL-60 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYrJcohq[mm2aX;uJI9nKGi3bXHuJGhNNTZyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUGuNVUhdk1w M3;SNHNCVkeHUh?=
human NCI-H1666 cell Mn\yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mm\nTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG2OlYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS5zNzDuUU4> NY\nZWJZW0GQR1XS
human A101D cell MoKyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4O0OWlvcGmkaYTpc44hd2ZiaIXtZY4hSTFyMVSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNU41PSCwTT6= MmDaV2FPT0WU
human RVH-421 cell MlS3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NETZVFlKdmirYnn0bY9vKG:oIHj1cYFvKFKYSD20NlEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi54NDDuUU4> NEHlNGpUSU6JRWK=
human Hs-578-T cell NXTqd2xST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVv6WJBWUW6qaXLpeIlwdiCxZjDoeY1idiCKcz21O|guXCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{Lke5JI5ONg>? MlvmV2FPT0WU
human A375 cells M4fzPHBzd2yrZnXyZZRqd25iYYPzZZk> NH7TT484OiCq M3W4S2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OUBk\WyuczDlfJBz\XO|aX7nJGJTSUZiVk[wNGUhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3ME2xN{BvVS5? M2PzdVI{PDd2M{i4
human DOK cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkHKTY5pcWKrdHnvckBw\iCqdX3hckBFV0tiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz60JI5ONg>? M4\vR3NCVkeHUh?=
human Mewo cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2XZcGlvcGmkaYTpc44hd2ZiaIXtZY4hVWW5bzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlQ2KG6PLh?= M322cnNCVkeHUh?=
human ONS-76 cell NGjCSJZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{f1d2lvcGmkaYTpc44hd2ZiaIXtZY4hV06VLUe2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPTFibl2u MoTRV2FPT0WU
human UACC-257 cell NYTSfnNOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYDITY1nUW6qaXLpeIlwdiCxZjDoeY1idiCXQVPDMVI2PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF2Lk[yJI5ONg>? Mne3V2FPT0WU
human SW626 cell NF\ZV5pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYLiW|A4UW6qaXLpeIlwdiCxZjDoeY1idiCVV{[yOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjlzIH7NMi=> NIPnZmVUSU6JRWK=
human SW620 cell MlPmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnW1TY5pcWKrdHnvckBw\iCqdX3hckBUXzZ{MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0Mlk2KG6PLh?= NFzYNXhUSU6JRWK=
human TYK-nu cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NETReoFKdmirYnn0bY9vKG:oIHj1cYFvKFS\Sz3ueUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjF|IH7NMi=> NXKzTJpVW0GQR1XS
human ACN cell NUHVNG5oT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{n0bmlvcGmkaYTpc44hd2ZiaIXtZY4hSUOQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuO|Yhdk1w NILyOZpUSU6JRWK=
human MIAPaCa2 cells MmDFVJJwdGmoZYLheIlwdiCjc4PhfS=> NXi1O4xJSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNTWFR[UOjMjDj[YxteyxiSVO1NF0yPyCwTT6= M{DWUVI{PDd2M{i4
human T-24 cell NEXvZpVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUHJcohq[mm2aX;uJI9nKGi3bXHuJHQuOjRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zOT63NUBvVS5? Mnq5V2FPT0WU
human AGS cell NVTHeVZbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWe0cmJ1UW6qaXLpeIlwdiCxZjDoeY1idiCDR2OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNE41OSCwTT6= M13nR3NCVkeHUh?=
human SW872 cell NITHc3RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIfIO|dKdmirYnn0bY9vKG:oIHj1cYFvKFOZOEeyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlcvQTlibl2u NUnvZW5MW0GQR1XS
human C2BBe1 cell NIPnfXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnLWTY5pcWKrdHnvckBw\iCqdX3hckBEOkKEZUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yPE42PCCwTT6= MWPTRW5ITVJ?
human MZ7-mel cell MnLES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGHPbI9KdmirYnn0bY9vKG:oIHj1cYFvKE2cNz3t[Ywh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQS52MzDuUU4> Mn;SV2FPT0WU
human HCC2998 cell NXXKOFJHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHXPe4NKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{K5PVgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Oy54NjDuUU4> NUHYVXVVW0GQR1XS
human HO-1-N-1 cell M4XxOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYLJcohq[mm2aX;uJI9nKGi3bXHuJGhQNTFvTj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|QvPDNibl2u MkX2V2FPT0WU
human SW756 cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYH4d5dxUW6qaXLpeIlwdiCxZjDoeY1idiCVV{e1OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM1NjR3IH7NMi=> NXPRd21[W0GQR1XS
human NCI-H1437 cell Moq0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUDje|RTUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE1OzdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|ND60PUBvVS5? MXXTRW5ITVJ?
human NCI-H747 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVTJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KN{S3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|QvQThibl2u MkD4V2FPT0WU
human SK-MEL-2 cell NVexXZlnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4q5fWlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{PS5{IH7NMi=> MWTTRW5ITVJ?
human MZ2-MEL cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1PS[WlvcGmkaYTpc44hd2ZiaIXtZY4hVVp{LV3FUEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM2NjZ3IH7NMi=> NF;tcnhUSU6JRWK=
human PSN1 cell M2rLd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV3HT3hoUW6qaXLpeIlwdiCxZjDoeY1idiCSU16xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|gvPDVibl2= MW\TRW5ITVJ?
human CAL-39 cell NFn1[olIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWHJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC1|OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO5MlA1KG6PLh?= MlHVV2FPT0WU
human LOXIMVI cell M{PGZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGPmZWJKdmirYnn0bY9vKG:oIHj1cYFvKEyRWFnNWmkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{QS5|OTDuUU4> NGPad4pUSU6JRWK=
human COLO-792 cell NVvhcolJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWrKd|FHUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVc6OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTR|LkG1JI5ONg>? NHyx[JdUSU6JRWK=
human CAL-27 cell NXXN[llCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYTJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC1{NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS0MlkyKG6P MXTTRW5ITVJ?
human AsPC-1 cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3XSPGlvcGmkaYTpc44hd2ZiaIXtZY4hSXOSQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFUvOjhibl2u M17nZ3NCVkeHUh?=
human NCI-H2291 cell NUnMUXBYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NY\3XoZiUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIzQTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12Nj60OkBvVS5? MYjTRW5ITVJ?
human RCM-1 cell NIPKRXpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWq4O2xtUW6qaXLpeIlwdiCxZjDoeY1idiCUQ12tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ3Njh3IH7NMi=> NEPaWJNUSU6JRWK=
human NCI-H292 cell NHLYNpZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmfKTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEK5NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ4NjN7IH7NMi=> MV;TRW5ITVJ?
human WM-115 cell NHuyb|FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{fjVGlvcGmkaYTpc44hd2ZiaIXtZY4hX01vMUG1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFgvPSCwTT6= M3\BOnNCVkeHUh?=
human RT-112 cell MoOzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWXJcohq[mm2aX;uJI9nKGi3bXHuJHJVNTFzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS4Mlg1KG6PLh?= M4jOOnNCVkeHUh?=
human HT-29 cell MmPMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3nLRWlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21NE41QSCwTT6= NVjvVXZyW0GQR1XS
human RKO cell growth MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{XxTGlvcGmkaYTpc44hd2ZiaIXtZY4hWkuRIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUKuNFIhdk1w NF[0WnpUSU6JRWK=
human KY821 cell NWTBV4hXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1HnXWlvcGmkaYTpc44hd2ZiaIXtZY4hU1l6MkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21N{4{KG6PLh?= NXSySHVDW0GQR1XS
human LB1047-RCC cell MkDQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NETZVWpKdmirYnn0bY9vKG:oIHj1cYFvKEyEMUC0O{1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13OT62OUBvVS5? MonBV2FPT0WU
human SW1116 cell NF\NUnpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1rlbWlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzMUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OlAvPDlibl2u M1zLSXNCVkeHUh?=
human P12-ICHIKAWA cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUHRUpg6UW6qaXLpeIlwdiCxZjDoeY1idiCSMUKtTWNJUUuDV1GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22Nk4zPyCwTT6= MnL5V2FPT0WU
human HCC70 cell NEXMTIdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHzWNHVKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{ewJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OlMvODFibl2u NILnNm9USU6JRWK=
human MIA-PaCa-2 cell NGq1XYtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnLETY5pcWKrdHnvckBw\iCqdX3hckBOUUFvUHHDZU0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PjNwNUOgcm0v MnPzV2FPT0WU
human LoVo cell M17sNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF;Ve4xKdmirYnn0bY9vKG:oIHj1cYFvKEyxVn:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22OU4zQSCwTT6= M{XERXNCVkeHUh?=
human LB2241-RCC cell M{Xj[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXjJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjJ2MT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03PS53MjDuUU4> MYfTRW5ITVJ?
human GAK cell M2HFRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWfJcohq[mm2aX;uJI9nKGi3bXHuJGdCUyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZ4Lki3JI5ONg>? M2X4O3NCVkeHUh?=
human RD cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYLJcohq[mm2aX;uJI9nKGi3bXHuJHJFKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PjdwMTDuUU4> MnjFV2FPT0WU
human KNS-62 cell NHfrWHpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MojjTY5pcWKrdHnvckBw\iCqdX3hckBMVlNvNkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22PU46QSCwTT6= MYDTRW5ITVJ?
human HD-MY-Z cell MmjUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3O0U2lvcGmkaYTpc44hd2ZiaIXtZY4hUERvTWmtXkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcyNjF{IH7NMi=> M4HHUnNCVkeHUh?=
human COR-L105 cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWPJcohq[mm2aX;uJI9nKGi3bXHuJGNQWi2OMUC1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O|EvPzFibl2u MUXTRW5ITVJ?
human IA-LM cell NXHsT4pvT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3S2e2lvcGmkaYTpc44hd2ZiaIXtZY4hUUFvTF2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23N{4zQCCwTT6= NXvqemR3W0GQR1XS
human EM-2 cell NH6xVmpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoHhTY5pcWKrdHnvckBw\iCqdX3hckBGVS1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;N{SuO{BvVS5? NGrMV|BUSU6JRWK=
human NB69 cell M1fES2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVrwTGVoUW6qaXLpeIlwdiCxZjDoeY1idiCQQk[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZk> NHrMVnRUSU6JRWK=
human HuP-T3 cell M4PnVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4WzOGlvcGmkaYTpc44hd2ZiaIXtZY4hUHWSLWSzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFMvQTNibl2u M1;TbHNCVkeHUh?=
human BB30-HNC cell M37ObGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4TYVmlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ|MD3IUmMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05PS53MTDuUU4> M3TIPXNCVkeHUh?=
human HT-1080 cell MmnhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHSwO4RKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUGwPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05PS56ODDuUU4> NFW0U4VUSU6JRWK=
human RMG-I cell NYrte3EzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{jXPWlvcGmkaYTpc44hd2ZiaIXtZY4hWk2JLVmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24O{4{PCCwTT6= NYrQWGNpW0GQR1XS
human HCC1419 cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{mxeGlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUSxPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkyNjN6IH7NMi=> NGe3WlZUSU6JRWK=
human SW780 cell M3vqUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUTSSoxHUW6qaXLpeIlwdiCxZjDoeY1idiCVV{e4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkzNjN{IH7NMi=> Mon5V2FPT0WU
human SNU-387 cell M{XYOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnezTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvM{i3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVMvOzZibl2= MlLqV2FPT0WU
human LAMA-84 cell MljuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4rzN2lvcGmkaYTpc44hd2ZiaIXtZY4hVEGPQT24OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk1NjZ6IH7NMi=> MkLtV2FPT0WU
human MV-4-11 cell NXqxXYxIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmjTTY5pcWKrdHnvckBw\iCqdX3hckBOXi12LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVQvPzNibl2u M1XIVXNCVkeHUh?=
human EGI-1 cell M3;UWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4HyUWlvcGmkaYTpc44hd2ZiaIXtZY4hTUeLLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25OU45OSCwTT6= M1vjfXNCVkeHUh?=
human NCI-SNU-1 cell NIPtOXhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHyycndKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3TUnUuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTl4LkezJI5ONg>? MVHTRW5ITVJ?
human MEG-01 cell NGXtNWVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUPONmRFUW6qaXLpeIlwdiCxZjDoeY1idiCPRVetNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Py55NzDuUU4> NF;qOVhUSU6JRWK=
human OMC-1 cell M3[4PGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWnGe|dFUW6qaXLpeIlwdiCxZjDoeY1idiCRTVOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExOC5{MzDuUU4> Mkf6V2FPT0WU
human NB10 cell NETmUIFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1jsZWlvcGmkaYTpc44hd2ZiaIXtZY4hVkJzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwNE41OiCwTT6= NHTmVppUSU6JRWK=
human CAL-62 cell NXvsS3VKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1\s[GlvcGmkaYTpc44hd2ZiaIXtZY4hS0GOLU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAxNjd6IH7NMi=> MmnNV2FPT0WU
human NCI-H2087 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIH0cpRKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlA5PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFyMT6xOEBvVS5? MlqyV2FPT0WU
human MDA-MB-175-VII cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3flRmlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVE4PS2YSVmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfS=> NVPzbnl6W0GQR1XS
human LS-513 cell NF\PV4xIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUjyN49iUW6qaXLpeIlwdiCxZjDoeY1idiCOUz21NVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOTRwOEOgcm0v MV3TRW5ITVJ?
human HN cell growth MnLwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoPPTY5pcWKrdHnvckBw\iCqdX3hckBJViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{Mj61PUBvVS5? NFnvdGpUSU6JRWK=
human ABC-1 cell MlPyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXTJcohq[mm2aX;uJI9nKGi3bXHuJGFDSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKzMlAzKG6PLh?= M{WxZ3NCVkeHUh?=
human SJSA-1 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYjqeXJuUW6qaXLpeIlwdiCxZjDoeY1idiCVSmPBMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOjNwMUmgcm0v M2L6bnNCVkeHUh?=
human PANC1 cells NXG3flQ{TnWwY4Tpc44h[XO|YYm= NWXJOoo4OTBizszN MkHLNUBp MXHJcohq[mm2aX;uJI9nKE2HS{GgbY4hcHWvYX6gVGFPSzFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJJBGemtzL{KgcIV3\WxiYYSgNVAhfU1iYX\0[ZIhOSCqcjDifUBY\XO2ZYLuJIJtd3S2aX7nJIFv[Wy7c3nz MorNNlU4PjZ4M{O=
human MCF7 cells MmnmSpVv[3Srb36gZZN{[Xl? MVu3OUBucW6| MXrJcohq[mm2aX;uJI9nKE2Ha{GvNkBqdiCqdX3hckBOS0Z5IHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJGVTUyCyaH;zdIhwenmuYYTpc44h[W[2ZYKgO|UhdWmwczDifUBY\XO2ZYLuJIJtd3S2aX7nJIFv[Wy7c3nz MX2yN|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]
- 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)
Water Insoluble
Ethanol '40 mg/mL
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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    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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    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 is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.

  • Trametinib (GSK1120212)

    Trametinib (GSK1120212) 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)

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  • U0126-EtOH

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID