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 164 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 MlWzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnzITY5pcWKrdHnvckBw\iCqdX3hckBEUFBvMkGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE42Ojdibl2u MX;TRW5ITVJ?
human M14 cell M3u0WGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWPJcohq[mm2aX;uJI9nKGi3bXHuJG0yPCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEWgcm0v NXvIXWpmW0GQR1XS
human SK-MEL-28 cell NHXie|JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXTJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvPTJibl2u MVzTRW5ITVJ?
human NOMO-1 cell NFXHNohIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFLFdGJKdmirYnn0bY9vKG:oIHj1cYFvKE6RTV:tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvODdibl2u M{DhcXNCVkeHUh?=
human A375 cell M3v1Smdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn;MTY5pcWKrdHnvckBw\iCqdX3hckBCOzd3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mj62PUBvVS5? MlHRV2FPT0WU
human DU-4475 cell MoLwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlHXTY5pcWKrdHnvckBw\iCqdX3hckBFXS12NEe1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{42PyCwTT6= NEDBbnpUSU6JRWK=
human C32 cell NXnmToRIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWfJcohq[mm2aX;uJI9nKGi3bXHuJGM{OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNwNkegcm0v MkLWV2FPT0WU
human BPH-1 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkjTTY5pcWKrdHnvckBw\iCqdX3hckBDWEhvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOuPVUhdk1w Mn3SV2FPT0WU
human CP50-MEL-B cell NXrnVVR5T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2nsR2lvcGmkaYTpc44hd2ZiaIXtZY4hS1B3MD3NSWwuSiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTRwNUigcm0v NU[xO2Y6W0GQR1XS
human H9 cell MmjpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXLZS2tHUW6qaXLpeIlwdiCxZjDoeY1idiCKOTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuO|chdk1w NGD2WWpUSU6JRWK=
human HTC-C3 cell M2HWZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4j2W2lvcGmkaYTpc44hd2ZiaIXtZY4hUFSFLVOzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU45QSCwTT6= MWfTRW5ITVJ?
human BHT-101 cell MorRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4nzfWlvcGmkaYTpc44hd2ZiaIXtZY4hSkiWLUGwNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvPyCwTT6= Mn:xV2FPT0WU
human COLO-741 cell NXXjWI5ET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWG4XJJPUW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVc1OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTdwMTDuUU4> MVLTRW5ITVJ?
human OVCAR-5 cell NUPJeXVwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1HmZWlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvQDJibl2u MkPsV2FPT0WU
human A549 cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4HZfmlvcGmkaYTpc44hd2ZiaIXtZY4hSTV2OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUeuPFkhdk1w NGfK[XpUSU6JRWK=
human SH-4 cell growth M1;zeWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHr0eoZKdmirYnn0bY9vKG:oIHj1cYFvKFOKLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24MlI3KG6PLh?= NFPXSFZUSU6JRWK=
human SK-N-AS cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIf0codKdmirYnn0bY9vKG:oIHj1cYFvKFONLV6tRXMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05NjR2IH7NMi=> MkXJV2FPT0WU
human HT-144 cell MlHwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWrDS4tpUW6qaXLpeIlwdiCxZjDoeY1idiCKVD2xOFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05Njl5IH7NMi=> NXHPbZBoW0GQR1XS
human MEL-HO cell MmPMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3TC[mlvcGmkaYTpc44hd2ZiaIXtZY4hVUWOLVjPJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU41QSCwTT6= NEjGRWFUSU6JRWK=
human COLO-679 cell M{fMR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkTBTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLU[3PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExNjBzIH7N M2j6e3NCVkeHUh?=
human HuP-T4 cell NXXi[GFHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2HtOGlvcGmkaYTpc44hd2ZiaIXtZY4hUHWSLWS0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvQThibl2u MlPzV2FPT0WU
human H-EMC-SS cell Mn;US5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3y4OGlvcGmkaYTpc44hd2ZiaIXtZY4hUC2HTVOtV3Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS5yMjDuUU4> NGfyNY9USU6JRWK=
human LB2518-MEL cell M4rW[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2exNmlvcGmkaYTpc44hd2ZiaIXtZY4hVEJ{NUG4MW1GVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFzLkGzJI5ONg>? NXjrRVBGW0GQR1XS
human HL-60 cell NGLlVHFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3PxS2lvcGmkaYTpc44hd2ZiaIXtZY4hUExvNkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNU4yPSCwTT6= M2PLfnNCVkeHUh?=
human NCI-H1666 cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4[1SGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixOlY3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTFwMUegcm0v NYTEdINtW0GQR1XS
human A101D cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{DYb2lvcGmkaYTpc44hd2ZiaIXtZY4hSTFyMVSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNU41PSCwTT6= M1:2VHNCVkeHUh?=
human RVH-421 cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYrHSoU2UW6qaXLpeIlwdiCxZjDoeY1idiCUVlitOFIyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwNkSgcm0v MmPJV2FPT0WU
human Hs-578-T cell NEGwUm1Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFfzRVVKdmirYnn0bY9vKG:oIHj1cYFvKEi|LUW3PE1VKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJwN{mgcm0v MUTTRW5ITVJ?
human A375 cells MnzzVJJwdGmoZYLheIlwdiCjc4PhfS=> MVS3NkBp NF;ifG5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO|Uh[2WubIOg[ZhxemW|c3nu[{BDWkGIIG[2NFBGKG23dHHueEBi\nSncjC3NkBpenNiYomgR4VtdCC2aYTldk1odG9iYYPzZZktKEmFNUC9NVMhdk1w MUeyN|Q4PDN6OB?=
human DOK cell NYXLc4ZET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV7EXJd5UW6qaXLpeIlwdiCxZjDoeY1idiCGT1ugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{41KG6PLh?= NVzIdWI{W0GQR1XS
human Mewo cell NFnvUY9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4XidWlvcGmkaYTpc44hd2ZiaIXtZY4hVWW5bzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlQ2KG6PLh?= MnLIV2FPT0WU
human ONS-76 cell NEDHcItIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXTJcohq[mm2aX;uJI9nKGi3bXHuJG9PWy15NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlUyKG6PLh?= MmnVV2FPT0WU
human UACC-257 cell Mm\iS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVPQO4ZbUW6qaXLpeIlwdiCxZjDoeY1idiCXQVPDMVI2PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF2Lk[yJI5ONg>? MnT0V2FPT0WU
human SW626 cell NWTIb2pCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1zue2lvcGmkaYTpc44hd2ZiaIXtZY4hW1d4Mk[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE46OSCwTT6= NYfXVZk3W0GQR1XS
human SW620 cell NHXVd3hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{PMRmlvcGmkaYTpc44hd2ZiaIXtZY4hW1d4MkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE46PSCwTT6= Mlu0V2FPT0WU
human TYK-nu cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkDyTY5pcWKrdHnvckBw\iCqdX3hckBVYUtvboWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU4yOyCwTT6= NIPCeItUSU6JRWK=
human ACN cell MnnXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1e1RWlvcGmkaYTpc44hd2ZiaIXtZY4hSUOQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuO|Yhdk1w NY[3WXd[W0GQR1XS
human MIAPaCa2 cells MYPQdo9tcW[ncnH0bY9vKGG|c3H5 NXnGWXlpSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNTWFR[UOjMjDj[YxteyxiSVO1NF0yPyCwTT6= M2\STVI{PDd2M{i4
human T-24 cell M3\5Zmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV3R[nNOUW6qaXLpeIlwdiCxZjDoeY1idiCWLUK0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVkvPzFibl2u NWLwT|J[W0GQR1XS
human AGS cell M1zaUmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NInLcIFKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKwMlQyKG6PLh?= MnvsV2FPT0WU
human SW872 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3rtcmlvcGmkaYTpc44hd2ZiaIXtZY4hW1d6N{KgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yO{46QSCwTT6= NWrNS5hNW0GQR1XS
human C2BBe1 cell MnjmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4PtR2lvcGmkaYTpc44hd2ZiaIXtZY4hSzKEQnWxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvPTRibl2u MoPvV2FPT0WU
human MZ7-mel cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mnz5TY5pcWKrdHnvckBw\iCqdX3hckBOYjdvbXXsJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlkvPDNibl2u NIDIWJNUSU6JRWK=
human HCC2998 cell MlnCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGPmRmFKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{K5PVgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Oy54NjDuUU4> NGq2SJdUSU6JRWK=
human HO-1-N-1 cell M1;h[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWrJcohq[mm2aX;uJI9nKGi3bXHuJGhQNTFvTj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|QvPDNibl2u NUPlTGtWW0GQR1XS
human SW756 cell NEPVeplIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoDCTY5pcWKrdHnvckBw\iCqdX3hckBUXzd3NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO0MlQ2KG6PLh?= NUPJT4Q4W0GQR1XS
human NCI-H1437 cell MmHpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFvqVWtKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVQ{PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN2LkS5JI5ONg>? NH7rbFhUSU6JRWK=
human NCI-H747 cell MkmxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlPnTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEe0O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM1Njl6IH7NMi=> NV\nUmlMW0GQR1XS
human SK-MEL-2 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXn6TY5EUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN3LkKgcm0v MXXTRW5ITVJ?
human MZ2-MEL cell MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHzOPW1KdmirYnn0bY9vKG:oIHj1cYFvKE2cMj3NSWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{PS54NTDuUU4> MWDTRW5ITVJ?
human PSN1 cell NVPEXG9OT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX72THRwUW6qaXLpeIlwdiCxZjDoeY1idiCSU16xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|gvPDVibl2= NInEfXFUSU6JRWK=
human CAL-39 cell NYDacXAzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGTMdXFKdmirYnn0bY9vKG:oIHj1cYFvKEODTD2zPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM6NjB2IH7NMi=> M3\qSHNCVkeHUh?=
human LOXIMVI cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGW0PWhKdmirYnn0bY9vKG:oIHj1cYFvKEyRWFnNWmkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{QS5|OTDuUU4> M{\jenNCVkeHUh?=
human COLO-792 cell NFLEW3NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIfB[lRKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tO|kzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PDNwMUWgcm0v NFywSHRUSU6JRWK=
human CAL-27 cell MoD3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4XmbWlvcGmkaYTpc44hd2ZiaIXtZY4hS0GOLUK3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFQvQTFibl2= NGmxXXlUSU6JRWK=
human AsPC-1 cell NHeyR4FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWLlSnNJUW6qaXLpeIlwdiCxZjDoeY1idiCDc2DDMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01PS5{ODDuUU4> M12zeHNCVkeHUh?=
human NCI-H2291 cell MlXkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUnJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkK5NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ3NjR4IH7NMi=> NGftPXRUSU6JRWK=
human RCM-1 cell M32zS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlLvTY5pcWKrdHnvckBw\iCqdX3hckBTS01vMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS2Mlg2KG6PLh?= NUW1T21vW0GQR1XS
human NCI-H292 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIn2c2FKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlkzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PDdwM{mgcm0v MorrV2FPT0WU
human WM-115 cell MoTuS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJHdONTFzNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS4MlUhdk1w NF23U5pUSU6JRWK=
human RT-112 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGfh[HdKdmirYnn0bY9vKG:oIHj1cYFvKFKWLUGxNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ5Njh2IH7NMi=> MVHTRW5ITVJ?
human HT-29 cell MmXXS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXz0OpVEUW6qaXLpeIlwdiCxZjDoeY1idiCKVD2yPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUxNjR7IH7NMi=> NG\DNWNUSU6JRWK=
human RKO cell growth NVvDSFRJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHrGO2FKdmirYnn0bY9vKG:oIHj1cYFvKFKNTzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWyMlAzKG6PLh?= NUjsdHhoW0GQR1XS
human KY821 cell NX7ydFAzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4TDb2lvcGmkaYTpc44hd2ZiaIXtZY4hU1l6MkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21N{4{KG6PLh?= M{Hue3NCVkeHUh?=
human LB1047-RCC cell Ml[1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4\BZ2lvcGmkaYTpc44hd2ZiaIXtZY4hVEJzMES3MXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTV7Lk[1JI5ONg>? Mnm4V2FPT0WU
human SW1116 cell M3Xjcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYHJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTFzNjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[wMlQ6KG6PLh?= NEnN[GtUSU6JRWK=
human P12-ICHIKAWA cell MmLxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{T2PWlvcGmkaYTpc44hd2ZiaIXtZY4hWDF{LVnDTGlMSVeDIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NkKuNlchdk1w Mk\5V2FPT0WU
human HCC70 cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIrIXGRKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{ewJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OlMvODFibl2u NGTJTpdUSU6JRWK=
human MIA-PaCa-2 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXHJcohq[mm2aX;uJI9nKGi3bXHuJG1KSS2SYVPhMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03Oy53MzDuUU4> MlT1V2FPT0WU
human LoVo cell M3XtcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGq0THFKdmirYnn0bY9vKG:oIHj1cYFvKEyxVn:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22OU4zQSCwTT6= NHrWbodUSU6JRWK=
human LB2241-RCC cell NX6wT2tWT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV;Jcohq[mm2aX;uJI9nKGi3bXHuJGxDOjJ2MT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03PS53MjDuUU4> MWHTRW5ITVJ?
human GAK cell MmDZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkPpTY5pcWKrdHnvckBw\iCqdX3hckBISUtiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD14Nj64O{BvVS5? M{i0TnNCVkeHUh?=
human RD cell NEW2emlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MljITY5pcWKrdHnvckBw\iCqdX3hckBTTCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZ5LkGgcm0v MVXTRW5ITVJ?
human KNS-62 cell NFv6ZlFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnTmTY5pcWKrdHnvckBw\iCqdX3hckBMVlNvNkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22PU46QSCwTT6= NYfpSGU3W0GQR1XS
human HD-MY-Z cell NE\5bY9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1raXmlvcGmkaYTpc44hd2ZiaIXtZY4hUERvTWmtXkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcyNjF{IH7NMi=> MlmyV2FPT0WU
human COR-L105 cell MkXtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1zlXWlvcGmkaYTpc44hd2ZiaIXtZY4hS0:ULVyxNFUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04OS55MTDuUU4> NWnLO5RjW0GQR1XS
human IA-LM cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVrJcohq[mm2aX;uJI9nKGi3bXHuJGlCNUyPIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;N{OuNlghdk1w NFT6UGVUSU6JRWK=
human EM-2 cell MkjsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUHBVopRUW6qaXLpeIlwdiCxZjDoeY1idiCHTT2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O|QvPyCwTT6= Ml;TV2FPT0WU
human NB69 cell NILJXFdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1j4PWlvcGmkaYTpc44hd2ZiaIXtZY4hVkJ4OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5 NHHNUVNUSU6JRWK=
human HuP-T3 cell NVz4fZhjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3q4d2lvcGmkaYTpc44hd2ZiaIXtZY4hUHWSLWSzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFMvQTNibl2u MnTVV2FPT0WU
human BB30-HNC cell NVXpbIVCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHrqNnFKdmirYnn0bY9vKG:oIHj1cYFvKEKEM{CtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QDVwNUGgcm0v MWTTRW5ITVJ?
human HT-1080 cell MmrPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmXSTY5pcWKrdHnvckBw\iCqdX3hckBJXC1zMEiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFUvQDhibl2u M3rI[3NCVkeHUh?=
human RMG-I cell M2jG[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4fZd2lvcGmkaYTpc44hd2ZiaIXtZY4hWk2JLVmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24O{4{PCCwTT6= NEDTSZRUSU6JRWK=
human HCC1419 cell NHnwbYFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MV3Jcohq[mm2aX;uJI9nKGi3bXHuJGhESzF2MUmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25NU4{QCCwTT6= MnzlV2FPT0WU
human SW780 cell NGSzOItIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXfsdoN6UW6qaXLpeIlwdiCxZjDoeY1idiCVV{e4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkzNjN{IH7NMi=> MljnV2FPT0WU
human SNU-387 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHfTSotKdmirYnn0bY9vKG:oIHj1cYFvKFOQVT2zPFch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Oy5|NjDuUS=> NUHrSlhNW0GQR1XS
human LAMA-84 cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmHhTY5pcWKrdHnvckBw\iCqdX3hckBNSU2DLUi0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVQvPjhibl2u MljnV2FPT0WU
human MV-4-11 cell NHrEdJlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGXTN2FKdmirYnn0bY9vKG:oIHj1cYFvKE2YLUStNVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06PC55MzDuUU4> M{OyUnNCVkeHUh?=
human EGI-1 cell NYLYVJRET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NE\NUWZKdmirYnn0bY9vKG:oIHj1cYFvKEWJST2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVUvQDFibl2u NVrUTXI6W0GQR1XS
human NCI-SNU-1 cell M1ziO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NViyeYl{UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtV25WNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD17Nj63N{BvVS5? NGDscolUSU6JRWK=
human MEG-01 cell NIPONYRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVnJcohq[mm2aX;uJI9nKGi3bXHuJG1GTy1yMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm3Mlc4KG6PLh?= MVHTRW5ITVJ?
human OMC-1 cell Mnq4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1XPVmlvcGmkaYTpc44hd2ZiaIXtZY4hV02FLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNFAvOjNibl2u Ml3BV2FPT0WU
human NB10 cell MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGj3N3VKdmirYnn0bY9vKG:oIHj1cYFvKE6EMUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNFAvPDJibl2u M17nN3NCVkeHUh?=
human CAL-62 cell Mn3DS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXzDeVBOUW6qaXLpeIlwdiCxZjDoeY1idiCFQVytOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yODBwN{igcm0v NHfaZ5FUSU6JRWK=
human NCI-H2087 cell Mo[wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHj5dIdKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlA5PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFyMT6xOEBvVS5? M3\WS3NCVkeHUh?=
human MDA-MB-175-VII cell M2jSV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVPMeItSUW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuOTd3LW\JTUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6 MlTHV2FPT0WU
human LS-513 cell NW\0TGN1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWPJcohq[mm2aX;uJI9nKGi3bXHuJGxUNTVzMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGxOE45OyCwTT6= NUD0eJY5W0GQR1XS
human HN cell growth NHHDOpRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mo\QTY5pcWKrdHnvckBw\iCqdX3hckBJViClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF{Mj61PUBvVS5? NWH5Nm9JW0GQR1XS
human ABC-1 cell Ml3wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4jLVWlvcGmkaYTpc44hd2ZiaIXtZY4hSUKFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNlMvODJibl2u M2PEOXNCVkeHUh?=
human SJSA-1 cell M3PIWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWTSOIo1UW6qaXLpeIlwdiCxZjDoeY1idiCVSmPBMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOjNwMUmgcm0v NWLy[XF1W0GQR1XS
human PANC1 cells M2S3[2Z2dmO2aX;uJIF{e2G7 MkCyNVAh|ryP NX;qeG9YOSCq MVHJcohq[mm2aX;uJI9nKE2HS{GgbY4hcHWvYX6gVGFPSzFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJJBGemtzL{KgcIV3\WxiYYSgNVAhfU1iYX\0[ZIhOSCqcjDifUBY\XO2ZYLuJIJtd3S2aX7nJIFv[Wy7c3nz M4S4VVI2PzZ4NkOz
human MCF7 cells MkG3SpVv[3Srb36gZZN{[Xl? MVq3OUBucW6| NVHsfYhEUW6qaXLpeIlwdiCxZjDNSYsyNzJiaX6gbJVu[W5iTVPGO{Bk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCHUlugdIhwe3Cqb4L5cIF1cW:wIHHmeIVzKDd3IH3pcpMh[nliV3XzeIVzdiCkbH;0eIlv\yCjbnHsfZNqew>? M1LQOFI{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

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Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID