Mirdametinib (PD0325901)

For research use only.

Licensed by Pfizer Catalog No.S1036

525 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 525 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 M4PPdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWLRZ|dKUW6qaXLpeIlwdiCxZjDoeY1idiCFSGCtNlEzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC53Mkegcm0v Mm\oV2FPT0WU
human M14 cell M2rOSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MorBTY5pcWKrdHnvckBw\iCqdX3hckBOOTRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkS1JI5ONg>? NXXhW3ZWW0GQR1XS
human SK-MEL-28 cell M1z4R2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mlr1TY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytNlgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjV{IH7NMi=> MXrTRW5ITVJ?
human NOMO-1 cell M4\lb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4PnWWlvcGmkaYTpc44hd2ZiaIXtZY4hVk:PTz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4xPyCwTT6= MmnhV2FPT0WU
human A375 cell NUPwNGRCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVHJcohq[mm2aX;uJI9nKGi3bXHuJGE{PzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{Lk[5JI5ONg>? M2DPe3NCVkeHUh?=
human DU-4475 cell NI\6RXpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWjJcohq[mm2aX;uJI9nKGi3bXHuJGRWNTR2N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlU4KG6PLh?= MWPTRW5ITVJ?
human C32 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NX3ZNoE1UW6qaXLpeIlwdiCxZjDoeY1idiCFM{KgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlY4KG6PLh?= NH3wb|hUSU6JRWK=
human BPH-1 cell M3XDeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NU\mSGRoUW6qaXLpeIlwdiCxZjDoeY1idiCEUFitNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvQTVibl2u M4j5N3NCVkeHUh?=
human CP50-MEL-B cell M3vkWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{fp[mlvcGmkaYTpc44hd2ZiaIXtZY4hS1B3MD3NSWwuSiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwNUigcm0v M4HGenNCVkeHUh?=
human H9 cell NWH3dXhDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIn4SIJKdmirYnn0bY9vKG:oIHj1cYFvKEh7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NT63O{BvVS5? NXLnUo1xW0GQR1XS
human HTC-C3 cell NF\lO2FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHnpeXlKdmirYnn0bY9vKG:oIHj1cYFvKEiWQz3DN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvQDlibl2u NXfOTHNGW0GQR1XS
human BHT-101 cell M2jme2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUPJcohq[mm2aX;uJI9nKGi3bXHuJGJJXC1zMEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22Mlchdk1w MkjyV2FPT0WU
human COLO-741 cell MlnzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MofuTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLUe0NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvOSCwTT6= NXniRVBLW0GQR1XS
human OVCAR-5 cell M{jmUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3\6cWlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvQDJibl2u NW\NT|NGW0GQR1XS
human A549 cell M1zMVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{D1emlvcGmkaYTpc44hd2ZiaIXtZY4hSTV2OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUeuPFkhdk1w NWPS[GlFW0GQR1XS
human SH-4 cell growth NWjqc3pTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2jlPGlvcGmkaYTpc44hd2ZiaIXtZY4hW0hvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUiuNlYhdk1w M2L3TXNCVkeHUh?=
human SK-N-AS cell NHfRSmRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1vWV2lvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTj3BV{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVgvPDRibl2u NGXkSGZUSU6JRWK=
human HT-144 cell NGPRU25Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmqyTY5pcWKrdHnvckBw\iCqdX3hckBJXC1zNESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24Mlk4KG6PLh?= MonGV2FPT0WU
human MEL-HO cell MmroS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXLJcohq[mm2aX;uJI9nKGi3bXHuJG1GVC2KTzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmuOFkhdk1w NVfTWoJKW0GQR1XS
human COLO-679 cell NXL3dHpOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml;0TY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLU[3PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExNjBzIH7N MYrTRW5ITVJ?
human HuP-T4 cell NGLVPZRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHjDb3dKdmirYnn0bY9vKG:oIHj1cYFvKEi3UD3UOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExNjl6IH7NMi=> NWrPOFV{W0GQR1XS
human H-EMC-SS cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVHLfnpTUW6qaXLpeIlwdiCxZjDoeY1idiCKLVXNR{1UWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFzLkCyJI5ONg>? NHfpelhUSU6JRWK=
human LB2518-MEL cell NX3I[|hrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnTITY5pcWKrdHnvckBw\iCqdX3hckBNSjJ3MUitUWVNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTFwMUOgcm0v MYrTRW5ITVJ?
human HL-60 cell MkTjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHiyWZRKdmirYnn0bY9vKG:oIHj1cYFvKEiOLU[wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVEvOTVibl2u MkK4V2FPT0WU
human NCI-H1666 cell NIHzRmlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMU[2OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjF5IH7NMi=> NIj0VGtUSU6JRWK=
human A101D cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoT3TY5pcWKrdHnvckBw\iCqdX3hckBCOTBzRDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGxMlQ2KG6PLh?= MUnTRW5ITVJ?
human RVH-421 cell M1XZSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX;Jcohq[mm2aX;uJI9nKGi3bXHuJHJXUC12MkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNk43PCCwTT6= Ml;EV2FPT0WU
human Hs-578-T cell NW\OSFNkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX7lZVlsUW6qaXLpeIlwdiCxZjDoeY1idiCKcz21O|guXCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{Lke5JI5ONg>? MkDVV2FPT0WU
human A375 cells M4TVTnBzd2yrZnXyZZRqd25iYYPzZZk> MlP1O|IhcA>? MVvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF|N{WgZ4VtdHNiZYjwdoV{e2mwZzDCVmFHKFZ4MEDFJI12fGGwdDDh[pRmeiB5MjDodpMh[nliQ3XscEB1cXSncj3ncI8h[XO|YYmsJGlEPTB;MUOgcm0v MkLRNlM1PzR|OEi=
human DOK cell MnriS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFv3R3hKdmirYnn0bY9vKG:oIHj1cYFvKESRSzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlQhdk1w MUDTRW5ITVJ?
human Mewo cell NEjTNVNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmCyTY5pcWKrdHnvckBw\iCqdX3hckBO\XexIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUSuOFUhdk1w M1rQbXNCVkeHUh?=
human ONS-76 cell NHHZcopIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3Tz[mlvcGmkaYTpc44hd2ZiaIXtZY4hV06VLUe2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPTFibl2u Mo\RV2FPT0WU
human UACC-257 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV;Jcohq[mm2aX;uJI9nKGi3bXHuJHVCS0NvMkW3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPjJibl2u M2mxTnNCVkeHUh?=
human SW626 cell NVPqPVExT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1vYN2lvcGmkaYTpc44hd2ZiaIXtZY4hW1d4Mk[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE46OSCwTT6= M2S4e3NCVkeHUh?=
human SW620 cell NXzGZms{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGXQO|VKdmirYnn0bY9vKG:oIHj1cYFvKFOZNkKwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvQTVibl2u NVztfGxJW0GQR1XS
human TYK-nu cell NUHWTGczT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MY\Jcohq[mm2aX;uJI9nKGi3bXHuJHR[Uy2wdTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG1MlE{KG6PLh?= M1\GS3NCVkeHUh?=
human ACN cell M2\RZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWfJcohq[mm2aX;uJI9nKGi3bXHuJGFEViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF3Lke2JI5ONg>? MYfTRW5ITVJ?
human MIAPaCa2 cells NXLTR|ZPWHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml6xRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPSVHQZWNiOiClZXzsd{whUUN3ME2xO{BvVS5? MlK5NlM1PzR|OEi=
human T-24 cell NVnrdHNIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHK0T5lKdmirYnn0bY9vKG:oIHj1cYFvKFRvMkSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPU44OSCwTT6= Mly5V2FPT0WU
human AGS cell NVTpPY1PT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWjJcohq[mm2aX;uJI9nKGi3bXHuJGFIWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJyLkSxJI5ONg>? MkC1V2FPT0WU
human SW872 cell M1TkR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWDJcohq[mm2aX;uJI9nKGi3bXHuJHNYQDd{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkeuPVkhdk1w MmT0V2FPT0WU
human C2BBe1 cell NHTNWmNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NInYOmNKdmirYnn0bY9vKG:oIHj1cYFvKEN{QlLlNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI5NjV2IH7NMi=> M1KzfXNCVkeHUh?=
human MZ7-mel cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVzJcohq[mm2aX;uJI9nKGi3bXHuJG1bPy2vZXygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yPU41OyCwTT6= NWT3R41OW0GQR1XS
human HCC2998 cell MlP1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmT2TY5pcWKrdHnvckBw\iCqdX3hckBJS0N{OUm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|MvPjZibl2u NWjaPWxUW0GQR1XS
human HO-1-N-1 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFnnW3hKdmirYnn0bY9vKG:oIHj1cYFvKEiRLUGtUk0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzRwNEOgcm0v NFvRO2NUSU6JRWK=
human SW756 cell NEXQNYhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV\1S4lHUW6qaXLpeIlwdiCxZjDoeY1idiCVV{e1OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM1NjR3IH7NMi=> M{PDV3NCVkeHUh?=
human NCI-H1437 cell M4nkV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFvLdWNKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVQ{PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN2LkS5JI5ONg>? MXLTRW5ITVJ?
human NCI-H747 cell NIHaTmRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NETWbHBKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IO|Q4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzRwOUigcm0v NHL3dW9USU6JRWK=
human SK-MEL-2 cell NH;KdohIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlTKTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM2NjJibl2u MojLV2FPT0WU
human MZ2-MEL cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV3Jcohq[mm2aX;uJI9nKGi3bXHuJG1bOi2PRVygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOU43PSCwTT6= MUTTRW5ITVJ?
human PSN1 cell NFnURVZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVrJcohq[mm2aX;uJI9nKGi3bXHuJHBUVjFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|OD60OUBvVQ>? Mk\nV2FPT0WU
human CAL-39 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYjMXpdtUW6qaXLpeIlwdiCxZjDoeY1idiCFQVytN|kh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{QS5yNDDuUU4> MXXTRW5ITVJ?
human LOXIMVI cell NEHMZ2ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3X6[GlvcGmkaYTpc44hd2ZiaIXtZY4hVE:[SV3WTUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM6NjN7IH7NMi=> NVjZT2tEW0GQR1XS
human COLO-792 cell MmjyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3;rSmlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz23PVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Oy5zNTDuUU4> NIPnTpZUSU6JRWK=
human CAL-27 cell NEj3TVdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NUPDTVB[UW6qaXLpeIlwdiCxZjDoeY1idiCFQVytNlch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01PC57MTDuUS=> NEHscGpUSU6JRWK=
human AsPC-1 cell MnvhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{HV[mlvcGmkaYTpc44hd2ZiaIXtZY4hSXOSQz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFUvOjhibl2u NUW2XHhtW0GQR1XS
human NCI-H2291 cell NFK0b25Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn7JTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKyPVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Pi52NjDuUU4> MmD6V2FPT0WU
human RCM-1 cell NEDRe2pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1G4eGlvcGmkaYTpc44hd2ZiaIXtZY4hWkOPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20Ok45PSCwTT6= MVfTRW5ITVJ?
human NCI-H292 cell MoPsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MknCTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEK5NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ4NjN7IH7NMi=> NEPNXm5USU6JRWK=
human WM-115 cell NFfrRpdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlLtTY5pcWKrdHnvckBw\iCqdX3hckBYVS1zMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20PE42KG6PLh?= MYrTRW5ITVJ?
human RT-112 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWPjU5UzUW6qaXLpeIlwdiCxZjDoeY1idiCUVD2xNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01QC56NDDuUU4> M{LHdnNCVkeHUh?=
human HT-29 cell NHzhdW9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmXFTY5pcWKrdHnvckBw\iCqdX3hckBJXC1{OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWwMlQ6KG6PLh?= NVPMe|Y1W0GQR1XS
human RKO cell growth MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVvRSHRuUW6qaXLpeIlwdiCxZjDoeY1idiCUS1:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Nk4xOiCwTT6= NXXV[JpHW0GQR1XS
human KY821 cell NWfBVXI2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHPSbGRKdmirYnn0bY9vKG:oIHj1cYFvKEu\OEKxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVMvOyCwTT6= NUmwdYpjW0GQR1XS
human LB1047-RCC cell NWq1bW5uT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M33MXWlvcGmkaYTpc44hd2ZiaIXtZY4hVEJzMES3MXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTV7Lk[1JI5ONg>? MmqyV2FPT0WU
human SW1116 cell NIDuW5pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXfFb|BwUW6qaXLpeIlwdiCxZjDoeY1idiCVV{GxNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03OC52OTDuUU4> MkTQV2FPT0WU
human P12-ICHIKAWA cell MYjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml\ETY5pcWKrdHnvckBw\iCqdX3hckBROTJvSVPITWtCX0FiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14Mj6yO{BvVS5? MVzTRW5ITVJ?
human HCC70 cell NHzjWmpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1S1UmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFN{CgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22N{4xOSCwTT6= M4\oZ3NCVkeHUh?=
human MIA-PaCa-2 cell NVnYd3dJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWrzWJYxUW6qaXLpeIlwdiCxZjDoeY1idiCPSVGtVIFE[S1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NkOuOVMhdk1w MkLUV2FPT0WU
human LoVo cell M4S0Smdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3\NeGlvcGmkaYTpc44hd2ZiaIXtZY4hVG:YbzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[1MlI6KG6PLh?= M3TzdXNCVkeHUh?=
human LB2241-RCC cell M{PX[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkDSTY5pcWKrdHnvckBw\iCqdX3hckBNSjJ{NEGtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PjVwNUKgcm0v MnP3V2FPT0WU
human GAK cell NFHsSYhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX3nS2FYUW6qaXLpeIlwdiCxZjDoeY1idiCJQVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22Ok45PyCwTT6= NGO0VpRUSU6JRWK=
human RD cell NHvSPJVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVnJcohq[mm2aX;uJI9nKGi3bXHuJHJFKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PjdwMTDuUU4> Mn;xV2FPT0WU
human KNS-62 cell NWSzZoVDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV\leYtzUW6qaXLpeIlwdiCxZjDoeY1idiCNTmOtOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03QS57OTDuUU4> MlPPV2FPT0WU
human HD-MY-Z cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUTJcohq[mm2aX;uJI9nKGi3bXHuJGhFNU2\LWqgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23NU4yOiCwTT6= NWK5XXRSW0GQR1XS
human COR-L105 cell NXjmfFk2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGNQWi2OMUC1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O|EvPzFibl2u NWLV[WZPW0GQR1XS
human IA-LM cell NFGxVHBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1;KOWlvcGmkaYTpc44hd2ZiaIXtZY4hUUFvTF2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23N{4zQCCwTT6= NFXH[pNUSU6JRWK=
human EM-2 cell M2\Vfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MorTTY5pcWKrdHnvckBw\iCqdX3hckBGVS1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;N{SuO{BvVS5? MoH6V2FPT0WU
human NB69 cell MkmwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWrJcohq[mm2aX;uJI9nKGi3bXHuJG5DPjliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeR?= NEPWOZlUSU6JRWK=
human HuP-T3 cell M1Lt[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYewUIhCUW6qaXLpeIlwdiCxZjDoeY1idiCKdWCtWFMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05Oy57MzDuUU4> NHX3SI9USU6JRWK=
human BB30-HNC cell M{TmNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUjJcohq[mm2aX;uJI9nKGi3bXHuJGJDOzBvSF7DJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFUvPTFibl2u MYPTRW5ITVJ?
human HT-1080 cell M2iwUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGGyNIhKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUGwPFAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05PS56ODDuUU4> NIjMNoFUSU6JRWK=
human RMG-I cell M4f0XWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2DqcmlvcGmkaYTpc44hd2ZiaIXtZY4hWk2JLVmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24O{4{PCCwTT6= M3XSWnNCVkeHUh?=
human HCC1419 cell NFj0fGdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFnLVpFKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{G0NVkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06OS5|ODDuUU4> MXrTRW5ITVJ?
human SW780 cell NGXxblJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2TReGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25Nk4{OiCwTT6= MWHTRW5ITVJ?
human SNU-387 cell NYPpc|JpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmXOTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvM{i3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVMvOzZibl2= MWjTRW5ITVJ?
human LAMA-84 cell MmHBS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFztb4tKdmirYnn0bY9vKG:oIHj1cYFvKEyDTVGtPFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06PC54ODDuUU4> NFOyUW1USU6JRWK=
human MV-4-11 cell M4fBdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmnkTY5pcWKrdHnvckBw\iCqdX3hckBOXi12LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVQvPzNibl2u M{nQbnNCVkeHUh?=
human EGI-1 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIi0enFKdmirYnn0bY9vKG:oIHj1cYFvKEWJST2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVUvQDFibl2u NX;ybllRW0GQR1XS
human NCI-SNU-1 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXzodVJtUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtV25WNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17Nj63N{BvVS5? MUjTRW5ITVJ?
human MEG-01 cell NHuwTINIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NETQemNKdmirYnn0bY9vKG:oIHj1cYFvKE2HRz2wNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk4Njd5IH7NMi=> NX\Hb|g4W0GQR1XS
human OMC-1 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVTJcohq[mm2aX;uJI9nKGi3bXHuJG9OSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUCwMlI{KG6PLh?= MWDTRW5ITVJ?
human NB10 cell NUHtR|hZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4W2cmlvcGmkaYTpc44hd2ZiaIXtZY4hVkJzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwNE41OiCwTT6= MkDnV2FPT0WU
human CAL-62 cell Mk\TS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mm\CTY5pcWKrdHnvckBw\iCqdX3hckBESUxvNkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNFAvPzhibl2u MX3TRW5ITVJ?
human NCI-H2087 cell NWL4e41DT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX;sbFVrUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxQDdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMEGuNVQhdk1w NITYcZRUSU6JRWK=
human MDA-MB-175-VII cell NEG3V|NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M13yUGlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVE4PS2YSVmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfS=> NVy3cnN6W0GQR1XS
human LS-513 cell NGDFZ2lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkTrTY5pcWKrdHnvckBw\iCqdX3hckBNWy13MUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNVQvQDNibl2u NY\iOYd[W0GQR1XS
human HN cell growth MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkXsTY5pcWKrdHnvckBw\iCqdX3hckBJViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{Mj61PUBvVS5? Mm\uV2FPT0WU
human ABC-1 cell MlPlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVnJcohq[mm2aX;uJI9nKGi3bXHuJGFDSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUKzMlAzKG6PLh?= MlHYV2FPT0WU
human SJSA-1 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVTJcohq[mm2aX;uJI9nKGi3bXHuJHNLW0FvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGyN{4yQSCwTT6= NYKxVlNxW0GQR1XS
human PANC1 cells M1PmemZ2dmO2aX;uJIF{e2G7 NXPKR4lZOTBizszN MYCxJIg> Ml7ITY5pcWKrdHnvckBw\iCPRVuxJIlvKGi3bXHuJHBCVkNzIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBxTXKtMT:yJIxmfmWuIHH0JFExKHWPIHHmeIVzKDFiaIKgZpkhX2W|dHXyckBjdG:2dHnu[{BidmGueYPpdy=> MWOyOVc3PjZ|Mx?=
human MCF7 cells M4i4VmZ2dmO2aX;uJIF{e2G7 NV3RenFqPzVibXnudy=> MnnYTY5pcWKrdHnvckBw\iCPRXuxM|IhcW5iaIXtZY4hVUOINzDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBGWkticHjvd5Bpd3K7bHH0bY9vKGGodHXyJFc2KG2rboOgZpkhX2W|dHXyckBjdG:2dHnu[{BidmGueYPpdy=> Mk\6NlM{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]

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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)
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 C1=CC(=C(C=C1I)F)NC2=C(C=CC(=C2F)F)C(=O)NOCC(CO)O

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    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/

MEK Signaling Pathway Map

MEK Inhibitors with Unique Features

Related MEK Products

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID