PD0325901(Mirdametinib)

Licensed by Pfizer Catalog No.S1036

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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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 M1fYPWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIrUNoFKdmirYnn0bY9vKG:oIHj1cYFvKEOKUD2yNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjV{NzDuUU4> NIP0eo9USU6JRWK=
human M14 cell M4nmWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVv1dXpVUW6qaXLpeIlwdiCxZjDoeY1idiCPMUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlQ2KG6PLh?= NX3tbol7W0GQR1XS
human SK-MEL-28 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlTvTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytNlgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjV{IH7NMi=> NHPwO4FUSU6JRWK=
human NOMO-1 cell NFvNOpFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmLRTY5pcWKrdHnvckBw\iCqdX3hckBPV02RLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlA4KG6PLh?= MmKwV2FPT0WU
human A375 cell M3vMcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXz5[41PUW6qaXLpeIlwdiCxZjDoeY1idiCDM{e1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk43QSCwTT6= M{HNbnNCVkeHUh?=
human DU-4475 cell NIOzNnBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUXJcohq[mm2aX;uJI9nKGi3bXHuJGRWNTR2N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlU4KG6PLh?= NYLhXlhIW0GQR1XS
human C32 cell M{\1[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGM{OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNwNkegcm0v MWXTRW5ITVJ?
human BPH-1 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2DJb2lvcGmkaYTpc44hd2ZiaIXtZY4hSlCKLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk2KG6PLh?= MWfTRW5ITVJ?
human CP50-MEL-B cell NHLZeVNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVzJcohq[mm2aX;uJI9nKGi3bXHuJGNRPTBvTVXMMWIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjV6IH7NMi=> M3TsSnNCVkeHUh?=
human H9 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFvINJVKdmirYnn0bY9vKG:oIHj1cYFvKEh7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT63O{BvVS5? M{e5U3NCVkeHUh?=
human HTC-C3 cell MljyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXPJcohq[mm2aX;uJI9nKGi3bXHuJGhVSy2FMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuPFkhdk1w NGPnd4JUSU6JRWK=
human BHT-101 cell MkK3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmTGTY5pcWKrdHnvckBw\iCqdX3hckBDUFRvMUCxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok44KG6PLh?= NIGzd3BUSU6JRWK=
human COLO-741 cell NXr2NpVRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWDJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vN{SxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O{4yKG6PLh?= MXTTRW5ITVJ?
human OVCAR-5 cell M4TkNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF3QSVJKdmirYnn0bY9vKG:oIHj1cYFvKE:YQ1HSMVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04Njh{IH7NMi=> NGfie5VUSU6JRWK=
human A549 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4DpfmlvcGmkaYTpc44hd2ZiaIXtZY4hSTV2OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUeuPFkhdk1w M17FcnNCVkeHUh?=
human SH-4 cell growth MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoLvTY5pcWKrdHnvckBw\iCqdX3hckBUUC12IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OD6yOkBvVS5? NWXqT3NzW0GQR1XS
human SK-N-AS cell NXjvNIY{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHjkV2pKdmirYnn0bY9vKG:oIHj1cYFvKFONLV6tRXMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05NjR2IH7NMi=> M4G5OHNCVkeHUh?=
human HT-144 cell NYXFbnJkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnK4TY5pcWKrdHnvckBw\iCqdX3hckBJXC1zNESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24Mlk4KG6PLh?= MYXTRW5ITVJ?
human MEL-HO cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml2zTY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlQ6KG6PLh?= M4jvWHNCVkeHUh?=
human COLO-679 cell NUDseI42T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1f0R2lvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz22O|kh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC5yMTDuUS=> M4TaUHNCVkeHUh?=
human HuP-T4 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYn3SnhoUW6qaXLpeIlwdiCxZjDoeY1idiCKdWCtWFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC57ODDuUU4> NV7oXYhsW0GQR1XS
human H-EMC-SS cell NH2ySVJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGLEbJVKdmirYnn0bY9vKG:oIHj1cYFvKEhvRV3DMXNUKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTFwMEKgcm0v NF;VbFFUSU6JRWK=
human LB2518-MEL cell NGDSXGlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYPJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjVzOD3NSWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS5zMzDuUU4> NYTBS4ZYW0GQR1XS
human HL-60 cell NIjsS3BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUTJcohq[mm2aX;uJI9nKGi3bXHuJGhNNTZyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUGuNVUhdk1w M1KyWXNCVkeHUh?=
human NCI-H1666 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{P2fGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlY3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTFwMUegcm0v MUTTRW5ITVJ?
human A101D cell NWrHNWZnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkHOTY5pcWKrdHnvckBw\iCqdX3hckBCOTBzRDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGxMlQ2KG6PLh?= M3m1bXNCVkeHUh?=
human RVH-421 cell NI\KS2JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV;Jcohq[mm2aX;uJI9nKGi3bXHuJHJXUC12MkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk43PCCwTT6= NYThT|BTW0GQR1XS
human Hs-578-T cell NGPiNndIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoHJTY5pcWKrdHnvckBw\iCqdX3hckBJey13N{itWEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjd7IH7NMi=> Ml6xV2FPT0WU
human A375 cells Mnv1VJJwdGmoZYLheIlwdiCjc4PhfS=> MXm3NkBp M3zqbWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OUBk\WyuczDlfJBz\XO|aX7nJGJTSUZiVk[wNGUhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3ME2xN{BvVS5? MlPFNlM1PzR|OEi=
human DOK cell MmDlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGRQUyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF|LkSgcm0v NUTDW5pPW0GQR1XS
human Mewo cell M4m4[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnOwTY5pcWKrdHnvckBw\iCqdX3hckBO\XexIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUSuOFUhdk1w NFrQO4NUSU6JRWK=
human ONS-76 cell NWLJU2FzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWj5cGRIUW6qaXLpeIlwdiCxZjDoeY1idiCRTmOtO|Yh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC53MTDuUU4> NXPxSJZHW0GQR1XS
human UACC-257 cell M3rXbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWDlfph4UW6qaXLpeIlwdiCxZjDoeY1idiCXQVPDMVI2PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF2Lk[yJI5ONg>? NIDMSJNUSU6JRWK=
human SW626 cell Mnj0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4npRWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4Mk[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE46OSCwTT6= M{TDO3NCVkeHUh?=
human SW620 cell NVXi[lJ{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXPJcohq[mm2aX;uJI9nKGi3bXHuJHNYPjJyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUSuPVUhdk1w M{nIVHNCVkeHUh?=
human TYK-nu cell M{fIUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NI\tb4ZKdmirYnn0bY9vKG:oIHj1cYFvKFS\Sz3ueUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjF|IH7NMi=> MYTTRW5ITVJ?
human ACN cell NF:wNJJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHnxXI1KdmirYnn0bY9vKG:oIHj1cYFvKEGFTjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG1Mlc3KG6PLh?= M4\DPHNCVkeHUh?=
human MIAPaCa2 cells M2HMNHBzd2yrZnXyZZRqd25iYYPzZZk> NYDifWk4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNTWFR[UOjMjDj[YxteyxiSVO1NF0yPyCwTT6= Ml6wNlM1PzR|OEi=
human T-24 cell NX7LeIN7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{TWfWlvcGmkaYTpc44hd2ZiaIXtZY4hXC1{NDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5MlcyKG6PLh?= NHjYd2ZUSU6JRWK=
human AGS cell NES4fGJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGTYd2xKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKwMlQyKG6PLh?= MXvTRW5ITVJ?
human SW872 cell MoLnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXLJcohq[mm2aX;uJI9nKGi3bXHuJHNYQDd{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkeuPVkhdk1w NGfvcVZUSU6JRWK=
human C2BBe1 cell MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX3hb2w3UW6qaXLpeIlwdiCxZjDoeY1idiCFMlLC[VEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQC53NDDuUU4> Mn3FV2FPT0WU
human MZ7-mel cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX7Jcohq[mm2aX;uJI9nKGi3bXHuJG1bPy2vZXygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yPU41OyCwTT6= NH3m[HRUSU6JRWK=
human HCC2998 cell MmCzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWOzUWNTUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyPVk5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzNwNk[gcm0v M3L3[3NCVkeHUh?=
human HO-1-N-1 cell NVLNe2pST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NXnve4hEUW6qaXLpeIlwdiCxZjDoeY1idiCKTz2xMW4uOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN2LkSzJI5ONg>? NX7KXFlzW0GQR1XS
human SW756 cell NG\HdHVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1W4cGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d5NU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOE41PSCwTT6= MVTTRW5ITVJ?
human NCI-H1437 cell NULSb2VNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGPwfIZKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVQ{PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN2LkS5JI5ONg>? MkLHV2FPT0WU
human NCI-H747 cell NXnsUpBKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXTJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KN{S3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|QvQThibl2u M1HpWXNCVkeHUh?=
human SK-MEL-2 cell MoPjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGPGS4VKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzVwMjDuUU4> M2[0XXNCVkeHUh?=
human MZ2-MEL cell M2ruNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGfwWJJKdmirYnn0bY9vKG:oIHj1cYFvKE2cMj3NSWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{PS54NTDuUU4> MoTQV2FPT0WU
human PSN1 cell NYfOeGtPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFyweGdKdmirYnn0bY9vKG:oIHj1cYFvKFCVTkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPE41PSCwTR?= MmD3V2FPT0WU
human CAL-39 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYXkclZFUW6qaXLpeIlwdiCxZjDoeY1idiCFQVytN|kh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{QS5yNDDuUU4> NVXGWYZQW0GQR1XS
human LOXIMVI cell NVrwU4ZXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml;LTY5pcWKrdHnvckBw\iCqdX3hckBNV1iLTW\JJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|kvOzlibl2u NXnkRYpCW0GQR1XS
human COLO-792 cell NInycWFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGjOemJKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tO|kzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PDNwMUWgcm0v NFj3UYVUSU6JRWK=
human CAL-27 cell NInFfZBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWrvdWh7UW6qaXLpeIlwdiCxZjDoeY1idiCFQVytNlch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01PC57MTDuUS=> MVjTRW5ITVJ?
human AsPC-1 cell M1LpXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIfWfVFKdmirYnn0bY9vKG:oIHj1cYFvKEG|UFOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ2NjJ6IH7NMi=> MmfpV2FPT0WU
human NCI-H2291 cell NVzk[WNET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVvifFRWUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIzQTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12Nj60OkBvVS5? MYTTRW5ITVJ?
human RCM-1 cell NYmyZWtkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NULSS4o1UW6qaXLpeIlwdiCxZjDoeY1idiCUQ12tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ3Njh3IH7NMi=> NUPZVWZVW0GQR1XS
human NCI-H292 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUDJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkmyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFcvOzlibl2u NYLTcGVoW0GQR1XS
human WM-115 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2q0fmlvcGmkaYTpc44hd2ZiaIXtZY4hX01vMUG1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFgvPSCwTT6= MlnDV2FPT0WU
human RT-112 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUT1VZVQUW6qaXLpeIlwdiCxZjDoeY1idiCUVD2xNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01QC56NDDuUU4> NXjiPFRQW0GQR1XS
human HT-29 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2frVWlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21NE41QSCwTT6= NYfMXZM2W0GQR1XS
human RKO cell growth MoniS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHKyOXRKdmirYnn0bY9vKG:oIHj1cYFvKFKNTzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWyMlAzKG6PLh?= M{jPOHNCVkeHUh?=
human KY821 cell NYDsdnhbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkDKTY5pcWKrdHnvckBw\iCqdX3hckBMYTh{MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWzMlMhdk1w M2q2bXNCVkeHUh?=
human LB1047-RCC cell NGrIcYJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYLJcohq[mm2aX;uJI9nKGi3bXHuJGxDOTB2Nz3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02QS54NTDuUU4> Ml;OV2FPT0WU
human SW1116 cell M{i2OWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYPzZodKUW6qaXLpeIlwdiCxZjDoeY1idiCVV{GxNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03OC52OTDuUU4> M1nEZ3NCVkeHUh?=
human P12-ICHIKAWA cell M1\Efmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXXTU3VOUW6qaXLpeIlwdiCxZjDoeY1idiCSMUKtTWNJUUuDV1GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22Nk4zPyCwTT6= NXewR4pPW0GQR1XS
human HCC70 cell M1XrZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NET1T|dKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{ewJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OlMvODFibl2u MYXTRW5ITVJ?
human MIA-PaCa-2 cell NI\BbIRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVPJcohq[mm2aX;uJI9nKGi3bXHuJG1KSS2SYVPhMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03Oy53MzDuUU4> NH3MSo1USU6JRWK=
human LoVo cell NIXEbXBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MULJcohq[mm2aX;uJI9nKGi3bXHuJGxwXm9iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14NT6yPUBvVS5? NIP5ZZFUSU6JRWK=
human LB2241-RCC cell NXu0U3lTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXzJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjJ2MT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03PS53MjDuUU4> M4CxWHNCVkeHUh?=
human GAK cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEfoZZFKdmirYnn0bY9vKG:oIHj1cYFvKEeDSzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[2Mlg4KG6PLh?= NInwNJBUSU6JRWK=
human RD cell MmnaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn;ITY5pcWKrdHnvckBw\iCqdX3hckBTTCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZ5LkGgcm0v MV\TRW5ITVJ?
human KNS-62 cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYHNWpRNUW6qaXLpeIlwdiCxZjDoeY1idiCNTmOtOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03QS57OTDuUU4> NFvJU|hUSU6JRWK=
human HD-MY-Z cell NU\jVmFQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVPJcohq[mm2aX;uJI9nKGi3bXHuJGhFNU2\LWqgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23NU4yOiCwTT6= Mn7SV2FPT0WU
human COR-L105 cell M1zGbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkfJTY5pcWKrdHnvckBw\iCqdX3hckBEV1JvTEGwOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcyNjdzIH7NMi=> NYqxVlh3W0GQR1XS
human IA-LM cell NEfOZ2NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXjBOGtWUW6qaXLpeIlwdiCxZjDoeY1idiCLQT3MUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVc{NjJ6IH7NMi=> MV3TRW5ITVJ?
human EM-2 cell M{Cyemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYfJcohq[mm2aX;uJI9nKGi3bXHuJGVONTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD15ND63JI5ONg>? M1zGVHNCVkeHUh?=
human NB69 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYTZSnZkUW6qaXLpeIlwdiCxZjDoeY1idiCQQk[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZk> NHzSb5JUSU6JRWK=
human HuP-T3 cell NIKyNphIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4DVR2lvcGmkaYTpc44hd2ZiaIXtZY4hUHWSLWSzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFMvQTNibl2u NIXPNWxUSU6JRWK=
human BB30-HNC cell MUDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M17acmlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ|MD3IUmMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05PS53MTDuUU4> NW\KPGxZW0GQR1XS
human HT-1080 cell NGKyTYVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYn5UGFiUW6qaXLpeIlwdiCxZjDoeY1idiCKVD2xNFgxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QDVwOEigcm0v M4TnZnNCVkeHUh?=
human RMG-I cell NIn1bVFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWe5[mhUUW6qaXLpeIlwdiCxZjDoeY1idiCUTVetTUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVg4NjN2IH7NMi=> MYHTRW5ITVJ?
human HCC1419 cell NF71e|BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVLIUopWUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OxOFE6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QTFwM{igcm0v M2O1T3NCVkeHUh?=
human SW780 cell M4eyVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWnNXZJCUW6qaXLpeIlwdiCxZjDoeY1idiCVV{e4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkzNjN{IH7NMi=> NVTzcIdlW0GQR1XS
human SNU-387 cell MlHZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkDITY5pcWKrdHnvckBw\iCqdX3hckBUVlVvM{i3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVMvOzZibl2= MlHEV2FPT0WU
human LAMA-84 cell NID1SG9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFjYTXJKdmirYnn0bY9vKG:oIHj1cYFvKEyDTVGtPFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06PC54ODDuUU4> NUnRfHFZW0GQR1XS
human MV-4-11 cell M2j4Tmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV[3WFN6UW6qaXLpeIlwdiCxZjDoeY1idiCPVj20MVEyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QTRwN{Ogcm0v M2HDbHNCVkeHUh?=
human EGI-1 cell M4O4UGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUfJcohq[mm2aX;uJI9nKGi3bXHuJGVIUS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OUWuPFEhdk1w MkKwV2FPT0WU
human NCI-SNU-1 cell NWLIWYxQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MomzTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvU17VMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Pi55MzDuUU4> MnnQV2FPT0WU
human MEG-01 cell NIDkSIxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1HEN2lvcGmkaYTpc44hd2ZiaIXtZY4hVUWJLUCxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVcvPzdibl2u MX7TRW5ITVJ?
human OMC-1 cell NWfZd5E2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mlq3TY5pcWKrdHnvckBw\iCqdX3hckBQVUNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwNE4zOyCwTT6= MVnTRW5ITVJ?
human NB10 cell NWOycFVZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXrJcohq[mm2aX;uJI9nKGi3bXHuJG5DOTBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMECuOFIhdk1w M4\KO3NCVkeHUh?=
human CAL-62 cell MoO0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoX3TY5pcWKrdHnvckBw\iCqdX3hckBESUxvNkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNFAvPzhibl2u NV\USVB1W0GQR1XS
human NCI-H2087 cell NITvfINIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIjIV3lKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlA5PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFyMT6xOEBvVS5? NEDCd3pUSU6JRWK=
human MDA-MB-175-VII cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVnJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2xO|UuXkmLIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYm= MVTTRW5ITVJ?
human LS-513 cell M2rNZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHPYS|VKdmirYnn0bY9vKG:oIHj1cYFvKEyVLUWxN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyPC56MzDuUU4> MYDTRW5ITVJ?
human HN cell growth MmLOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4L6SmlvcGmkaYTpc44hd2ZiaIXtZY4hUE5iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMkKuOVkhdk1w NIjCR|JUSU6JRWK=
human ABC-1 cell M1vo[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmDPTY5pcWKrdHnvckBw\iCqdX3hckBCSkNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGyN{4xOiCwTT6= NF[1dZpUSU6JRWK=
human SJSA-1 cell NEj1fFJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1rkWGlvcGmkaYTpc44hd2ZiaIXtZY4hW0qVQT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVI{NjF7IH7NMi=> M2TjNXNCVkeHUh?=
human PANC1 cells M3nsRmZ2dmO2aX;uJIF{e2G7 NXjwUJR6OTBizszN MXixJIg> MlS5TY5pcWKrdHnvckBw\iCPRVuxJIlvKGi3bXHuJHBCVkNzIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBxTXKtMT:yJIxmfmWuIHH0JFExKHWPIHHmeIVzKDFiaIKgZpkhX2W|dHXyckBjdG:2dHnu[{BidmGueYPpdy=> MmfCNlU4PjZ4M{O=
human MCF7 cells NGjqfmpHfW6ldHnvckBie3OjeR?= MkfZO|UhdWmwcx?= MlT1TY5pcWKrdHnvckBw\iCPRXuxM|IhcW5iaIXtZY4hVUOINzDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBGWkticHjvd5Bpd3K7bHH0bY9vKGGodHXyJFc2KG2rboOgZpkhX2W|dHXyckBjdG:2dHnu[{BidmGueYPpdy=> MoHWNlM{QTh2NUO=

... 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
  • Formulation: 80 mM citric buffer (pH 7)
  • 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

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    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

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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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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

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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/

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MEK Signaling Pathway Map

MEK Inhibitors with Unique Features

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  • BI-847325 New

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  • Trametinib (GSK1120212)

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    Features:More potent than PD0325901 or AZD6244.

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  • PD98059

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID