PD0325901

Licensed by Pfizer Catalog No.S1036

PD0325901 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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Cited by 138 Publications

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Biological Activity

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

PD0325901 shows higher permeability than CI-1040, another MEK inhibitor. PD0325901 should be able to achieve higher systemic exposures than CI-1040. [1] PD0325901 is exquisitely specific and highly potent against purified MEK, revealing a Kiapp of 1 nM against activated MEK1 and MEK2. [2] PD0325901 is roughly 500-fold more potent than CI-1040 with respect to its cellular effects on phosphorylation of ERK1 and ERK2, displaying subnanomolar activity. [2] PD0325901 prevents the growth of melanoma cell lines. PD0325901 inhibits the growth of TPC-1 cells and K2 cells with GI50 of 11 nM and 6.3 nM, respectively. [3] PD0325901 significantly prevents the the growth of PTC cells harboring a BRAF mutation at very low concentration (10 nM) and only moderately increases the growth of the PTC cells carrying the RET/PTC1 rearrangement at the same concentration. PD0325901 effectively inhibits the phosphorylation of ERK1/2 in multiple PTC cell lines. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human CHP-212 cell M1;zfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGNJWC1{MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlUzPyCwTT6= MkjRV2FPT0WU
human M14 cell NVfxe3ByT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVvJcohq[mm2aX;uJI9nKGi3bXHuJG0yPCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEWgcm0v M3nHb3NCVkeHUh?=
human SK-MEL-28 cell MoLIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1\pXGlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVI5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS53MjDuUU4> MVTTRW5ITVJ?
human NOMO-1 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXXJcohq[mm2aX;uJI9nKGi3bXHuJG5QVU9vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKuNFchdk1w NWDORpBvW0GQR1XS
human A375 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXzJcohq[mm2aX;uJI9nKGi3bXHuJGE{PzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{Lk[5JI5ONg>? NYTodolEW0GQR1XS
human DU-4475 cell MkPMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIqz[ZNKdmirYnn0bY9vKG:oIHj1cYFvKESXLUS0O|Uh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjV5IH7NMi=> NUHmWXZXW0GQR1XS
human C32 cell NF7ac3RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2TMWGlvcGmkaYTpc44hd2ZiaIXtZY4hSzN{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mz62O{BvVS5? NVPpUHFqW0GQR1XS
human BPH-1 cell NIfoTpFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEH5XVdKdmirYnn0bY9vKG:oIHj1cYFvKEKSSD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PSCwTT6= Mnq0V2FPT0WU
human CP50-MEL-B cell NYnFT4hWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2rZemlvcGmkaYTpc44hd2ZiaIXtZY4hS1B3MD3NSWwuSiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwNUigcm0v Mo\OV2FPT0WU
human H9 cell NILOclZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mly2TY5pcWKrdHnvckBw\iCqdX3hckBJQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwN{egcm0v NFGxfnZUSU6JRWK=
human HTC-C3 cell NGr6fnVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkK2TY5pcWKrdHnvckBw\iCqdX3hckBJXENvQ{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlg6KG6PLh?= NWHz[odEW0GQR1XS
human BHT-101 cell NWXKTW9mT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJGJJXC1zMEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22Mlchdk1w NUC2PHlOW0GQR1XS
human COLO-741 cell M1XYT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEixZ3BKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tO|QyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Py5zIH7NMi=> MXvTRW5ITVJ?
human OVCAR-5 cell MlS2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIi4bXZKdmirYnn0bY9vKG:oIHj1cYFvKE:YQ1HSMVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04Njh{IH7NMi=> MnXhV2FPT0WU
human A549 cell NVnDcmJTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVrJcohq[mm2aX;uJI9nKGi3bXHuJGE2PDliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD15Lki5JI5ONg>? M1T2VHNCVkeHUh?=
human SH-4 cell growth NW\qS4hDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF;mUpJKdmirYnn0bY9vKG:oIHj1cYFvKFOKLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24MlI3KG6PLh?= M{WzRXNCVkeHUh?=
human SK-N-AS cell M1j2[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYnJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU5vQWOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24MlQ1KG6PLh?= NUDNPFZ3W0GQR1XS
human HT-144 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGhVNTF2NDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUiuPVchdk1w NFHQVINUSU6JRWK=
human MEL-HO cell M1TCfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYXNe5lWUW6qaXLpeIlwdiCxZjDoeY1idiCPRVytTG8h[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjR7IH7NMi=> Mn;jV2FPT0WU
human COLO-679 cell M4XQUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4jVT2lvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz22O|kh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOC5yMTDuUS=> M3PjTnNCVkeHUh?=
human HuP-T4 cell NF3RdndIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkjCTY5pcWKrdHnvckBw\iCqdX3hckBJfVBvVESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE46QCCwTT6= NVK2SY5PW0GQR1XS
human H-EMC-SS cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoXGTY5pcWKrdHnvckBw\iCqdX3hckBJNUWPQz3TV{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjB{IH7NMi=> MmqyV2FPT0WU
human LB2518-MEL cell Mn;4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEXsPG5KdmirYnn0bY9vKG:oIHj1cYFvKEyEMkWxPE1OTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMT6xN{BvVS5? MX;TRW5ITVJ?
human HL-60 cell M1;Sdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHvYeoFKdmirYnn0bY9vKG:oIHj1cYFvKEiOLU[wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVEvOTVibl2u MnjvV2FPT0WU
human NCI-H1666 cell NUTwVZB[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHTIeJVKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVY3PiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFzLkG3JI5ONg>? M3;BcHNCVkeHUh?=
human A101D cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUnTcZZCUW6qaXLpeIlwdiCxZjDoeY1idiCDMUCxSEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjR3IH7NMi=> M{TkbXNCVkeHUh?=
human RVH-421 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2TXSmlvcGmkaYTpc44hd2ZiaIXtZY4hWl[KLUSyNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjZ2IH7NMi=> MYLTRW5ITVJ?
human Hs-578-T cell NYjORpQ4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEDPd|dKdmirYnn0bY9vKG:oIHj1cYFvKEi|LUW3PE1VKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwN{mgcm0v MVPTRW5ITVJ?
human A375 cells M4f2UnBzd2yrZnXyZZRqd25iYYPzZZk> NVTqcYNIPzJiaB?= M363T2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OUBk\WyuczDlfJBz\XO|aX7nJGJTSUZiVk[wNGUhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3ME2xN{BvVS5? Ml\1NlM1PzR|OEi=
human DOK cell Moq4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGPoPVlKdmirYnn0bY9vKG:oIHj1cYFvKESRSzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlQhdk1w NFe0eWxUSU6JRWK=
human Mewo cell NFX3OotIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX;Jcohq[mm2aX;uJI9nKGi3bXHuJG1mf29iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zND60OUBvVS5? MmLvV2FPT0WU
human ONS-76 cell MlPsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2jaPWlvcGmkaYTpc44hd2ZiaIXtZY4hV06VLUe2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPTFibl2u MVfTRW5ITVJ?
human UACC-257 cell NUnlNVQxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3vTNWlvcGmkaYTpc44hd2ZiaIXtZY4hXUGFQz2yOVch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC54MjDuUU4> MUTTRW5ITVJ?
human SW626 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4\rcWlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4Mk[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE46OSCwTT6= NHf1bI5USU6JRWK=
human SW620 cell M1y3bmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUPJcohq[mm2aX;uJI9nKGi3bXHuJHNYPjJyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUSuPVUhdk1w NUDNNVFiW0GQR1XS
human TYK-nu cell Mle2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEXvfpZKdmirYnn0bY9vKG:oIHj1cYFvKFS\Sz3ueUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE2NjF|IH7NMi=> MY\TRW5ITVJ?
human ACN cell M37ZOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3rMbmlvcGmkaYTpc44hd2ZiaIXtZY4hSUOQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuO|Yhdk1w NUfWWVR5W0GQR1XS
human MIAPaCa2 cells NEHIUmNRem:uaX\ldoF1cW:wIHHzd4F6 NGjleXRCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3JRXBiS2F{IHPlcIx{NCCLQ{WwQVE4KG6PLh?= NH\Z[YIzOzR5NEO4PC=>
human T-24 cell NInOTIxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoP3TY5pcWKrdHnvckBw\iCqdX3hckBVNTJ2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUmuO|Ehdk1w M2DMUXNCVkeHUh?=
human AGS cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXLJcohq[mm2aX;uJI9nKGi3bXHuJGFIWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJyLkSxJI5ONg>? M3\ydHNCVkeHUh?=
human SW872 cell NIXlXo1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIf2R4ZKdmirYnn0bY9vKG:oIHj1cYFvKFOZOEeyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlcvQTlibl2u Mkf3V2FPT0WU
human C2BBe1 cell Mmr4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoS4TY5pcWKrdHnvckBw\iCqdX3hckBEOkKEZUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yPE42PCCwTT6= NH30VotUSU6JRWK=
human MZ7-mel cell MlW1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVnkPI97UW6qaXLpeIlwdiCxZjDoeY1idiCPWketcYVtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjlwNEOgcm0v MV;TRW5ITVJ?
human HCC2998 cell MoDGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4q0VWlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMkm5PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM{NjZ4IH7NMi=> MlvwV2FPT0WU
human HO-1-N-1 cell MojOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkPFTY5pcWKrdHnvckBw\iCqdX3hckBJVy1zLV6tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM1NjR|IH7NMi=> NHf6[ZFUSU6JRWK=
human SW756 cell NF\Xd2lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXTUTlhsUW6qaXLpeIlwdiCxZjDoeY1idiCVV{e1OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM1NjR3IH7NMi=> NVjVVG4xW0GQR1XS
human NCI-H1437 cell Mm\WS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NE[4NXZKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVQ{PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN2LkS5JI5ONg>? MXLTRW5ITVJ?
human NCI-H747 cell M3exfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{DGWWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi3OFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{PC57ODDuUU4> MV;TRW5ITVJ?
human SK-MEL-2 cell MlLsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVzUU3BzUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN3LkKgcm0v NWqzbVdFW0GQR1XS
human MZ2-MEL cell NVLGWJIxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXPJcohq[mm2aX;uJI9nKGi3bXHuJG1bOi2PRVygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOU43PSCwTT6= Mn\3V2FPT0WU
human PSN1 cell M{TI[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYnIVIRxUW6qaXLpeIlwdiCxZjDoeY1idiCSU16xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|gvPDVibl2= M4\CfXNCVkeHUh?=
human CAL-39 cell M3XldGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEHy[VVKdmirYnn0bY9vKG:oIHj1cYFvKEODTD2zPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM6NjB2IH7NMi=> NXPES491W0GQR1XS
human LOXIMVI cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGxQYEmPVlmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPU4{QSCwTT6= NIPUcZhUSU6JRWK=
human COLO-792 cell NGTKbVhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWfQcm42UW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVc6OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTR|LkG1JI5ONg>? NFPwPFhUSU6JRWK=
human CAL-27 cell NUnYZo92T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NES1OZNKdmirYnn0bY9vKG:oIHj1cYFvKEODTD2yO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ1NjlzIH7N MmDuV2FPT0WU
human AsPC-1 cell M4PkT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlLXTY5pcWKrdHnvckBw\iCqdX3hckBCe1CFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20OU4zQCCwTT6= M3q2cnNCVkeHUh?=
human NCI-H2291 cell MkPWS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXvRN3NtUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIzQTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12Nj60OkBvVS5? NFzJNXVUSU6JRWK=
human RCM-1 cell M3HsVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVLyN41EUW6qaXLpeIlwdiCxZjDoeY1idiCUQ12tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ3Njh3IH7NMi=> NI\0W|RUSU6JRWK=
human NCI-H292 cell MkLyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlzRTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEK5NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ4NjN7IH7NMi=> Mk\pV2FPT0WU
human WM-115 cell M13EUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkLpTY5pcWKrdHnvckBw\iCqdX3hckBYVS1zMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20PE42KG6PLh?= MmjrV2FPT0WU
human RT-112 cell NXu0WYdWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{T5TmlvcGmkaYTpc44hd2ZiaIXtZY4hWlRvMUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFgvQDRibl2u MXLTRW5ITVJ?
human HT-29 cell MkTvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUjPR2dEUW6qaXLpeIlwdiCxZjDoeY1idiCKVD2yPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUxNjR7IH7NMi=> NUTBd3FoW0GQR1XS
human RKO cell growth MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUPJcohq[mm2aX;uJI9nKGi3bXHuJHJMVyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTV{LkCyJI5ONg>? NIjjb2dUSU6JRWK=
human KY821 cell M2eweGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlvhTY5pcWKrdHnvckBw\iCqdX3hckBMYTh{MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWzMlMhdk1w MlK1V2FPT0WU
human LB1047-RCC cell NWTDd3BzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1;PR2lvcGmkaYTpc44hd2ZiaIXtZY4hVEJzMES3MXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTV7Lk[1JI5ONg>? M3[3VnNCVkeHUh?=
human SW1116 cell NIPNOFhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3m2[GlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzMUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OlAvPDlibl2u M1XDN3NCVkeHUh?=
human P12-ICHIKAWA cell NUfCS3NGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3PldmlvcGmkaYTpc44hd2ZiaIXtZY4hWDF{LVnDTGlMSVeDIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NkKuNlchdk1w M3zvdnNCVkeHUh?=
human HCC70 cell NWPCUlZzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlTBTY5pcWKrdHnvckBw\iCqdX3hckBJS0N5MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[zMlAyKG6PLh?= NY[0Z2RrW0GQR1XS
human MIA-PaCa-2 cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnrmTY5pcWKrdHnvckBw\iCqdX3hckBOUUFvUHHDZU0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PjNwNUOgcm0v NWnpSWdUW0GQR1XS
human LoVo cell NYi3WHdNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF71Tm5KdmirYnn0bY9vKG:oIHj1cYFvKEyxVn:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22OU4zQSCwTT6= NU\DdGtUW0GQR1XS
human LB2241-RCC cell NXzZRpVNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnTTTY5pcWKrdHnvckBw\iCqdX3hckBNSjJ{NEGtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PjVwNUKgcm0v MlTSV2FPT0WU
human GAK cell M{\MVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1vpeGlvcGmkaYTpc44hd2ZiaIXtZY4hT0GNIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Nk[uPFchdk1w NXzjT|d2W0GQR1XS
human RD cell NYTOUGlTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoXKTY5pcWKrdHnvckBw\iCqdX3hckBTTCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZ5LkGgcm0v MoHDV2FPT0WU
human KNS-62 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXXB[YNEUW6qaXLpeIlwdiCxZjDoeY1idiCNTmOtOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03QS57OTDuUU4> MlPMV2FPT0WU
human HD-MY-Z cell MmH4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn[yTY5pcWKrdHnvckBw\iCqdX3hckBJTC2PWT3aJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O|EvOTJibl2u M{jYfHNCVkeHUh?=
human COR-L105 cell NX;MW3kzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWHJcohq[mm2aX;uJI9nKGi3bXHuJGNQWi2OMUC1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O|EvPzFibl2u M{H6OnNCVkeHUh?=
human IA-LM cell M3HMR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUTTdYJIUW6qaXLpeIlwdiCxZjDoeY1idiCLQT3MUUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVc{NjJ6IH7NMi=> NUPNRY82W0GQR1XS
human EM-2 cell M2XiNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{GwOGlvcGmkaYTpc44hd2ZiaIXtZY4hTU1vMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUe0Mlchdk1w NEXVeGVUSU6JRWK=
human NB69 cell NV7kVZB[T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoW0TY5pcWKrdHnvckBw\iCqdX3hckBPSjZ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYm= M2H5OHNCVkeHUh?=
human HuP-T3 cell MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2T6XWlvcGmkaYTpc44hd2ZiaIXtZY4hUHWSLWSzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFMvQTNibl2u MmLwV2FPT0WU
human BB30-HNC cell MljOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml\HTY5pcWKrdHnvckBw\iCqdX3hckBDSjNyLVjOR{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVg2NjVzIH7NMi=> MoDOV2FPT0WU
human HT-1080 cell MnXmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1XSTmlvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMUC4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVg2Njh6IH7NMi=> MnTyV2FPT0WU
human RMG-I cell NYrsUJJ5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFntVXBKdmirYnn0bY9vKG:oIHj1cYFvKFKPRz3JJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFcvOzRibl2u Ml7hV2FPT0WU
human HCC1419 cell NYjJcHU2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{[yOmlvcGmkaYTpc44hd2ZiaIXtZY4hUEOFMUSxPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkyNjN6IH7NMi=> MkS3V2FPT0WU
human SW780 cell MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFe0cnlKdmirYnn0bY9vKG:oIHj1cYFvKFOZN{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVIvOzJibl2u MXXTRW5ITVJ?
human SNU-387 cell M{jCfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3OzSmlvcGmkaYTpc44hd2ZiaIXtZY4hW06XLUO4O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk{NjN4IH7N NHG2UZZUSU6JRWK=
human LAMA-84 cell NGfZSoJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVXJcohq[mm2aX;uJI9nKGi3bXHuJGxCVUFvOESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25OE43QCCwTT6= NGLPS3FUSU6JRWK=
human MV-4-11 cell NUSydJZQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MULJcohq[mm2aX;uJI9nKGi3bXHuJG1XNTRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25OE44OyCwTT6= M4fpcHNCVkeHUh?=
human EGI-1 cell NHj6S3JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkPLTY5pcWKrdHnvckBw\iCqdX3hckBGT0lvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm1MlgyKG6PLh?= NH;0XnlUSU6JRWK=
human NCI-SNU-1 cell M1yxUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4e3RmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLWPOWU0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QTZwN{Ogcm0v M33NWXNCVkeHUh?=
human MEG-01 cell Ml24S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYnJcohq[mm2aX;uJI9nKGi3bXHuJG1GTy1yMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm3Mlc4KG6PLh?= M4O2XnNCVkeHUh?=
human OMC-1 cell NW\JcW5uT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV7OfHU5UW6qaXLpeIlwdiCxZjDoeY1idiCRTVOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExOC5{MzDuUU4> NGHLRYtUSU6JRWK=
human NB10 cell NIOwN2FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NITzS2xKdmirYnn0bY9vKG:oIHj1cYFvKE6EMUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNFAvPDJibl2u MkXsV2FPT0WU
human CAL-62 cell NH;lXphIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXrMVZA2UW6qaXLpeIlwdiCxZjDoeY1idiCFQVytOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yODBwN{igcm0v MVPTRW5ITVJ?
human NCI-H2087 cell NV\U[plGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkDjTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwPFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yODFwMUSgcm0v MmjpV2FPT0WU
human MDA-MB-175-VII cell MYrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mne0TY5pcWKrdHnvckBw\iCqdX3hckBOTEFvTVKtNVc2NV[LSTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5 NV33[Hh2W0GQR1XS
human LS-513 cell NXv0VYpOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWXCNXpxUW6qaXLpeIlwdiCxZjDoeY1idiCOUz21NVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOTRwOEOgcm0v MYXTRW5ITVJ?
human HN cell growth MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml\UTY5pcWKrdHnvckBw\iCqdX3hckBJViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{Mj61PUBvVS5? M4LPbXNCVkeHUh?=
human ABC-1 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4PJ[GlvcGmkaYTpc44hd2ZiaIXtZY4hSUKFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNlMvODJibl2u M2PzV3NCVkeHUh?=
human SJSA-1 cell NXvGW|VGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MoHZTY5pcWKrdHnvckBw\iCqdX3hckBUUlODLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNlMvOTlibl2u MkDtV2FPT0WU
human PANC1 cells Moj1SpVv[3Srb36gZZN{[Xl? MnnvNVAh|ryP M{DrU|EhcA>? M{XQ[WlvcGmkaYTpc44hd2ZiTVXLNUBqdiCqdX3hckBRSU6FMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4heEW{a{GvNkBt\X[nbDDheEAyOCC3TTDh[pRmeiBzIHjyJIJ6KFenc4Tldo4h[myxdITpcoch[W6jbInzbZM> NFz6cWgzPTd4Nk[zNy=>
human MCF7 cells M1qxVWZ2dmO2aX;uJIF{e2G7 MYK3OUBucW6| MoXCTY5pcWKrdHnvckBw\iCPRXuxM|IhcW5iaIXtZY4hVUOINzDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBGWkticHjvd5Bpd3K7bHH0bY9vKGGodHXyJFc2KG2rboOgZpkhX2W|dHXyckBjdG:2dHnu[{BidmGueYPpdy=> M4DobVI{Ozl6NEWz

... 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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • 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

Bio Calculators

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    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

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02510001 Active not recruiting Solid Tumor|Colorectal Cancer University of Oxford|Queen''s University Belfast|Oxford University Hospitals NHS Trust|Velindre NHS Trust|University Hospital Antwerp|Hospital Vall d''Hebron|Saint Antoine University Hospital|European Georges Pompidou Hospital|Pfizer|University of Turin Italy|Belfast Health and Social Care Trust|Beaumont Hospital|European Commission|Array BioPharma|University of Paris 5 - Rene Descartes November 2014 Phase 1
NCT02510001 Active not recruiting Solid Tumor|Colorectal Cancer University of Oxford|Queen''s University Belfast|Oxford University Hospitals NHS Trust|Velindre NHS Trust|University Hospital Antwerp|Hospital Vall d''Hebron|Saint Antoine University Hospital|European Georges Pompidou Hospital|Pfizer|University of Turin Italy|Belfast Health and Social Care Trust|Beaumont Hospital|European Commission|Array BioPharma|University of Paris 5 - Rene Descartes November 2014 Phase 1
NCT02096471 Completed Neurofibromatosis Type 1 and Growing or Symptomatic Inoperable PN University of Alabama at Birmingham June 2014 Phase 2
NCT02096471 Completed Neurofibromatosis Type 1 and Growing or Symptomatic Inoperable PN University of Alabama at Birmingham June 2014 Phase 2
NCT02039336 Recruiting Colorectal Cancer The Netherlands Cancer Institute|Pfizer January 2014 Phase 1|Phase 2
NCT02022982 Active not recruiting KRAS Mutant Non-Small Cell Lung Cancer|Solid Tumors Dana-Farber Cancer Institute January 2014 Phase 1|Phase 2

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 Products4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID