PD98059

For research use only. Not for use in humans.

目录号:S1177

PD98059 Chemical Structure

CAS No. 167869-21-8

PD98059 是一种非ATP竞争性的MEK抑制剂,无细胞试验中IC50为2 μM,特异性抑制MEK-1介导的MAPK激活;不直接抑制ERK1或ERK2。PD98059 是一种aryl hydrocarbon receptor (AHR)的配体并起到拮抗剂的功能。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1099.68 现货
RMB 1213.08 现货
RMB 3845.73 现货
RMB 5489.52 现货
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客户使用Selleck生产的PD98059发表文献386篇:

产品安全说明书

MEK抑制剂选择性比较

生物活性

产品描述 PD98059 是一种非ATP竞争性的MEK抑制剂,无细胞试验中IC50为2 μM,特异性抑制MEK-1介导的MAPK激活;不直接抑制ERK1或ERK2。PD98059 是一种aryl hydrocarbon receptor (AHR)的配体并起到拮抗剂的功能。
特性 PD98059不会抑制已经被c-Raf磷酸化的 MEK1
靶点
AhR [1]
(Cell-free assay)
MEK1 [1]
(Cell-free assay)
1 μM 2 μM
体外研究

PD98059 要么抑制本底的MEK1,要么抑制一种被部分激活的MEK突变体,该突变体是 218 和 222号位上丝氨酸突变为谷氨酸后形成的(MEK-2E), IC50 为2 μM. PD98059 不会抑制JNK和P38这两个 MAPK 的同系物. PD98059会高度选择性的抑制MEK, 因为对其它包括Raf 激酶, cAMP-依赖性激酶, 蛋白激酶C, v-Src, 表皮生长因子 (EGF) 受体激酶, 胰岛素受体激酶, PDGF 受体激酶, 和磷脂酰肌醇(-3)激酶等在内的一系列激酶都没有抑制性。 PD98059 会抑制经过PDGF刺激而活化的MAPK 和胸苷 进入 3T3 细胞, IC50分别为 ~10 μM 和 ~7 μM [1]。PD98059可以有效地阻止 MEK1 被Raf 或者MEK 激酶活化, IC50为4 μM, 可以微弱地 抑制MEK2被 Raf 活化, IC50 为50 μM。 在KB 和 PC12 细胞中, PD98059 不会抑制MKK4 和RK激酶这两个参与压力和白细胞介素-1介导的激酶级联反应的MEK的同系物的活化,在Swiss 3T3 细胞中也不会通过胰岛素或者表皮生长因子抑制p70 S6 激酶的活化[2]。PD98059会在不改变细胞生存能力的情况下完全阻断 神经生长因子(NGF)诱导的 PC12 细胞的分化[3] 。PD98059会以剂量依赖性的方式抑制培养在含有破骨细胞分化因子培养基中的 RAW264.7细胞的增值,进而导致TRAP阳性细胞数量明显下降[6]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A2780  M4TMXGZ2dmO2aX;uJGF{e2G7 M1P1d|IxyqEQvF2= M1v6dlEhcA>? NFTMOIljdG:la4OgSHRETC2rbnT1Z4VlKESUNTDlfJBz\XO|aX;u NWDX[Xk5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2PVY5PjJpPkKzOlk3QDZ{PD;hQi=>
AML 1# M4rN[mFxd3C2b4Ppd{BCe3OjeR?= MUCyNOKh|ryP NHj6fGwyOiCq NV60WoJP\W6qYX7j[ZMh[2WubDDhdI9xfG:|aYOgbY5lfWOnZDDifUBUOQ>? NGXTSlI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{ewOlY6OSd-MkO3NFY3QTF:L3G+
KG-1  M2[xbGFxd3C2b4Ppd{BCe3OjeR?= NHfXcG8zOMLizszN M4fyeFEzKGh? MYrlcohidmOnczDj[YxtKGGyb4D0c5NqeyCrbnT1Z4VlKGK7IGOx MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzdyNk[5NUc,OjN5ME[2PVE9N2F-
HUVECs NIrvPZJCeG:ydH;zbZMhSXO|YYm= NUXPcnpyOi92IN88US=> M{izTlI1NzR6IHi= M3GzRYlv\HWlZYOgZ4VtdCCmZXH0bC=> M3L2c|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{C3OVIxLz5{M{ewO|UzODxxYU6=
HepG2  M1LyZmZ2dmO2aX;uJGF{e2G7 MXOyNOKh|ryP MWWyOEBp MYDpcohq[mm2czD0bIUhUE9vMTDwdo91\WmwIHX4dJJme3Orb36gZ48ufHKnYYTl[EB4cXSqIH3leIZwem2rbh?= MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzdyN{[wPUc,OjN5MEe2NFk9N2F-
NB4  NH;Rd3hCeG:ydH;zbZMhSXO|YYm= MlG1NVAwOjBxNkCg{txO MoTPNU42KGh? NVy2VHRYTE2VTx?= NVf0T5Js\GWlcnXhd4V{KGOnbHygeoli[mmuaYT5JINwNXS{ZXH0[YQhf2m2aDDQZYNtcXSjeHXs NGHEbWo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{ezOVU1OSd-MkO3N|U2PDF:L3G+
BxPC-3 cells NXrYUmc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\2N|IxyqEQvF2= NIXmOGgxNjViaB?= M4K3dIlvcGmkaYTzJHZGT0ZvQT3y[Yd2dGG2ZXSgTHVXTUNiZ4Lve5RpKGGwZDD0eYJmKG[xcn3heIlwdiCrbnT1Z4VlKGK7IGDBVk0zKEGS M1fKXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{[0NFQ3Lz5{M{e2OFA1PjxxYU6=
MKN45 MnmxRZBweHSxc3nzJGF{e2G7 NFjCWo8yOCEQvF5CpC=> Mn7PNlQhcA>? MVLpcoNz\WG|ZYOgeIhmKESDUGStbY5lfWOnZDDj[YxtKGGyb4D0c5Nqew>? MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzd7MkW4PEc,OjN5OUK1PFg9N2F-
SGC7901 Mnj6RZBweHSxc3nzJGF{e2G7 Ml3CNVAh|ryPwrC= M4m1W|I1KGh? MkXNbY5kemWjc3XzJJRp\SCGQWDUMYlv\HWlZXSgZ4VtdCCjcH;weI9{cXN? MlPDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN5OUK1PFgoRjJ|N{myOVg5RC:jPh?=
MKN45 MoXISpVv[3Srb36gRZN{[Xl? MXGxNEDPxE4EoB?= MlnRNlQhcA>? M2rCcolvcGmkaYTzJJRp\SCneIDy[ZN{cW:wIH;mJJBpd3OyaH;yfYxifGWmIFXST|EwOg>? NFn0T4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlU5QCd-MkO3PVI2QDh:L3G+
SGC7901 MlnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPYR2syOCEQvF5CpC=> NYPzVJdrOjRxNEivO|IhcA>? M{LlPYlvcGmkaYTzJINmdGxiZ4Lve5RpKGOxLYTy[YF1\WRid3n0bEBFSVCW NXTtV49kRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO3PVI2QDhpPkKzO|kzPTh6PD;hQi=>
MKN45 NEm0blZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XSd|ExKM7:TdMg NUDwNXVDOjRxNEivO|IhcA>? MVPpcohq[mm2czDj[YxtKGe{b4f0bEBkdy22cnXheIVlKHerdHigSGFRXA>? NFzYUpg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlU5QCd-MkO3PVI2QDh:L3G+
SGC7901 Mnf1SpVv[3Srb36gRZN{[Xl? NFX6eIoyOCEQvF5CpC=> M1nVNlI1KGh? MXjpcohq[mm2czD0bIUh\XiycnXzd4lwdiCxZjDwbI9{eGixconsZZRm\CCHUluxM|I> NITMc|Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{e5NlU5QCd-MkO3PVI2QDh:L3G+
HUASMCs MVPGeY5kfGmxbjDBd5NigQ>? Mof0NVAh|ryPwrC= MUOyOEBp NYG1PG13\GmvaX7pd4hmeyCDbnegTWku[2G3c3XkJHNQS1N|IH3SUmEh[W6mIIDyc5RmcW5iZYjwdoV{e2mxbtMg NY\FdmtYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO4NVY1PjhpPkKzPFE3PDZ6PD;hQi=>
HUASMCs NWHV[lQ{TnWwY4Tpc44hSXO|YYm= MYSxNEDPxE4EoB?= M2rLZlI1KGh? MVrpcohq[mm2czDBcochUUlvaX7keYNm\CCHUluxM|IheGixc4Doc5J6dGG2aX;uJIxmfmWu MmjEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6MU[0OlgoRjJ|OEG2OFY5RC:jPh?=
EPOR/CR3 NYi1SJdbTnWwY4Tpc44hSXO|YYm= NVziSpFUPTEEoN88US=> MVyzJIg> MmKwdoVlfWOnczDFVG8h[W6mL3;yJGlNNTNvaX7keYNm\CC2aHWgeJlzd3OrbnWgdIhwe3Cqb4L5cIF1cW:wwrC= M{K0SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|OEKwO|MyLz5{M{iyNFc{OTxxYU6=
NB4  NV36VGhJTnWwY4Tpc44hSXO|YYm= MYKxNEDPxE4EoB?= NELxeYg4OiCq M3ryNGROW09? NFfidFdqdmirYnn0d{Bl[XOjdHnubYIucW6mdXPl[EBETDFzYjDlfJBz\XO|aX;u NHyzb5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{iyOVU5PSd-MkO4NlU2QDV:L3G+
HL60  NX3IRndTTnWwY4Tpc44hSXO|YYm= M2HTZVIxyqEQvF2= MkizO|IhcA>? MoHQSG1UVw>? M3TYeYlvcGmkaYTzJIRie2G2aX7pZk1qdmS3Y3XkJGNFOTGkIHX4dJJme3Orb36= NHTZVo49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{iyOVU5PSd-MkO4NlU2QDV:L3G+
HUVECs MWHGeY5kfGmxbjDBd5NigQ>? NW\MeFVMOjVizszN NXm4elJpOSCq MonsbY5kemWjc3WgUmYu|rqEIIC2OUBvfWOuZXHyJJRz[W6|bH;jZZRqd25? MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzlyMUCwPEc,OjN7MEGwNFg9N2F-
LNCaP  Mn\RSpVv[3Srb36gRZN{[Xl? NVL4OYtTOTBizszNxsA> MlrYNUBp M2XyZYRm[3KnYYPld{B1cGViRVfGJJVxemWpdXzheIVlKHBvWVKtNS=> MkfkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN6M{izNVgoRjJ|OEO4N|E5RC:jPh?=
HL-60 NWfucmk4SXCxcITvd4l{KEG|c3H5 NYPIbJJ7PTEEoN88US=> M4Ht[VEhcA>? NIHHVVJz\XOldXXzJGJCOTR3IH3l[IlifGWmIHHwc5B1d3Orcx?= NETydog9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m0PFc2OSd-MkO5OFg4PTF:L3G+
HepG2 MnfESpVv[3Srb36gRZN{[Xl? NF[wNXg1OCEQvF2= NGnmfnA3NzF{IHi= MkD6bY5pcWKrdIOgeIhmKGmwY4LlZZNmKG:oIICtSXJMOSCjbnSgdE1kNUq3bjDwdo91\WmwIHX4dJJme3Orb36gZpkhWEx? NXvhbWZ2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5OFI5PTFpPkKzPVQzQDVzPD;hQi=>
HPAF-II MXnGeY5kfGmxbjDBd5NigQ>? MnfhNVAh|ryPwrC= M{PGVFYhcA>? NX7PfGJXcW6lcnXhd4UhdWmULUG0N{BmgHC{ZYPzbY9v MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzl5M{exNEc,OjN7N{O3NVA9N2F-
BxPC-3 M33PO2Z2dmO2aX;uJGF{e2G7 NVfPU2huOTBizszNxsA> NVPUfnk1PiCq M1ntTolv[3KnYYPlJI1qWi1zNEOg[ZhxemW|c3nvci=> Mo[yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7N{O3NVAoRjJ|OUezO|ExRC:jPh?=
COLO205 M2jWU2Fxd3C2b4Ppd{BCe3OjeR?= NET5XpYyOC9{MD:0NEDPxE1? NXKxdIxoOjRiaB?= MkfnbY5lfWOnczDEUmEhdGGmZHXyJIZwem2jdHnvci=> NX;wXnlZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNVkyODhpPkK0NFE6OTB6PD;hQi=>
G292  NUXiZml5SXCxcITvd4l{KEG|c3H5 MX[zNOKh|ryP MlrqNkBp NYPY[5pMemW|dH;y[ZMh[2Gyc3HpZ4lvNWmwZIXj[YQh[2WubDDk[YF1cA>? MoXzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyMUK5N|AoRjJ2MEGyPVMxRC:jPh?=
SGC7901 NUTHTplOSXCxcITvd4l{KEG|c3H5 NYHzVZROOjEEoN88US=> NVKwPZVvOSCq MmrNbY5pcWKrdIOgZZBweHSxc3nzJIlv\HWlZXSgZpkhUU[QLd8xxsBidmRiNfMAtk1FTlWU NWXNW4F[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwNlc4PTBpPkK0NFI4PzVyPD;hQi=>
MGC803  NYD1[nRnSXCxcITvd4l{KEG|c3H5 NWXPV|VlOjEEoN88US=> MXyxJIg> NVPaXmp6cW6qaXLpeJMh[XCxcITvd4l{KGmwZIXj[YQh[nliSV\OMe6yyqCjbnSgOgKBui2GRmXS MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB{N{e1NEc,OjRyMke3OVA9N2F-
HPMC MXPBdI9xfG:|aYOgRZN{[Xl? MYCxNOKh|ryP MXeyOOKhcA>? M3;pOJJmfmW{c3XzJIRm[3KnYYPlJIlvKGOnbHygeoli[mmuaYT5JIlv\HWlZXSgZpkhUEeSRGO= Mm\0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNEK4N|goRjJ2MESyPFM5RC:jPh?=
HCT-8 MmDZRZBweHSxc3nzJGF{e2G7 MonNNVDDqM7:TR?= MnrqNlTDqGh? Mkj4[IVkemWjc3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgOU1HXQ>? MnztQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyOUW4OlMoRjJ2MEm1PFY{RC:jPh?=
HPMC NWXYU4JLTnWwY4Tpc44hSXO|YYm= M4HlO|ExyqEQvF2= MoTQOFghcA>? NYLqSWNKemW4ZYLz[ZMhfGinIHPoZY5o\XNiaX6gZ4VtdCCvb4LwbI9td2e7IHnu[JVk\WRiYomgTGdRTFN? MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDB2MkizPEc,OjRyNEK4N|g9N2F-
A549 MUnGeY5kfGmxbjDBd5NigQ>? NHfaNW02OMLizszN NXjwVoJWOiCq MlXOZoxw[2u|IFXST{BxcG:|cHjvdplt[XSrb36gcYVlcWG2ZXSgZpkhOSx{LV7R NVXsZZRURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSwOlc4OjdpPkK0NFY4PzJ5PD;hQi=>
Caco-2  M4j3c2Fxd3C2b4Ppd{BCe3OjeR?= NUGzWmdXOTEEoN88US=> NHT3cJEzPMLiaB?= MmHQ[IVkemWjc3XzJINmdGxiYYDvdJRwe2m|IHnu[JVk\WRiYomgOU1HXQ>? M1i1TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEm1PFY{Lz5{NEC5OVg3OzxxYU6=
AGS MVHGeY5kfGmxbjDBd5NigQ>? NGTSU|QyOCEQvF5CpC=> Mn36NE42KGh? MlX6bY5pcWKrdIOgeIhmKHWycnXneYxifGmxbjDv[kB1cGViSVytPEBo\W6n NWnNNWZwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxNFYyPjZpPkK0NVA3OTZ4PD;hQi=>
Ca9-22 Mlz1SpVv[3Srb36gRZN{[Xl? NGDSSWE{KM7:TR?= NFzaOIkyNzJiaB?= M{PlcJJm\HWlZYOgTIJTNWmwZIXj[YQhSVSILUKgdIhwe3Cqb4L5cIF1cW:w MlzGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzMk[1N|IoRjJ2MUK2OVMzRC:jPh?=
Ca9-22 MljHSpVv[3Srb36gRZN{[Xl? MWKzJO69VQ>? NILMTo0yKGh? Mlf1ZYJwdGm|aHXzJJRp\SCjYnnsbZR6KG:oIFjiVkB1dyCrbnT1Z4UhUUxvODDwdo9lfWO2aX;u M3HBelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUK2OVMzLz5{NEGyOlU{OjxxYU6=
HAECs NFewOG9HfW6ldHnvckBCe3OjeR?= MV:xNEDPxE1? MWWxJIg> MVtCpIF1fGWwdXH0[ZMhXE6ILd8xMZN1cW23bHH0[YQhUUODTT2xJIFv\CCYQ1HNMVEh\XiycnXzd4lwdg>? NHH6b|M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGzOFY2Pyd-MkSxN|Q3PTd:L3G+
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MCF-7 MVfBdI9xfG:|aYOgRZN{[Xl? NHr6NnQzOCEQvF2= NWLkeIJIOSCq MonabY5kemWjc3XzJINie3Cjc3WtPUBmdnq7bXWgZYN1cX[rdIm= NIXSUJE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEKxOlI5QSd-MkSyNVYzQDl:L3G+
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ARPE-19 M1PpXGZ2dmO2aX;uJGF{e2G7 M3nMZ|IxKM7:TR?= NGLle5MxNjViaB?= M4Dsc4lvcGmkaYTzJGFx\Wyrbj3pcoR2[2WmIIDoc5NxcG:{eXzheIlwdiCxZjDFdosh[W6mIFHreC=> NFmzU4E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEKyO|kyQCd-MkSyNlc6OTh:L3G+
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SGC-7901  M{\SbWFxd3C2b4Ppd{BCe3OjeR?= NUfSW|VVOjBizszN MW[yOEBp NWjBOmxIcW6qaXLpeJMhS1BvbXXkbYF1\WRiYYDvdJRwe2m| NH6ybIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK0NVM2OSd-MkSyOFE{PTF:L3G+
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KATOIII  MWjGeY5kfGmxbjDBd5NigQ>? NFXaZVU2OCEQvF2= M3TV[lQ5KGh? M2T1dGROW09? MWLpcoNz\WG|ZYOg[ZhxemW|c3nvckBw\iCKTFGtRVAzKG:{IFjMRU1COjRibX;s[YN2dGW| MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ2NECyN{c,OjR{NESwNlM9N2F-
NCI-N87  NIrLcYVHfW6ldHnvckBCe3OjeR?= MWW1NEDPxE1? NX7udYV7PDhiaB?= M1npS2ROW09? M4L0[4lv[3KnYYPld{BmgHC{ZYPzbY9vKG:oIFjMRU1CODJib4KgTGxCNUF{NDDtc4xm[3WuZYO= NV3QdZhpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOFQxOjNpPkK0NlQ1ODJ|PD;hQi=>
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KYSE30 MojvSpVv[3Srb36gRZN{[Xl? MlHTOVAh|ryP NITF[3E1QCCq MV\EUXNQ NXro[XRNfXC{ZXf1cIF1\XNidHjlJIV5eHKnc4Ppc44hd2ZiSFzBJINt[XO|IFm= MnnWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{NESwNlMoRjJ2MkS0NFI{RC:jPh?=
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TE1 MnPySpVv[3Srb36gRZN{[Xl? M{nPSlUxKM7:TR?= NI[zW3M1QCCq NELiTGdFVVOR NFS1d5F2eHKnZ4XsZZRmeyC2aHWg[ZhxemW|c3nvckBw\iCKTFGgZ4xie3NiSR?= MlfGQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{NESwNlMoRjJ2MkS0NFI{RC:jPh?=
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KYSE30 MknDSpVv[3Srb36gRZN{[Xl? MXGyNE82OC9zMECg{txO M4PLUVQ5KGh? NGrtb2NFVVOR NVPId5pmcW6qaXLpeJMheC2HcnugZY5lKHexcoTtZY5vcW5iZH;3cpJm\3WuYYTl[EBxNUGtdDDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NUTTcod6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOFQxOjNpPkK0NlQ1ODJ|PD;hQi=>
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HepG2 Mk\wRZBweHSxc3nzJGF{e2G7 NYj6fGs{OjBizszN MoDmNlQhcA>? NHvxN4hqdmirYnn0d{BGWktzL{KgdIhwe3Cqb4L5cIF1cW:wIHHu[EBmdmijbnPld{BXSjFvaX7keYNm\CCjcH;weI9{cXN? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDJ2N{mwPUc,OjR{NEe5NFk9N2F-
HepG2 NVvGUFdRTnWwY4Tpc44hSXO|YYm= MVyyNEDPxE1? NUm2Rmh{OiCq MXTlcohidmOnczDWRlEucW6mdXPl[EBHV1iRM3GgeJJidnOlcnnweIlwdmGuIHHjeIl3cXS7 M{j0UlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MkS3PVA6Lz5{NEK0O|kxQTxxYU6=
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Raji  MoHKSpVv[3Srb36gRZN{[Xl? NVy5VWExOTBizszN NHfCelQyKGh? NUXXWFlI[myxY3vzJIh{SkGIRjDpcoR2[2WmIFXyb|EwOiCyaH;zdIhwenmuYYTpc44> NYq1epZHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyOlk3OzBpPkK0NlY6PjNyPD;hQi=>
Raji  Mn;kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nJ[|ExKM7:TR?= MVixJIg> MUXpcohq[mm2czD0bIUh[mG|YXygc5IhcHOEQV\GMZN1cW23bHH0[YQh[2WubDDwdo9tcW[ncnH0bY9vKGGwZDD2bYFjcWyrdIm= M3XadlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Mk[5OlMxLz5{NEK2PVY{ODxxYU6=
A549 NX;SSop1TnWwY4Tpc44hSXO|YYm= NYe0NFVZOzBizszN MXKwMlUhcA>? Ml3tSG1UVw>? NFjSXYpqdmirYnn0d{B1cHKxbXLpck1qdmS3Y3XkJGMwTUKSzsKgWIhzOjN3wrDwbI9{eGixconsZZRqd25? MojCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR{N{e2PVYoRjJ2Mke3Olk3RC:jPh?=
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PANC-1 NVvrS4hFTnWwY4Tpc44hSXO|YYm= Ml3LNlAh|ryP MkLPOFghcA>? NYHEfWhGcW6qaXLpeJMhfGinIHX4dJJme3Orb36gc4Yh|pR4RDDpckBz\XOyb37z[UB1dyC2aHWgVHBCWs72wrDh[49vcXO2wrC= NI\aOFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEK5OFE{Oyd-MkSyPVQyOzN:L3G+
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SW480 NWfxXm9bTnWwY4Tpc44hSXO|YYm= MY[xNEDPxE1? MWSyNEBp Mlu0SG1UVw>? NWPsW|lOe3WycILld5NmeyC2aHWgR3JVKGGldHn2bZR6 Mkm5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|MkSzOlYoRjJ2M{K0N|Y3RC:jPh?=
HEK 293 M4LPe2Z2dmO2aX;uJGF{e2G7 MmqwNVAh|ryP NUHIfoRFPSCq NGKzNHlFVVOR MUHpcohq[mm2czDXcpQucW6mdXPl[EDPui2lYYTlcolvN1SFRkSgZYN1cX[rdImgZY5lKG63Y3zlZZIh|rJvY3H0[Y5qdiCjY3P1cZVt[XSrb36= M{m0[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{K0N|Y3Lz5{NEOyOFM3PjxxYU6=
HEK 293 NEDOTnZHfW6ldHnvckBCe3OjeR?= MX2xNEDPxE1? M32w[lUhcA>? M2PYZmROW09? Mn3Kd5VxeHKnc4Pld{B1cGViQ2LUJIFkfGm4aYT5 NH32NI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEOyOFM3Pid-MkSzNlQ{PjZ:L3G+
HL-60  NInxWXdHfW6ldHnvckBCe3OjeR?= NWL0OoFZOTBxMkCg{txO NFXlO3cyKGh? NGPnV2NqdmirYnn0d{B1cGYEoF6uJINpcW6nboPpd4V5fHKjY4VCpIlv\HWlZXSg[Iln\mW{ZX70bYF1cW:wIHnueI8h\3KjboXsc4N6fGW| NGLsOYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1O|AzOCd-MkSzOVcxOjB:L3G+
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HUVECs MmTDSpVv[3Srb36gRZN{[Xl? NF7R[GgyOMLizszN M1HvTlEhcA>? NVOwTphMcW6qaXLpeJMhfGinIFjEUEBz\WS3Y3XkJGNQYC1{IHX4dJJme3Orb36gZY5lKFCJST2yJJJmdGWjc3W= NXL4cXBqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSzPFUyODlpPkK0N|g2OTB7PD;hQi=>
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HCT-15 Mn:wRZBweHSxc3nzJGF{e2G7 MkXTNUBp MWfhZo9tcXOqZYOgeIhmKHC{b4TlZ5RqfmViZX\m[YN1eyCxZjDQS2UzyqCjZ3HpcpN1KGO3cnP1cYlvNWmwZIXj[YQh[XCxcITvd4l{ NGizdoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUSzNVQzPSd-MkW0N|E1OjV:L3G+
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HepG2  M1PuT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLTcnp4OjBizszN NFTpcWYzPCCq NHXWeY1{fXCycnXzd4V{KFSJRj5OtlEucW6mdXPl[EBk\WyuIIDyc4xq\mW{YYTpc44h[W6mIHnueoF{cW:w M2SyXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3NU[wOFg5Lz5{NUW2NFQ5QDxxYU6=
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HepG2  MUjGeY5kfGmxbjDBd5NigQ>? Ml3ONVAh|ryP MX61JIg> MWPicI9kc3NicHjvd5Bpd3K7bHH0[YQhVUGSS4OgbY5lfWOnZDDifUBmgG:pZX7veZMhXEeILd8yNS=> NFTr[WE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW2NFQ5QCd-MkW1OlA1QDh:L3G+
MCF-7  NXjzUGxHTnWwY4Tpc44hSXO|YYm= MoewNVAh|ryP MnnhNUBp NV;aSYlKcW6qaXLpeJMhUUxvMUit[Y5p[W6lZXSgZ4VtdCCvaXfyZZRqd25? M{TZN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3N{K3NFEyLz5{NUeyO|AyOTxxYU6=
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RD NWXQTZVGeUiWUzDhd5NigQ>? Mo[zdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVmQh[2WubIO= M3zSRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC Mne2dWhVWyCjc4PhfS=> NHLtOllyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> NUjUXYd4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
TC32 MVzxTHRUKGG|c3H5 NHvxcY9yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBVSzN{IHPlcIx{ MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MDA-MB-231 NVu5bVJ2TnWwY4Tpc44h[XO|YYm= NGTqW2s2OCC3TR?= NIPrfoRFd3ewcnXneYxifGmxbjDv[kBOVVB{IHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYSgOVAhfU1iYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ M2DXT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUK2NlI3Lz5{MkmyOlIzPjxxYU6=
MDA-MB-231 Ml;CSpVv[3Srb36gZZN{[Xl? MUK1NEB2VQ>? NHTOWI9Fd3ewcnXneYxifGmxbjDv[kBOVVB7IHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYSgOVAhfU1iYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ M4mzOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUK2NlI3Lz5{MkmyOlIzPjxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
c-Jun / α-tubulin / p-ERK / ERK / p-AKT / AKT; 

PubMed: 17482134     


ERK regulates c-Jun levels in melanoma. The indicated melanoma cell lines were treated with 50μM PD98059 (PD) or 10μM LY294002 (LY) for 12h in the absence of serum. Protein samples were analyzed by Western blots using the indicated antibodies. α-Tubulin reveals equal loading.

p-JNK / JNK / Cyclin D1 ; 

PubMed: 17482134     


Inhibition of the MEK/ERK pathway affects c-Jun, P-JNK and cyclin D1 levels. The indicated melanoma cell lines were treated with 50μM PD98059 for 16h. Protein samples were analyzed by Western blots using the indicated antibodies. α-Tubulin reveals equal loading.

p-HER2 / HER2 ; 

PubMed: 24244023     


TE1cells were treated with wortmannin (Akt signal inhibitor), PD98059 (MAPK signal inhibitor), or lapatinib (EGFR and HER2 dual inhibitor) at the indicated doses or with DMSO as a negative control for 48 h. HER2-related signaling molecules were assessed by Western blot. 

MMP9 / XIAP / VEGF ; 

PubMed: 29695559     


SK-Hep1 cells were treated 10 μM PD98059 for 48 h.  Protein levels of MMP-9, XIAP, VEGF, cyclin-D1, and pERK were evaluated with western blotting assay.

17482134 24244023 29695559
体内研究

在大脑缺血前30分钟用PD98059处理小鼠可以明显减轻伤害, 使脑梗塞的体积减小[4]。基于胰腺的湿重和组织学研究发现,提前30分钟用PD98059预处理 (10 mg/kg 静脉注射) 然后每小时注射一次蛙皮素连续三次的小鼠可以明显改善蛙皮素诱导的急性胰腺炎[7]。卡拉胶损伤一小时后用PD98059 (10 mg/kg) 对小鼠进行治疗可以发现与炎症相关的所有指标均有所下降[11]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

- 合并

体外MEK激酶活性测定:

在含有44-kDa GST-MAPK 或者45-kDa GST-MEK1的体系中检测32P被掺入蛋白 MBP中的情况。 反应体系50 μL ,含有50 mM Tris, pH 7.4/10 mM MgCl2/2 mM EGTA/10 μM [γ-32P]ATP, 加入10 μg GST-MEK1, 0.5 μg GST-MAPK和 40 μg MBP。30°C 孵育15 分钟, 加入Laemmli SDS 样品缓冲液终止反应。磷酸化的MBP 进行10% SDS-PAGE分析
细胞实验:

[1]

- 合并
  • Cell lines: K-Balb, KNRK, v-raf-3Y1, SRA/3Y1, EGFR/3T3, 和K562
  • Concentrations: 溶于DMSO, 终浓度~100 μM
  • Incubation Time: 3 天, 或者7-10天
  • Method:

    细胞按10,000-20,000个/mL的密度接种在多孔平板中进行单层生长。48小时后把不同浓度的PD98059 加到细胞培养基孵育3天。 然后通过胰酶将细胞从平板中消化下来并用Coulter 计数器计数。 将细胞按5,000-10,000每皿的浓度接种在35 mm的培养皿中,培养基中含有0.3% 的琼脂和期望浓度的PD98059,让细胞在软琼脂上生长.经过7-10天的生长, 可以借助解剖显微镜将可见的菌落数出来。


    (Only for Reference)
动物实验:

[7]

- 合并
  • Animal Models: 患有急性胰腺炎的雄性Sprague–Dawley 大鼠
  • Dosages: 10 mg/kg
  • Administration: 静脉注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 14 mg/mL warmed (52.37 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
1mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 267.28
化学式

C16H13NO3

CAS号 167869-21-8
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    How to formulate this inhibitor for i.p. injection?

  • 回答:

    You can prepare the stock by the vehicle 30% PEG400/0.5% Tween80/5% Propylene glycol, 0.5% CMC.

MEK Signaling Pathway Map

MEK Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID