PD0325901(Mirdametinib)

For research use only. Not for use in humans.

Licensed by Pfizer Catalog No.S1036

492 publications

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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Selleck's PD0325901(Mirdametinib) has been cited by 492 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 MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWPETFN5UW6qaXLpeIlwdiCxZjDoeY1idiCFSGCtNlEzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC53Mkegcm0v NFHpd4xUSU6JRWK=
human M14 cell NHztZpVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWfpOXZ6UW6qaXLpeIlwdiCxZjDoeY1idiCPMUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlQ2KG6PLh?= M3vOfnNCVkeHUh?=
human SK-MEL-28 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVzSfZprUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOjhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkWyJI5ONg>? NFz4dXBUSU6JRWK=
human NOMO-1 cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYLVWpBVUW6qaXLpeIlwdiCxZjDoeY1idiCQT13PMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjB5IH7NMi=> M36wW3NCVkeHUh?=
human A375 cell NYPqVYdNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUTuXnJjUW6qaXLpeIlwdiCxZjDoeY1idiCDM{e1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk43QSCwTT6= NGDOZoJUSU6JRWK=
human DU-4475 cell MmHTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3fwXGlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPTdibl2u NETFTnJUSU6JRWK=
human C32 cell NX2xRnZYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkfhTY5pcWKrdHnvckBw\iCqdX3hckBEOzJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Lk[3JI5ONg>? M4jS[XNCVkeHUh?=
human BPH-1 cell M4PlN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGW5[W1KdmirYnn0bY9vKG:oIHj1cYFvKEKSSD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PSCwTT6= NEOwTVRUSU6JRWK=
human CP50-MEL-B cell NEXOdXRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVzJcohq[mm2aX;uJI9nKGi3bXHuJGNRPTBvTVXMMWIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01NjV6IH7NMi=> NGLMeWdUSU6JRWK=
human H9 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoLsTY5pcWKrdHnvckBw\iCqdX3hckBJQSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTVwN{egcm0v MXPTRW5ITVJ?
human HTC-C3 cell NYLwVJFjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn;oTY5pcWKrdHnvckBw\iCqdX3hckBJXENvQ{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21Mlg6KG6PLh?= MU\TRW5ITVJ?
human BHT-101 cell MkfZS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV7tOIFGUW6qaXLpeIlwdiCxZjDoeY1idiCESGStNVAyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi55IH7NMi=> MUDTRW5ITVJ?
human COLO-741 cell NYT3b5V1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEmxT5FKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tO|QyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Py5zIH7NMi=> NUDjSpZ5W0GQR1XS
human OVCAR-5 cell MnLJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1LMS2lvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvQDJibl2u NITzXHpUSU6JRWK=
human A549 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHS4WlJKdmirYnn0bY9vKG:oIHj1cYFvKEF3NEmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23Mlg6KG6PLh?= MWPTRW5ITVJ?
human SH-4 cell growth M{Po[Wdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWfJcohq[mm2aX;uJI9nKGi3bXHuJHNJNTRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD16LkK2JI5ONg>? MWrTRW5ITVJ?
human SK-N-AS cell MmfsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH;DemJKdmirYnn0bY9vKG:oIHj1cYFvKFONLV6tRXMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05NjR2IH7NMi=> NG[0SZZUSU6JRWK=
human HT-144 cell M3rhV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIniPW1KdmirYnn0bY9vKG:oIHj1cYFvKEiWLUG0OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVgvQTdibl2u M2Phe3NCVkeHUh?=
human MEL-HO cell NHrnOW5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnTtTY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlQ6KG6PLh?= M2jTW3NCVkeHUh?=
human COLO-679 cell NIO2e|hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUXJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vNke5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvODFibl2= M4jaN3NCVkeHUh?=
human HuP-T4 cell NF;ZeFZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mme4TY5pcWKrdHnvckBw\iCqdX3hckBJfVBvVESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE46QCCwTT6= NXfFc4tjW0GQR1XS
human H-EMC-SS cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGPIZ41KdmirYnn0bY9vKG:oIHj1cYFvKEhvRV3DMXNUKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTFwMEKgcm0v NFPSNlRUSU6JRWK=
human LB2518-MEL cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mlf5TY5pcWKrdHnvckBw\iCqdX3hckBNSjJ3MUitUWVNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTFwMUOgcm0v Mmf0V2FPT0WU
human HL-60 cell M2fpOGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1nPd2lvcGmkaYTpc44hd2ZiaIXtZY4hUExvNkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNU4yPSCwTT6= M{ntcHNCVkeHUh?=
human NCI-H1666 cell NWfGZ|BOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkTSTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG2OlYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS5zNzDuUU4> M{L0T3NCVkeHUh?=
human A101D cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlLNTY5pcWKrdHnvckBw\iCqdX3hckBCOTBzRDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGxMlQ2KG6PLh?= M2TDNXNCVkeHUh?=
human RVH-421 cell MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1K4UWlvcGmkaYTpc44hd2ZiaIXtZY4hWl[KLUSyNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjZ2IH7NMi=> MljoV2FPT0WU
human Hs-578-T cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4SwZmlvcGmkaYTpc44hd2ZiaIXtZY4hUHNvNUe4MXQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOi55OTDuUU4> MV7TRW5ITVJ?
human A375 cells NXLhZ3V1WHKxbHnm[ZJifGmxbjDhd5NigQ>? M3rieVczKGh? MlzGRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDM{e1JINmdGy|IHX4dJJme3OrbnegRnJCTiCYNkCwSUBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIwhfGm2ZYKt[4xwKGG|c3H5MEBKSzVyPUGzJI5ONg>? MXiyN|Q4PDN6OB?=
human DOK cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoHZTY5pcWKrdHnvckBw\iCqdX3hckBFV0tiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz60JI5ONg>? MWrTRW5ITVJ?
human Mewo cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWL2PGszUW6qaXLpeIlwdiCxZjDoeY1idiCPZYfvJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPDVibl2u NV:wXVFkW0GQR1XS
human ONS-76 cell NGLoOoxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1;oV2lvcGmkaYTpc44hd2ZiaIXtZY4hV06VLUe2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPTFibl2u M2OxOXNCVkeHUh?=
human UACC-257 cell MojrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXHJcohq[mm2aX;uJI9nKGi3bXHuJHVCS0NvMkW3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvPjJibl2u NIfQWZNUSU6JRWK=
human SW626 cell Mom5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXjJcohq[mm2aX;uJI9nKGi3bXHuJHNYPjJ4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUSuPVEhdk1w NF\UVJBUSU6JRWK=
human SW620 cell NELBVnJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVPJcohq[mm2aX;uJI9nKGi3bXHuJHNYPjJyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUSuPVUhdk1w M3W5WXNCVkeHUh?=
human TYK-nu cell NUO1VlVqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUCwPVBMUW6qaXLpeIlwdiCxZjDoeY1idiCWWVutcpUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS5zMzDuUU4> MW\TRW5ITVJ?
human ACN cell NVjmPIJwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1G4SWlvcGmkaYTpc44hd2ZiaIXtZY4hSUOQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuO|Yhdk1w MV;TRW5ITVJ?
human MIAPaCa2 cells NHPHRWFRem:uaX\ldoF1cW:wIHHzd4F6 NEm4NZlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3JRXBiS2F{IHPlcIx{NCCLQ{WwQVE4KG6PLh?= MWCyN|Q4PDN6OB?=
human T-24 cell NYW0TXo{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVnBR|dZUW6qaXLpeIlwdiCxZjDoeY1idiCWLUK0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVkvPzFibl2u NYPVPJlHW0GQR1XS
human AGS cell M1nz[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUTncGxtUW6qaXLpeIlwdiCxZjDoeY1idiCDR2OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNE41OSCwTT6= NIjub5FUSU6JRWK=
human SW872 cell M1zDUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXzJcohq[mm2aX;uJI9nKGi3bXHuJHNYQDd{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkeuPVkhdk1w MW\TRW5ITVJ?
human C2BBe1 cell Mk\NS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVfOZXp5UW6qaXLpeIlwdiCxZjDoeY1idiCFMlLC[VEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQC53NDDuUU4> NFHnb2hUSU6JRWK=
human MZ7-mel cell NEfLPYFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXnJTIdPUW6qaXLpeIlwdiCxZjDoeY1idiCPWketcYVtKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjlwNEOgcm0v MlywV2FPT0WU
human HCC2998 cell MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUPJcohq[mm2aX;uJI9nKGi3bXHuJGhESzJ7OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zN{43PiCwTT6= NHqwb4ZUSU6JRWK=
human HO-1-N-1 cell NWCyRm1OT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYHJcohq[mm2aX;uJI9nKGi3bXHuJGhQNTFvTj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|QvPDNibl2u MoKwV2FPT0WU
human SW756 cell NXrpWo8yT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVK1Z3p1UW6qaXLpeIlwdiCxZjDoeY1idiCVV{e1OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM1NjR3IH7NMi=> NUDYTI5oW0GQR1XS
human NCI-H1437 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFjGRmZKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVQ{PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN2LkS5JI5ONg>? MlPrV2FPT0WU
human NCI-H747 cell MWPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnniTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEe0O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM1Njl6IH7NMi=> NH3Id5ZUSU6JRWK=
human SK-MEL-2 cell Mlm4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWrJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|UvOiCwTT6= MXPTRW5ITVJ?
human MZ2-MEL cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIG4WGhKdmirYnn0bY9vKG:oIHj1cYFvKE2cMj3NSWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{PS54NTDuUU4> NH7O[XVUSU6JRWK=
human PSN1 cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHXYNVBKdmirYnn0bY9vKG:oIHj1cYFvKFCVTkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPE41PSCwTR?= NX:wV2pNW0GQR1XS
human CAL-39 cell M2jqNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3TnR2lvcGmkaYTpc44hd2ZiaIXtZY4hS0GOLUO5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|kvODRibl2u NHnESFdUSU6JRWK=
human LOXIMVI cell NG\1O4tIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mo\3TY5pcWKrdHnvckBw\iCqdX3hckBNV1iLTW\JJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|kvOzlibl2u MW\TRW5ITVJ?
human COLO-792 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoDsTY5pcWKrdHnvckBw\iCqdX3hckBEV0yRLUe5NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ{NjF3IH7NMi=> NEnBbIpUSU6JRWK=
human CAL-27 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHzvb2lKdmirYnn0bY9vKG:oIHj1cYFvKEODTD2yO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ1NjlzIH7N NWfUVJZlW0GQR1XS
human AsPC-1 cell Mo\LS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVXJcohq[mm2aX;uJI9nKGi3bXHuJGF{WENvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS1MlI5KG6PLh?= Mn[3V2FPT0WU
human NCI-H2291 cell NEKzbWFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVv6W|F2UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIzQTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD12Nj60OkBvVS5? MmTzV2FPT0WU
human RCM-1 cell NFrVRpVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHHVTo5KdmirYnn0bY9vKG:oIHj1cYFvKFKFTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFYvQDVibl2u M1LyOXNCVkeHUh?=
human NCI-H292 cell NWjVRpNZT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlTXTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEK5NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ4NjN7IH7NMi=> MlTIV2FPT0WU
human WM-115 cell MljIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVrTR2VyUW6qaXLpeIlwdiCxZjDoeY1idiCZTT2xNVUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01QC53IH7NMi=> MmK2V2FPT0WU
human RT-112 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYW0Zm9LUW6qaXLpeIlwdiCxZjDoeY1idiCUVD2xNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01QC56NDDuUU4> NH73U2NUSU6JRWK=
human HT-29 cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml3sTY5pcWKrdHnvckBw\iCqdX3hckBJXC1{OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWwMlQ6KG6PLh?= NWDUWYc1W0GQR1XS
human RKO cell growth M33yTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4P5PWlvcGmkaYTpc44hd2ZiaIXtZY4hWkuRIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NUKuNFIhdk1w NFLVfodUSU6JRWK=
human KY821 cell M2rnVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF7Hb4FKdmirYnn0bY9vKG:oIHj1cYFvKEu\OEKxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVMvOyCwTT6= NFnVd49USU6JRWK=
human LB1047-RCC cell NGLv[|RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH;j[YNKdmirYnn0bY9vKG:oIHj1cYFvKEyEMUC0O{1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13OT62OUBvVS5? NVHqUm8xW0GQR1XS
human SW1116 cell M4jSN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M37jVWlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzMUG2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OlAvPDlibl2u MnPoV2FPT0WU
human P12-ICHIKAWA cell NEfkSZRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M37XdmlvcGmkaYTpc44hd2ZiaIXtZY4hWDF{LVnDTGlMSVeDIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NkKuNlchdk1w NXPGdnBwW0GQR1XS
human HCC70 cell MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NY\rXGFHUW6qaXLpeIlwdiCxZjDoeY1idiCKQ1O3NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVY{NjBzIH7NMi=> NXXDW|l7W0GQR1XS
human MIA-PaCa-2 cell NYrVeoFLT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkS0TY5pcWKrdHnvckBw\iCqdX3hckBOUUFvUHHDZU0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PjNwNUOgcm0v M1TYW3NCVkeHUh?=
human LoVo cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NF:3RWFKdmirYnn0bY9vKG:oIHj1cYFvKEyxVn:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22OU4zQSCwTT6= M3HWRXNCVkeHUh?=
human LB2241-RCC cell NEO3[ndIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVXJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjJ2MT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03PS53MjDuUU4> MkjYV2FPT0WU
human GAK cell NYDRT2JuT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXrJcohq[mm2aX;uJI9nKGi3bXHuJGdCUyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZ4Lki3JI5ONg>? MXrTRW5ITVJ?
human RD cell MkLGS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnnmTY5pcWKrdHnvckBw\iCqdX3hckBTTCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZ5LkGgcm0v M174ZXNCVkeHUh?=
human KNS-62 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYqwUppIUW6qaXLpeIlwdiCxZjDoeY1idiCNTmOtOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03QS57OTDuUU4> M3GwSXNCVkeHUh?=
human HD-MY-Z cell M{\ZZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NWD2Vos1UW6qaXLpeIlwdiCxZjDoeY1idiCKRD3NXU1bKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PzFwMUKgcm0v NWrCOW9ZW0GQR1XS
human COR-L105 cell NGHteGpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVHJcohq[mm2aX;uJI9nKGi3bXHuJGNQWi2OMUC1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O|EvPzFibl2u MkK1V2FPT0WU
human IA-LM cell M4\3N2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkjKTY5pcWKrdHnvckBw\iCqdX3hckBKSS2OTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUezMlI5KG6PLh?= MVPTRW5ITVJ?
human EM-2 cell NYniW4dXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFHKdpZKdmirYnn0bY9vKG:oIHj1cYFvKEWPLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23OE44KG6PLh?= MnL3V2FPT0WU
human NB69 cell M4\2dWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXPJcohq[mm2aX;uJI9nKGi3bXHuJG5DPjliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeR?= MX\TRW5ITVJ?
human HuP-T3 cell NIrqdHlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIjjWmVKdmirYnn0bY9vKG:oIHj1cYFvKEi3UD3UN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVg{Njl|IH7NMi=> NYn2W3Z5W0GQR1XS
human BB30-HNC cell NVHMXWdGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYjJfmRDUW6qaXLpeIlwdiCxZjDoeY1idiCEQkOwMWhPSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTh3LkWxJI5ONg>? MlLoV2FPT0WU
human HT-1080 cell NIDqdoVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYTCO5BUUW6qaXLpeIlwdiCxZjDoeY1idiCKVD2xNFgxKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QDVwOEigcm0v M1TmU3NCVkeHUh?=
human RMG-I cell NFLUcYtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXHGOlBmUW6qaXLpeIlwdiCxZjDoeY1idiCUTVetTUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVg4NjN2IH7NMi=> Mk\VV2FPT0WU
human HCC1419 cell MlPOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHvRVWxKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{G0NVkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06OS5|ODDuUU4> M1Pud3NCVkeHUh?=
human SW780 cell MWHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkTXTY5pcWKrdHnvckBw\iCqdX3hckBUXzd6MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmyMlMzKG6PLh?= MoDRV2FPT0WU
human SNU-387 cell MnTxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYHMOYViUW6qaXLpeIlwdiCxZjDoeY1idiCVTmWtN|g4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QTNwM{[gcm0> Mn:xV2FPT0WU
human LAMA-84 cell NVnQV|lTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NV\a[GN{UW6qaXLpeIlwdiCxZjDoeY1idiCOQV3BMVg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QTRwNkigcm0v Ml7KV2FPT0WU
human MV-4-11 cell MmTlS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnP4TY5pcWKrdHnvckBw\iCqdX3hckBOXi12LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVQvPzNibl2u NXe3XIhuW0GQR1XS
human EGI-1 cell NWfjO4dGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIDQVHJKdmirYnn0bY9vKG:oIHj1cYFvKEWJST2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVUvQDFibl2u MkSxV2FPT0WU
human NCI-SNU-1 cell NUDUU41PT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M17keGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLWPOWU0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QTZwN{Ogcm0v NHrTZWFUSU6JRWK=
human MEG-01 cell NUDrS2ZNT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NIH0fW9KdmirYnn0bY9vKG:oIHj1cYFvKE2HRz2wNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVk4Njd5IH7NMi=> Mny4V2FPT0WU
human OMC-1 cell NEXZeZpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MonTTY5pcWKrdHnvckBw\iCqdX3hckBQVUNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwNE4zOyCwTT6= NXTVcIR[W0GQR1XS
human NB10 cell MljHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NEXTdmdKdmirYnn0bY9vKG:oIHj1cYFvKE6EMUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNFAvPDJibl2u MXLTRW5ITVJ?
human CAL-62 cell MlS1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYnJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC14MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwNE44QCCwTT6= MmHmV2FPT0WU
human NCI-H2087 cell M{jIZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1fXVWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFg4KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTBzLkG0JI5ONg>? NEDQT5RUSU6JRWK=
human MDA-MB-175-VII cell M161eWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXrJcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj2xO|UuXkmLIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYm= MYjTRW5ITVJ?
human LS-513 cell MoXLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVvzR5R2UW6qaXLpeIlwdiCxZjDoeY1idiCOUz21NVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOTRwOEOgcm0v NHrUUopUSU6JRWK=
human HN cell growth NGX4eXpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4S0VWlvcGmkaYTpc44hd2ZiaIXtZY4hUE5iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMkKuOVkhdk1w NVfqbWxPW0GQR1XS
human ABC-1 cell M{LifWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmLPTY5pcWKrdHnvckBw\iCqdX3hckBCSkNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGyN{4xOiCwTT6= NFzYPVNUSU6JRWK=
human SJSA-1 cell M{fDXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUTCUHFEUW6qaXLpeIlwdiCxZjDoeY1idiCVSmPBMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOjNwMUmgcm0v NXTucFRvW0GQR1XS
human PANC1 cells NWfnNpZ1TnWwY4Tpc44h[XO|YYm= MkjUNVAh|ryP M3j1[FEhcA>? MVLJcohq[mm2aX;uJI9nKE2HS{GgbY4hcHWvYX6gVGFPSzFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIHnuJJBGemtzL{KgcIV3\WxiYYSgNVAhfU1iYX\0[ZIhOSCqcjDifUBY\XO2ZYLuJIJtd3S2aX7nJIFv[Wy7c3nz MU[yOVc3PjZ|Mx?=
human MCF7 cells NXr2dHExTnWwY4Tpc44h[XO|YYm= M2HrW|c2KG2rboO= M{nUUmlvcGmkaYTpc44hd2ZiTVXrNU8zKGmwIHj1cYFvKE2FRkegZ4VtdHNiYYPz[ZN{\WRiYYOg[IVkemWjc3WgbY4hTVKNIIDoc5NxcG:{eXzheIlwdiCjZoTldkA4PSCvaX7zJIJ6KFenc4Tldo4h[myxdITpcoch[W6jbInzbZM> NInpNZMzOzN7OES1Ny=>

... 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
  • 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
Smiles OCC(O)CONC(=O)C1=C(NC2=CC=C(I)C=C2F)C(=C(F)C=C1)F

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  • 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

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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/

selleck catalog

MEK Signaling Pathway Map

MEK Inhibitors with Unique Features

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  • BI-847325 New

    BI-847325 is an orally bioavailable, and selective dual MEK/Aurora kinase inhibitor with IC50 of 3 nM, 25 nM, 15 nM, 25 nM, and 4 nM for Xenopus laevis Aurora B, human Aurora A and Aurora C, as well as human MEK1 and MEK2, respectively. Phase 1.

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  • Trametinib (GSK1120212)

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    Features:More potent than PD0325901 or AZD6244.

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    PD98059 is a non-ATP competitive MEK inhibitor with IC50 of 2 μM in a cell-free assay, specifically inhibits MEK-1-mediated activation of MAPK; does not directly inhibit ERK1 or ERK2.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID