PD0325901

PD0325901は選択的です、そして、非ATP競争的有糸分裂促進物質はMEK活動のinhibitonのためにプロテインキナーゼ・キナーゼ(MEKまたはMAPKK)MEK阻害剤を起動させました。IC50 が 0.33 nMになる。

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PD0325901 化学構造
分子量: 482.19

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製品説明

  • Compare MEK Inhibitors
    MEK製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 PD0325901は選択的です、そして、非ATP競争的有糸分裂促進物質はMEK活動のinhibitonのためにプロテインキナーゼ・キナーゼ(MEKまたはMAPKK)MEK阻害剤を起動させました。IC50 が 0.33 nMになる。
ターゲット

MEK

IC50

0.33 nM [1]

In vitro試験 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
human CHP-212 cell NVLWO4VXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{\ofWlvcGmkaYTpc44hd2ZiaIXtZY4hS0iSLUKxNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPTJ5IH7NMi=> MYfTRW5ITVJ?
human M14 cell MnXMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV;Jcohq[mm2aX;uJI9nKGi3bXHuJG0yPCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNEWgcm0v M4jzNHNCVkeHUh?=
human SK-MEL-28 cell MnX6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NI\2UHZKdmirYnn0bY9vKG:oIHj1cYFvKFONLV3FUE0zQCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFwNUKgcm0v NU\URYRDW0GQR1XS
human NOMO-1 cell Mo\XS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3zCSWlvcGmkaYTpc44hd2ZiaIXtZY4hVk:PTz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk4xPyCwTT6= M4jBNXNCVkeHUh?=
human A375 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYDJcohq[mm2aX;uJI9nKGi3bXHuJGE{PzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{Lk[5JI5ONg>? M4fsW3NCVkeHUh?=
human DU-4475 cell NYrHUYl6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUnJcohq[mm2aX;uJI9nKGi3bXHuJGRWNTR2N{WgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlU4KG6PLh?= Mn30V2FPT0WU
human C32 cell MmDyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWLJcohq[mm2aX;uJI9nKGi3bXHuJGM{OiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNwNkegcm0v M4XnXnNCVkeHUh?=
human BPH-1 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIXWSINKdmirYnn0bY9vKG:oIHj1cYFvKEKSSD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{46PSCwTT6= NYHzcXhrW0GQR1XS
human CP50-MEL-B cell NWfXOGZmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYqxVno{UW6qaXLpeIlwdiCxZjDoeY1idiCFUEWwMW1GVC2EIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;ND61PEBvVS5? M2D4[nNCVkeHUh?=
human H9 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXfJcohq[mm2aX;uJI9nKGi3bXHuJGg6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PS55NzDuUU4> NXnheGp[W0GQR1XS
human HTC-C3 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUTUS3BwUW6qaXLpeIlwdiCxZjDoeY1idiCKVFOtR|Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njh7IH7NMi=> NEPnbmlUSU6JRWK=
human BHT-101 cell NEXQ[25Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX\0OG5KUW6qaXLpeIlwdiCxZjDoeY1idiCESGStNVAyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi55IH7NMi=> Mm\5V2FPT0WU
human COLO-741 cell NHnTb|hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3mxRmlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz23OFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04NjFibl2u M4HwfXNCVkeHUh?=
human OVCAR-5 cell M4qxNWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mnm5TY5pcWKrdHnvckBw\iCqdX3hckBQXkODUj21JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O{45OiCwTT6= Ml\1V2FPT0WU
human A549 cell NHTRR4xIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2SzcGlvcGmkaYTpc44hd2ZiaIXtZY4hSTV2OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUeuPFkhdk1w MXPTRW5ITVJ?
human SH-4 cell growth MmXFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXnLW|d[UW6qaXLpeIlwdiCxZjDoeY1idiCVSD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PE4zPiCwTT6= M3XXOXNCVkeHUh?=
human SK-N-AS cell NUS3XVRnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkSyTY5pcWKrdHnvckBw\iCqdX3hckBUUy2QLVHTJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PE41PCCwTT6= NHvNSpZUSU6JRWK=
human HT-144 cell NVfQWoJzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYHJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTF2NDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUiuPVchdk1w NUjxbFBFW0GQR1XS
human MEL-HO cell MlzKS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlS3TY5pcWKrdHnvckBw\iCqdX3hckBOTUxvSF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlQ6KG6PLh?= MlfNV2FPT0WU
human COLO-679 cell M3;xTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEPMb4NKdmirYnn0bY9vKG:oIHj1cYFvKEORTF:tOlc6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTBwMEGgcm0> MXHTRW5ITVJ?
human HuP-T4 cell Mn7oS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkfPTY5pcWKrdHnvckBw\iCqdX3hckBJfVBvVESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE46QCCwTT6= M2f0cXNCVkeHUh?=
human H-EMC-SS cell M{XwOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NU[3d|BkUW6qaXLpeIlwdiCxZjDoeY1idiCKLVXNR{1UWyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFzLkCyJI5ONg>? M4HxRnNCVkeHUh?=
human LB2518-MEL cell NIOzSJdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYrJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjVzOD3NSWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS5zMzDuUU4> MlrmV2FPT0WU
human HL-60 cell MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1e4dmlvcGmkaYTpc44hd2ZiaIXtZY4hUExvNkCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNU4yPSCwTT6= MWnTRW5ITVJ?
human NCI-H1666 cell M3;jRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYfBRoljUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PjZiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMT6xO{BvVS5? MXHTRW5ITVJ?
human A101D cell MXrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1Xi[GlvcGmkaYTpc44hd2ZiaIXtZY4hSTFyMVSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNU41PSCwTT6= M2nUdXNCVkeHUh?=
human RVH-421 cell NEmxbHBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3TwNmlvcGmkaYTpc44hd2ZiaIXtZY4hWl[KLUSyNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjZ2IH7NMi=> MVXTRW5ITVJ?
human Hs-578-T cell NFfOT4JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlzxTY5pcWKrdHnvckBw\iCqdX3hckBJey13N{itWEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEzNjd7IH7NMi=> NVLBUpFyW0GQR1XS
human A375 cells Mn32VJJwdGmoZYLheIlwdiCjc4PhfS=> NILGR2U4OiCq M2XISmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OUBk\WyuczDlfJBz\XO|aX7nJGJTSUZiVk[wNGUhdXW2YX70JIFnfGW{IEeyJIhzeyCkeTDD[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3ME2xN{BvVS5? MkTlNlM1PzR|OEi=
human DOK cell NVLodHZ7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4qzTmlvcGmkaYTpc44hd2ZiaIXtZY4hTE:NIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuOEBvVS5? NHK5TYpUSU6JRWK=
human Mewo cell M2PPcmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mm\RTY5pcWKrdHnvckBw\iCqdX3hckBO\XexIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUSuOFUhdk1w NInyZmJUSU6JRWK=
human ONS-76 cell M{PNPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHrFPYdKdmirYnn0bY9vKG:oIHj1cYFvKE:QUz23OkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjVzIH7NMi=> NGXBN|lUSU6JRWK=
human UACC-257 cell MkX6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmDnTY5pcWKrdHnvckBw\iCqdX3hckBWSUOFLUK1O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE1NjZ{IH7NMi=> NIT1U45USU6JRWK=
human SW626 cell MkDQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmP3TY5pcWKrdHnvckBw\iCqdX3hckBUXzZ{NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG0MlkyKG6PLh?= M1n0bXNCVkeHUh?=
human SW620 cell NY\ZU2FoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF61elNKdmirYnn0bY9vKG:oIHj1cYFvKFOZNkKwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVQvQTVibl2u MoGzV2FPT0WU
human TYK-nu cell M{WySWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmDvTY5pcWKrdHnvckBw\iCqdX3hckBVYUtvboWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOU4yOyCwTT6= NELhdndUSU6JRWK=
human ACN cell MonvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{fuWmlvcGmkaYTpc44hd2ZiaIXtZY4hSUOQIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUWuO|Yhdk1w NW\rdplPW0GQR1XS
human MIAPaCa2 cells MoDyVJJwdGmoZYLheIlwdiCjc4PhfS=> NIHGcIZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3JRXBiS2F{IHPlcIx{NCCLQ{WwQVE4KG6PLh?= NYfFOY1TOjN2N{SzPFg>
human T-24 cell NWjGb4ptT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYLJcohq[mm2aX;uJI9nKGi3bXHuJHQuOjRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zOT63NUBvVS5? MlHmV2FPT0WU
human AGS cell MkK0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlLBTY5pcWKrdHnvckBw\iCqdX3hckBCT1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{MD60NUBvVS5? MUPTRW5ITVJ?
human SW872 cell NFXiR4VIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUPJcohq[mm2aX;uJI9nKGi3bXHuJHNYQDd{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkeuPVkhdk1w MW\TRW5ITVJ?
human C2BBe1 cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NULpV4FwUW6qaXLpeIlwdiCxZjDoeY1idiCFMlLC[VEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zQC53NDDuUU4> Ml\6V2FPT0WU
human MZ7-mel cell NVr1XGxGT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1LZUGlvcGmkaYTpc44hd2ZiaIXtZY4hVVp5LX3lcEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI6NjR|IH7NMi=> NIL0VFBUSU6JRWK=
human HCC2998 cell MnrFS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGLnPIxKdmirYnn0bY9vKG:oIHj1cYFvKEiFQ{K5PVgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Oy54NjDuUU4> M1frPHNCVkeHUh?=
human HO-1-N-1 cell MnvES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NY\ZWWFmUW6qaXLpeIlwdiCxZjDoeY1idiCKTz2xMW4uOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN2LkSzJI5ONg>? NEHidG9USU6JRWK=
human SW756 cell M2LXWmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3uyN2lvcGmkaYTpc44hd2ZiaIXtZY4hW1d5NU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOE41PSCwTT6= NVjKT3RxW0GQR1XS
human NCI-H1437 cell M{XrS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGPHVI1KdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVQ{PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN2LkS5JI5ONg>? NHzwcpFUSU6JRWK=
human NCI-H747 cell MmrzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnXkTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEe0O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM1Njl6IH7NMi=> MkXpV2FPT0WU
human SK-MEL-2 cell Mn35S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXLJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|UvOiCwTT6= MnT5V2FPT0WU
human MZ2-MEL cell NFXzWVVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn7iTY5pcWKrdHnvckBw\iCqdX3hckBOYjJvTVXMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|UvPjVibl2u Mnu5V2FPT0WU
human PSN1 cell NUjadFFFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX6wcYxiUW6qaXLpeIlwdiCxZjDoeY1idiCSU16xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|gvPDVibl2= NVz3Tmd[W0GQR1XS
human CAL-39 cell M1PzO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFXiTmhKdmirYnn0bY9vKG:oIHj1cYFvKEODTD2zPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM6NjB2IH7NMi=> NXjnZYJlW0GQR1XS
human LOXIMVI cell M3vwT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mlu4TY5pcWKrdHnvckBw\iCqdX3hckBNV1iLTW\JJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|kvOzlibl2u NFLrN5RUSU6JRWK=
human COLO-792 cell NE\aN|JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1:xOWlvcGmkaYTpc44hd2ZiaIXtZY4hS0:OTz23PVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01Oy5zNTDuUU4> M3PXTHNCVkeHUh?=
human CAL-27 cell M1zxOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEjifnBKdmirYnn0bY9vKG:oIHj1cYFvKEODTD2yO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ1NjlzIH7N MULTRW5ITVJ?
human AsPC-1 cell NH7HO|NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFmxNZpKdmirYnn0bY9vKG:oIHj1cYFvKEG|UFOtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ2NjJ6IH7NMi=> MmHOV2FPT0WU
human NCI-H2291 cell NH7MTXJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWnJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkK5NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ3NjR4IH7NMi=> NH7kOlFUSU6JRWK=
human RCM-1 cell NVnMfXhDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEC1N4JKdmirYnn0bY9vKG:oIHj1cYFvKFKFTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFYvQDVibl2u Mlm2V2FPT0WU
human NCI-H292 cell M2XLO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVTJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkmyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFcvOzlibl2u MWjTRW5ITVJ?
human WM-115 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlnmTY5pcWKrdHnvckBw\iCqdX3hckBYVS1zMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20PE42KG6PLh?= M1q0ZnNCVkeHUh?=
human RT-112 cell NWL4V29ST3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXLJcohq[mm2aX;uJI9nKGi3bXHuJHJVNTFzMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS4Mlg1KG6PLh?= NHy0cJRUSU6JRWK=
human HT-29 cell M3vUbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV\nOpJkUW6qaXLpeIlwdiCxZjDoeY1idiCKVD2yPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUxNjR7IH7NMi=> MoXBV2FPT0WU
human RKO cell growth NXjmNGZOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWPJcohq[mm2aX;uJI9nKGi3bXHuJHJMVyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTV{LkCyJI5ONg>? M4nJRXNCVkeHUh?=
human KY821 cell M{SwfWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF;Qd|RKdmirYnn0bY9vKG:oIHj1cYFvKEu\OEKxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OVMvOyCwTT6= Ml7uV2FPT0WU
human LB1047-RCC cell M3n2NWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NE\IboNKdmirYnn0bY9vKG:oIHj1cYFvKEyEMUC0O{1TS0NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD13OT62OUBvVS5? NVHYUIhPW0GQR1XS
human SW1116 cell MmHhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHrPNnFKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUGxOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYxNjR7IH7NMi=> NV2yfZY5W0GQR1XS
human P12-ICHIKAWA cell NGjubHpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4TP[mlvcGmkaYTpc44hd2ZiaIXtZY4hWDF{LVnDTGlMSVeDIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NkKuNlchdk1w NVrYZVlzW0GQR1XS
human HCC70 cell MnLzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXfJcohq[mm2aX;uJI9nKGi3bXHuJGhESzdyIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;NkOuNFEhdk1w NFvGVHRUSU6JRWK=
human MIA-PaCa-2 cell M{DGRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlziTY5pcWKrdHnvckBw\iCqdX3hckBOUUFvUHHDZU0zKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PjNwNUOgcm0v M3jQfHNCVkeHUh?=
human LoVo cell NFjGWoZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3LPW2lvcGmkaYTpc44hd2ZiaIXtZY4hVG:YbzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[1MlI6KG6PLh?= NUnTVoNjW0GQR1XS
human LB2241-RCC cell M4n3U2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml7ITY5pcWKrdHnvckBw\iCqdX3hckBNSjJ{NEGtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PjVwNUKgcm0v MkD1V2FPT0WU
human GAK cell MkXjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NW\xR29DUW6qaXLpeIlwdiCxZjDoeY1idiCJQVugZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME22Ok45PyCwTT6= NEHSPJBUSU6JRWK=
human RD cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoLpTY5pcWKrdHnvckBw\iCqdX3hckBTTCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZ5LkGgcm0v NGS1[IpUSU6JRWK=
human KNS-62 cell NXfLUI9YT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVHNUIZEUW6qaXLpeIlwdiCxZjDoeY1idiCNTmOtOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03QS57OTDuUU4> NGjCelFUSU6JRWK=
human HD-MY-Z cell Mme0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGHDRoxKdmirYnn0bY9vKG:oIHj1cYFvKEiGLV3ZMXoh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04OS5zMjDuUU4> M4rlOXNCVkeHUh?=
human COR-L105 cell NETieY5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlzOTY5pcWKrdHnvckBw\iCqdX3hckBEV1JvTEGwOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcyNjdzIH7NMi=> NWjTN4NiW0GQR1XS
human IA-LM cell NEPOSpVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmftTY5pcWKrdHnvckBw\iCqdX3hckBKSS2OTTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUezMlI5KG6PLh?= M{TQXXNCVkeHUh?=
human EM-2 cell NXPzRoV1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXvJcohq[mm2aX;uJI9nKGi3bXHuJGVONTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD15ND63JI5ONg>? MXHTRW5ITVJ?
human NB69 cell NFrtVHpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWHoOGFkUW6qaXLpeIlwdiCxZjDoeY1idiCQQk[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZk> MW\TRW5ITVJ?
human HuP-T3 cell M1XTemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYfJcohq[mm2aX;uJI9nKGi3bXHuJGh2WC2WMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUizMlk{KG6PLh?= NE\hN5ZUSU6JRWK=
human BB30-HNC cell NX\we|drT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYLNOWJ1UW6qaXLpeIlwdiCxZjDoeY1idiCEQkOwMWhPSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTh3LkWxJI5ONg>? NIrD[nJUSU6JRWK=
human HT-1080 cell NH:3NFRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkLVTY5pcWKrdHnvckBw\iCqdX3hckBJXC1zMEiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PFUvQDhibl2u NXrkTG5zW0GQR1XS
human RMG-I cell NIH4TVBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2iy[WlvcGmkaYTpc44hd2ZiaIXtZY4hWk2JLVmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24O{4{PCCwTT6= NEHXXXhUSU6JRWK=
human HCC1419 cell NVfSbZVqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mk\jTY5pcWKrdHnvckBw\iCqdX3hckBJS0NzNEG5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVEvOzhibl2u Mn33V2FPT0WU
human SW780 cell NVG3OI9oT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGjrXnJKdmirYnn0bY9vKG:oIHj1cYFvKFOZN{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVIvOzJibl2u NX;JPZlmW0GQR1XS
human SNU-387 cell NILlcoFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn\VTY5pcWKrdHnvckBw\iCqdX3hckBUVlVvM{i3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PVMvOzZibl2= MXvTRW5ITVJ?
human LAMA-84 cell MknLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHTHSmVKdmirYnn0bY9vKG:oIHj1cYFvKEyDTVGtPFQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06PC54ODDuUU4> MXfTRW5ITVJ?
human MV-4-11 cell M1HzSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXzJcohq[mm2aX;uJI9nKGi3bXHuJG1XNTRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25OE44OyCwTT6= MWLTRW5ITVJ?
human EGI-1 cell M3vrcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Ml7VTY5pcWKrdHnvckBw\iCqdX3hckBGT0lvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUm1MlgyKG6PLh?= NV;aZ5hHW0GQR1XS
human NCI-SNU-1 cell NHPEOWVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1nldmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLWPOWU0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QTZwN{Ogcm0v MmnBV2FPT0WU
human MEG-01 cell Mm\xS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVzpfFlFUW6qaXLpeIlwdiCxZjDoeY1idiCPRVetNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06Py55NzDuUU4> MkjwV2FPT0WU
human OMC-1 cell NXrt[oZtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn23TY5pcWKrdHnvckBw\iCqdX3hckBQVUNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwNE4zOyCwTT6= M{nofXNCVkeHUh?=
human NB10 cell MofES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3r5NGlvcGmkaYTpc44hd2ZiaIXtZY4hVkJzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwNE41OiCwTT6= MW\TRW5ITVJ?
human CAL-62 cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3viNWlvcGmkaYTpc44hd2ZiaIXtZY4hS0GOLU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAxNjd6IH7NMi=> NXLWcHRLW0GQR1XS
human NCI-H2087 cell NFK5W3NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWPJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkC4O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExOS5zNDDuUU4> NWHqU4tQW0GQR1XS
human MDA-MB-175-VII cell NWD3fGE6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVnpcGlkUW6qaXLpeIlwdiCxZjDoeY1idiCPRFGtUWIuOTd3LW\JTUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6 MlzBV2FPT0WU
human LS-513 cell NFnBdphIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGrmXlBKdmirYnn0bY9vKG:oIHj1cYFvKEyVLUWxN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyPC56MzDuUU4> MojVV2FPT0WU
human HN cell growth NWHvcnNIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGhPKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTJ{LkW5JI5ONg>? MVXTRW5ITVJ?
human ABC-1 cell MmXnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3fwXGlvcGmkaYTpc44hd2ZiaIXtZY4hSUKFLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNlMvODJibl2u MX7TRW5ITVJ?
human SJSA-1 cell NIm1bmVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoK5TY5pcWKrdHnvckBw\iCqdX3hckBUUlODLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNlMvOTlibl2u NFHnOpZUSU6JRWK=
human PANC1 cells MVPGeY5kfGmxbjDhd5NigQ>? M4DudVExKM7:TR?= NXTkR29iOSCq M{n1fmlvcGmkaYTpc44hd2ZiTVXLNUBqdiCqdX3hckBRSU6FMTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4heEW{a{GvNkBt\X[nbDDheEAyOCC3TTDh[pRmeiBzIHjyJIJ6KFenc4Tldo4h[myxdITpcoch[W6jbInzbZM> NX7VfHY3OjV5Nk[2N|M>
human MCF7 cells M1HzeWZ2dmO2aX;uJIF{e2G7 NUG2ZXpiPzVibXnudy=> NUDyWGtLUW6qaXLpeIlwdiCxZjDNSYsyNzJiaX6gbJVu[W5iTVPGO{Bk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCHUlugdIhwe3Cqb4L5cIF1cW:wIHHmeIVzKDd3IH3pcpMh[nliV3XzeIVzdiCkbH;0eIlv\yCjbnHsfZNqew>? NGPBbZkzOzN7OES1Ny=>

... Click to View More Cell Line Experimental Data

In vivo試験 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]
臨床試験 Combined with PF-04691502/PF-05212384/CPT-11, PD-0325901 is currently in Phase I clinical trial for advanced cancer.
特集

プロトコル (参考用のみ)

キナーゼアッセイ:

[1]

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.

細胞アッセイ:

[3]

細胞株 PTC cells
濃度 0.1 nM- 1 μM
反応時間 48 hours
実験の流れ

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.

動物実験:

[3]

動物モデル Ncr-nu/nu mice bearing PTC cells
製剤 80 mM citric buffer (pH 7)
投薬量 20-25 mg/kg
投与方法 Oral gavage

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download PD0325901 SDF
分子量 482.19
化学式

C16H14F3IN2O4

CAS No. 391210-10-9
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 96 mg/mL (199.09 mM)
Ethanol 40 mg/mL (82.95 mM)
Water <1 mg/mL
In vivo 30% PEG 400+5% Tween 80+ddH2O 10mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
化学名 (R)-N-(2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodophenylamino)benzamide

文献中の引用 (89)

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/

技術サポート&よくある質問(FAQ)

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    BI-847325は一種の経口生物利用可能で、選択性的な二重MEK/オーロラキナーゼ阻害剤です。BI-847325はアフリカツメガエル(Xenopus laevis)オーロラB、人間オーロラAとオーロラC、及び人間MEK1とMEK2に作用する時のIC50値が3 nM、25 nM、15 nM、25 nMと4 nMそれぞれに分かれます。臨床1期。

  • GDC-0623

    GDC-0623は1種の有効的で、 ATP非競争性のMEK1阻害剤で、 Ki値は0.13 nMです。臨床1期。

  • GDC-0994

    GDC-0994 is a potent, orally available ERK1/2 inhibitor. Phase 1.

  • Trametinib (GSK1120212)

    Trametinib (GSK1120212)は、非常に特定で有力なMEK1MEK2 阻害剤で、IC50 がそれぞれ 0.92 nM と 1.8 nMです。

    Features:More potent than PD0325901 or AZD6244.

  • Selumetinib (AZD6244)

    Selumetinib (AZD6244) は有効的にMEK1を抑制して、IC50 が14 nMになる.

    Features:First MEK inhibitor being tested in Phase II clinical trials.

  • U0126-EtOH

    U0126-EtOH は化学的に合成されて非常に選択的な阻害剤で、MEK1 とMEK2 に作用すると、 IC50 がそれぞれ0.07 μM と 0.06 μMになる。

    Features:A chemically synthesized and highly selective inhibitor of both MEK1 and MEK2.

  • PD98059

    PD98059は、非競争的MEK</bです> 阻害剤で、IC50 が2 μMです.

    Features:Does not inhibit c-Raf phosphorylated MEK1.

  • PD184352 (CI-1040)

    PD184352 (CI-1040)は、ATP非競争MEK1/2阻害剤で、IC50 が 17 nMです。

    Features:First MEK inhibitor to begin clinical development.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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