SCH772984

For research use only. Not for use in humans.

目录号:S7101

SCH772984 Chemical Structure

Molecular Weight(MW): 587.67

SCH772984是一种新型特异性的ERK1/2抑制剂,无细胞试验中IC50分别为4 nM和1 nM, 对含有RAS或BRAF突变的癌细胞具有强大的功效。

规格 价格 库存 购买数量  
RMB 2210.07 现货
RMB 8763.3 现货
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客户使用Selleck生产的SCH772984发表文献277篇:

产品安全说明书

ERK抑制剂选择性比较

生物活性

产品描述 SCH772984是一种新型特异性的ERK1/2抑制剂,无细胞试验中IC50分别为4 nM和1 nM, 对含有RAS或BRAF突变的癌细胞具有强大的功效。
特性 SCH772984不直接抑制MEK1, MEK2, BRAF, 或 CRAF酶活性。
靶点
ERK2 [1]
(Cell-free assay)
ERK1 [1]
(Cell-free assay)
1 nM 4 nM
体外研究

SCH772984是新型,选择性,ATP竞争性的ERK1/2抑制剂。SCH772984抑制ERK底物p90核糖体S6激酶(T359/S363 磷酸化-RSK)的磷酸化,这种作用存在剂量依赖性。SCH772984也能抑制ERK自身活化环中残基的磷酸化。SCH772984分别抑制约88%和49%BRAF突变型或RAS-突变型肿瘤细胞系,EC50值<500 nM。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
2P-ERK2 M{OwVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTBwMkSgcm0> MnTENlU{PTB7M{G=
WM-266-4 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTJyIH7N M2HkbFI{PjF2OEm4
UACC-62 NVfX[VNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3iNo9MUUN3ME2zNEBvVQ>? NX;6UVVOOjN4MUS4PVg>
Colo-205 M3rnVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDUTWM2OD1|NjDuUS=> MXKyN|YyPDh7OB?=
SK-Mel-1 NXfjWpdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTN5IH7N NVL2WGNCOjN4MUS4PVg>
WiDr MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;kbmlEPTB;M{mgcm0> M1zkZlI{PjF2OEm4
M14 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTR5IH7N MYmyN|YyPDh7OB?=
HT-29 NEWxUZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjEeodnUUN3ME21NEBvVQ>? NXXQOlVUOjN4MUS4PVg>
8505C M3\rZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTVyIH7N M2q0dFI{PjF2OEm4
HT-144 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDmPIlKSzVyPU[wJI5O M1\nW|I{PjF2OEm4
SK-Mel-5 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M36yc2lEPTB;Nk[gcm0> NGrHdmIzOzZzNEi5PC=>
A375-SM MnXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjH[2x7UUN3ME23OUBvVQ>? Mn\FNlM3OTR6OUi=
SK-Mel-28 NXLUPHBtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTh3IH7N NXH5b5JTOjN4MUS4PVg>
LOX MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\STWM2OD1zMECgcm0> MknQNlM3OTR6OUi=
SK-Mel-3 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\kTWM2OD1zMUigcm0> NVHhOWtMOjN4MUS4PVg>
K1 M4q5PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInmTWRKSzVyPUGzNEBvVQ>? MXWyN|YyPDh7OB?=
Hs-695T Mm\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HmUWlEPTB;MU[1JI5O M4XVXlI{PjF2OEm4
BHT-101 M1nEeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvSTWM2OD1|MECgcm0> NV;TV2toOjN4MUS4PVg>
RPMI-7951 MoLUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTN2NDDuUS=> NFnxWI4zOzZzNEi5PC=>
A2058 NEXlU2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTN4MDDuUS=> M{PsW|I{PjF2OEm4
SK-Hep-1 MlXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGqyXnRKSzVyPUG0NlIhdk1? M1PlVlI{PjF2OEm4
A673 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzQ[mJKSzVyPUOwNFEhdk1? MoDpNlM3OTR6OUi=
DBTRG-05MG M{[zXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIriU|lKSzVyPUOwNFEhdk1? MWKyN|YyPDh7OB?=
SW-626 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTN|IH7N NXHER|ZZOjN4MUS4PVg>
LoVo MmrwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTR5IH7N NE\3VGwzOzZzNEi5PC=>
MiaPaCa NXrH[2o3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXuZlNKSzVyPUWzJI5O NVTuUHNYOjN4MUS4PVg>
SW-620 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTFyNDDuUS=> M1jHbVI{PjF2OEm4
CAPAN-1 NUHONHozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfSTWM2OD1zMESgcm0> MVKyN|YyPDh7OB?=
SW-527 NGi0b2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm[5TWM2OD1zMkGgcm0> MWiyN|YyPDh7OB?=
HCT-116 NV3hcFhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1[2PWlEPTB;MUK4JI5O MlvsNlM3OTR6OUi=
SW-480 M1XlfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXPdnpKSzVyPUG2OUBvVQ>? NVH0bGZKOjN4MUS4PVg>
HPAC NYrqc4V7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\HbmRKSzVyPUG3NEBvVQ>? MWGyN|YyPDh7OB?=
OVCAR-5 NFz4bXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLmWW1KUUN3ME2yNFghdk1? NF\6O2YzOzZzNEi5PC=>
AsPc-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2W4d2lEPTB;MkewJI5O M4nje|I{PjF2OEm4
A549 M1vGcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHHTWM2OD1|Mk[gcm0> MmXENlM3OTR6OUi=
SNU-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DDdmlEPTB;M{W0JI5O MVeyN|YyPDh7OB?=
HOP62 MoX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXtTWM2OD14N{[gcm0> MonMNlM3OTR6OUi=
H23 NUnrO21VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzYeGF4UUN3ME2xNFAxKG6P NEfyToMzOzZzNEi5PC=>
MB-231 NHrNWZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvzTWM2OD1zMECwJI5O M4TDcFI{PjF2OEm4
SU.86.86 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDMXWd7UUN3ME2xNFAyKG6P NHq0V|UzOzZzNEi5PC=>
CFPAC-1 NVXZOXI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTFyMEGgcm0> NXX4O|Z{OjN4MUS4PVg>
A427 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnruTWM2OD1zNEOzJI5O NYT6eYhlOjN4MUS4PVg>
MDAH-2774 NHy2cpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrvbGRKSzVyPUK2OVchdk1? NHjwSoQzOzZzNEi5PC=>
NCI-H157 Mlv5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfqTWM2OD1|MECwJI5O M3jBU|I{PjF2OEm4
HTB-177 MkPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGL0eFdKSzVyPUOwNFAhdk1? MXeyN|YyPDh7OB?=
UM-UC-3 MnvwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rBV2lEPTB;M{CwNUBvVQ>? MknSNlM3OTR6OUi=
HCT-8 Mn\WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvsc|hzUUN3ME2zNFAyKG6P MVOyN|YyPDh7OB?=
Panc-1 NYnkfYl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3PTVVnUUN3ME2zNFAyKG6P NVHMeJZqOjN4MUS4PVg>
DLD-1 MnPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\UTWM2OD1|MECxJI5O MU[yN|YyPDh7OB?=
HCT-15 NILMe3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\1NYdKSzVyPUOwNFEhdk1? MViyN|YyPDh7OB?=
HL-60 MnzZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTNyIH7N MnmyNlM3OTR6OUi=
SK-Mel-2 NWPxXWZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPTd|dKSzVyPUO0JI5O NFXKe|IzOzZzNEi5PC=>
RD NIHQRVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTF{MzDuUS=> NF\VRZAzOzZzNEi5PC=>
HT-1197 NYPoNnU3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjLTWM2OD1|MU[gcm0> M{[0XVI{PjF2OEm4
Molt-3 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTZyMDDuUS=> NFXwSoczOzZzNEi5PC=>
PA-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVL4c|lEUUN3ME2xNFAyKG6P M3S2ZlI{PjF2OEm4
Molt-4 NEnRbJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDJTWM2OD1|MECxJI5O NWGzTZl2OjN4MUS4PVg>
NCI-H292 NHzIdmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorsTWM2OD17MDDuUS=> NFjsPJIzOzZzNEi5PC=>
A2780 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTF2MzDuUS=> Mm[wNlM3OTR6OUi=
IGROV-1 NV3yZYlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zOUmlEPTB;MUS2JI5O NFT2b3ozOzZzNEi5PC=>
SK-N-SH MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYf6VFZEUUN3ME2xOVAhdk1? MkiyNlM3OTR6OUi=
N-87 M{nKRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlr4TWM2OD1|MEegcm0> MnXHNlM3OTR6OUi=
H322 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7qbZQ5UUN3ME2zNlUhdk1? MViyN|YyPDh7OB?=
H716 NYSxXnN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTN|NDDuUS=> NWr0T|A1OjN4MUS4PVg>
TT NYLqb3VwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjVWVJKSzVyPUSwOkBvVQ>? NXm0V|FjOjN4MUS4PVg>
Caki-1 NHzqXmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTR3MDDuUS=> MV:yN|YyPDh7OB?=
5637 NULK[pJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTZzMDDuUS=> NVLEfpdVOjN4MUS4PVg>
MB-453 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTZ5MjDuUS=> M2TOT|I{PjF2OEm4
RT-4 NUG4NZJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\STWM2OD16MUCgcm0> M2XrO|I{PjF2OEm4
HOP92 M{jJTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTh{MDDuUS=> NWrZdllEOjN4MUS4PVg>
KG-1 M{j2OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XGV2lEPTB;OUCwJI5O MYeyN|YyPDh7OB?=
Hs-294T NVPqWYFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTl2NTDuUS=> MkfoNlM3OTR6OUi=
SF-539 MlXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mor3TWM2OD1zMECwJI5O MVOyN|YyPDh7OB?=
U-251 NUjKSGN5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3z5[2lEPTB;MUCwNEBvVQ>? NEHRW2ozOzZzNEi5PC=>
MB-468 NFH5OZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;4VWlEPTB;MUCwNEBvVQ>? NUjZTI5yOjN4MUS4PVg>
HS746T M3;OS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTFyMECgcm0> MX[yN|YyPDh7OB?=
SCABER MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTFyMECgcm0> MmX1NlM3OTR6OUi=
MCF-7 Mnm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fncGlEPTB;MUCwNUBvVQ>? NVTrZ2tJOjN4MUS4PVg>
CHL-1 NXraZoIzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fKWmlEPTB;MUS2NEBvVQ>? MWWyN|YyPDh7OB?=
U87MG MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX[zNJlPUUN3ME2yNFAxKG6P MX:yN|YyPDh7OB?=
SJCRH30 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITyTmRKSzVyPUKwNFIhdk1? M3[4dFI{PjF2OEm4
ES-2 M{Xx[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrkTWM2OD1{NkW5JI5O MkHQNlM3OTR6OUi=
HT-1376 M2PQ[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1H0c2lEPTB;MkiwNEBvVQ>? MkHBNlM3OTR6OUi=
A172 NYDFWItzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjv[oo3UUN3ME2zNFAxKG6P MXSyN|YyPDh7OB?=
769P NYq2OJFMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHxXJRKSzVyPUOwNFAhdk1? M4fnWlI{PjF2OEm4
NCI-H520 NVHJfYxtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTNyMECgcm0> M2i1OVI{PjF2OEm4
DU145 NXryPWhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PTV2lEPTB;M{CwNEBvVQ>? M2LNcFI{PjF2OEm4
K562 NHr0dnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTuVFJKSzVyPUOwNFAhdk1? M3;aVlI{PjF2OEm4
U-937 NIr4c5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXL0SoR5UUN3ME2zNFAxKG6P Mlv2NlM3OTR6OUi=
A204 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LqT2lEPTB;M{CwNUBvVQ>? Mk\KNlM3OTR6OUi=
DAOY MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnXwTWM2OD1|MECxJI5O NIf6VZAzOzZzNEi5PC=>
SF-268 MkDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTNyMEGgcm0> M1LSPVI{PjF2OEm4
SF-295 M1W1d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTNyMEGgcm0> M1m1clI{PjF2OEm4
SNB-19 M1LaWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrQXG5KSzVyPUOwNFEhdk1? NITwNIYzOzZzNEi5PC=>
SNB-75 NEHD[ZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWfQS4FwUUN3ME2zNFAyKG6P M2GxOlI{PjF2OEm4
U373-MG M1\hZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWn0Tmo3UUN3ME2zNFAyKG6P M1jHS|I{PjF2OEm4
786-O MorDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTNyMEGgcm0> MlzaNlM3OTR6OUi=
A498 Ml;sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\rTWM2OD1|MECxJI5O MYOyN|YyPDh7OB?=
ACHN MkK3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLoe5pFUUN3ME2zNFAyKG6P MnHFNlM3OTR6OUi=
EKVX MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrx[JF1UUN3ME2zNFAyKG6P NVj5dJNDOjN4MUS4PVg>
H226 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTNyMEGgcm0> M{DwNVI{PjF2OEm4
H522 NELr[|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTITWM2OD1|MECxJI5O NWK4VHNiOjN4MUS4PVg>
HeLa M37GZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTNyMEGgcm0> M2\6[FI{PjF2OEm4
SK-OV-3 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILJflRKSzVyPUOwNFEhdk1? MV:yN|YyPDh7OB?=
Ln Cap MnXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHtUJRKSzVyPUOwNFEhdk1? NWLUbXVlOjN4MUS4PVg>
PC3 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPK[HhTUUN3ME2zNFAyKG6P Mnf4NlM3OTR6OUi=
SNU-16 NVXXcWlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTNyMEGgcm0> M3zW[FI{PjF2OEm4
FTC-133 NGXL[5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXixd29ZUUN3ME2zNFAyKG6P NVPST283OjN4MUS4PVg>
Ro82-W-1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTNyMEGgcm0> M3PRelI{PjF2OEm4
Daudi MnnMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTNyMEGgcm0> M4[0d|I{PjF2OEm4
Jijoye NX7jV|lCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTNyMEGgcm0> NYDTZZpnOjN4MUS4PVg>
Jurkat MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF:3VnNKSzVyPUOwNFEhdk1? NVP6O3RJOjN4MUS4PVg>
J-82 M2LXc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\JOIN6UUN3ME2zNFAyKG6P MonHNlM3OTR6OUi=
TCC-SUP MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTNyMEGgcm0> NVizNol{OjN4MUS4PVg>
BT-474 M1L5UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTNyMEGgcm0> NG[0eYczOzZzNEi5PC=>
ZR-75-1 NYPKXIpLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrFTWM2OD1|MECxJI5O NH7WWpkzOzZzNEi5PC=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
cyclin B1 / cyclin D1 / p21; 

PubMed: 26725216     


Cells treated as above were collected for western blot for total cyclin B1, cyclin D1 and p21, and of phosphorylated, inactivated RB (S807/811; pRB). Western blot for pERK was done to verify SCH772984 inhibition; β-actin was the loading control.

pRSK / pERK / pAKT / pMEK; 

PubMed: 26725216     


Cells were treated for 4 or 24 hr with DMSO vehicle or SCH772984, then evaluated by western blot with phospho-specific antibodies for RSK (T395/S363; pRSK), MEK1/2 (S217/221; pMEK), AKT (S473; pAKT), and ERK (T202/Y204; pERK). Total RSK, ERK, AKT, MEK and β-actin were also analyzed. Data are representative of three independent experiments.

DUSP1 / DUSP4 / DUSP6; 

PubMed: 26725216     


Cells were treated for 4 or 24 hr with DMSO vehicle or SCH772984 for 72 hr and evaluated by western blot for DUSP1, DUSP4, DUSP6 and β-actin.

pCRAF(S338, S289, S296, S301); 

PubMed: 26725216     


Cells were treated for 4 or 24 hr with DMSO vehicle or SCH772984 for 72 hr and evaluated by western blot for pCRAF (S338), pCRAF (S289/296/301), total CRAF and β-actin.

Aurora B / ETS1 / ETS2; 

PubMed: 26725216     


Cells were treated with vehicle or SCH772984 for 7 days, then immunoblotted for Aurora B, MYC, ETS1 or ETS2, and β-actin. Data are representative of three independent experiments.

26725216
Growth inhibition assay
Cell viability; 

PubMed: 30118499     


NCI-H747, SW837, SW480, and SW620 cells were treated with the ERK inhibitor SCH772984 at indicated concentrations for 72 hours. Dimethyl sulfoxide (DMSO) (0.01%) was used as the control treatment. Each data point represents the mean of five replicates; error bars indicate one SD.

30118499
Immunofluorescence
TOMM20; 

PubMed: 30833752     


Mitochondrial morphologies of PDAC cells treated with SCH772984 (ERKi, 1 µM) for 24 h. Green, Anti-TOMM20; blue, DAPI; scale bar, 20 μm.

pERK1/2; 

PubMed: 30213106     


After treatment with 10 µM of the ERIK1/2 inhibitors, the expression of p-ERK1/2 protein in HeLa cells was detected using immunofluorescence (400×), bar = 50 μm.

30833752 30213106
体内研究 SCH772984按耐受剂量处理移植瘤模型,诱导肿瘤衰退。SCH772984作用于抗BRAF或MEK抑制剂的模型,有效抑制MAPK信号和细胞增殖。[1]

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

ERK2 IMAP 酶实验:

SCH772984作用于纯化的ERK2或ERK1,按一式两份进行8点稀释曲线。酶添加到实验板中。与化合物温育,然后加入底物肽和ATP溶液中。384孔板中每孔加入14μl稀释的酶(每组反应含0.3ng活性ERK2)。实验板轻轻震荡混合试剂,然后在室温下温育45分钟。加入60μl of IMAP 结合溶液 (IMAP珠在1X结合缓冲液中按1:2200稀释)终止反应。实验板在室温下再温育0.5小时,使磷酸肽与IMAP珠完全结合。然后在 LJL分析仪上读数。
细胞实验:

[1]

- 合并
  • Cell lines: BRAF突变型或 RAS突变型肿瘤系
  • Concentrations: ~10 μM
  • Incubation Time: 5 天
  • Method:

    在96孔板中进行细胞增殖实验,细胞按每孔 4,000个的密度接种。接种24小时后,使用DMSO处理细胞,9点IC50稀释 (0.001-10 μM) ,DMSO终浓度为1%。使用ViaLight发光试剂盒5天后,测定存活力。细胞系存活力检测中,使用SCH772984处理细胞4天,然后进行CellTiterGlo发光细胞活力检测。


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: 裸鼠
  • Dosages: 12.5 mg/kg, 25 mg/kg, 50 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 14 mg/mL warmed (23.82 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):
5% DMSO+30% PEG 300+ddH2O
0.6mg/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 587.67
化学式

C33H33N9O2

CAS号 942183-80-4
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(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:

    I would like to inhibit Erk1/2 by treating the mice with the inhibitor. by what kind of administration way and at what concentration could it be done?

  • 回答:

    SCH772984 can be administrated by I.P. The dosages can be used as: 12.5 mg/kg, 25 mg/kg, 50 mg/kg. For more detail information please find the paper below: http://cancerdiscovery.aacrjournals.org/content/3/7/742.full

ERK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID