SCH772984

For research use only. Not for use in humans.

目录号:S7101

SCH772984 Chemical Structure

CAS No. 942183-80-4

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 11049.1 现货
RMB 44144.7 现货
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客户使用Selleck生产的SCH772984发表文献388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 NFyyXWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTBwMkSgcm0> MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTN3MEmzNUc,OjV|NUC5N|E9N2F-
WM-266-4 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnGSYhlUUN3ME2yNEBvVQ>? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
UACC-62 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nwSWlEPTB;M{Cgcm0> NYfGd4N{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
Colo-205 M{njPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfQPWhlUUN3ME2zOkBvVQ>? NUf5b3VlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
SK-Mel-1 NVX5VYgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXpTWM2OD1|NzDuUS=> M{T2SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
WiDr M4TMe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3MTWM2OD1|OTDuUS=> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
M14 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NELJb2FKSzVyPUS3JI5O NGDMTI49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
HT-29 MlPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jpNmlEPTB;NUCgcm0> M3LaZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
8505C MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\QeFFYUUN3ME21NEBvVQ>? NFfCUoI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
HT-144 MnLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTZyIH7N M3PUNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
SK-Mel-5 NHraT|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\yTWM2OD14NjDuUS=> MkXSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
A375-SM M3fiNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Moi3TWM2OD15NTDuUS=> Mm\wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
SK-Mel-28 M1z5UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDkTWM2OD16NTDuUS=> MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
LOX NYr3U3JrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TBdGlEPTB;MUCwJI5O M4XBOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
SK-Mel-3 NUP4UollT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTFzODDuUS=> M1zhfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
K1 NV;4[Hc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1q4TGlEPTB;MUOwJI5O NFH6Z2E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
Hs-695T MmWwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfZNXBKSzVyPUG2OUBvVQ>? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
BHT-101 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm[1TWM2OD1|MECgcm0> NFXFd2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
RPMI-7951 NXTLUoRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnxZnRCUUN3ME2zOFQhdk1? NGTaflU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
A2058 Mn\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTN4MDDuUS=> NF7nU5U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
SK-Hep-1 MorHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnOemNvUUN3ME2xOFIzKG6P NVn0OIw{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
A673 NH7wcFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPKZ5pkUUN3ME2zNFAyKG6P MlzQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
DBTRG-05MG MoLES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofqTWM2OD1|MECxJI5O NXns[|JURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
SW-626 MnvVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGWwc4hKSzVyPUOzJI5O MoKxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
LoVo MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTR5IH7N NHHLWG89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
MiaPaCa NFn6[5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{[5e2lEPTB;NUOgcm0> Mm\sQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
SW-620 Mn;VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTFyNDDuUS=> Moj3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
CAPAN-1 NXXFVWFlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml:wTWM2OD1zMESgcm0> MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
SW-527 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXqfVBKSzVyPUGyNUBvVQ>? NIDYepg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
HCT-116 NHHHTFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2m4cGlEPTB;MUK4JI5O MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
SW-480 NIiwXlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTF4NTDuUS=> NYTXOFRPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
HPAC NXm5dXk1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrWUJdKSzVyPUG3NEBvVQ>? M3\IT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
OVCAR-5 NXHB[HNLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUO2TmtyUUN3ME2yNFghdk1? M1fsS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
AsPc-1 Mk\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYeyRWlHUUN3ME2yO|Ahdk1? NF32fZo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
A549 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTN{NjDuUS=> M4X2WlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
SNU-1 MmL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3y3cGlEPTB;M{W0JI5O MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
HOP62 NXO4NIhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTZ5NjDuUS=> MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
H23 M3v3Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;OOXR5UUN3ME2xNFAxKG6P NWLHUFl6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
MB-231 NWXLeWhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzwTWM2OD1zMECwJI5O MnG2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
SU.86.86 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTFyMEGgcm0> NHHycm89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
CFPAC-1 NUTUTJhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jGPGlEPTB;MUCwNUBvVQ>? NWHxTXJwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
A427 M13lWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3RPIVKSzVyPUG0N|Mhdk1? MnX1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
MDAH-2774 NELq[YpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTJ4NUegcm0> Mk\VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
NCI-H157 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLmZolKSzVyPUOwNFAhdk1? MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
HTB-177 NWnQcmlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3tWIFKSzVyPUOwNFAhdk1? MnThQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
UM-UC-3 NUe3fYVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTNyMEGgcm0> MlvyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
HCT-8 NESzS2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2THWWlEPTB;M{CwNUBvVQ>? M2[xWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
Panc-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPNeJJKUUN3ME2zNFAyKG6P NF3oOGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
DLD-1 M2jkW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrZTWM2OD1|MECxJI5O NFezVVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
HCT-15 NInLWVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\hTWM2OD1|MECxJI5O MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
HL-60 M33YNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2e4O2lEPTB;M{Cgcm0> MlHqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
SK-Mel-2 NWj1fpJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlT4TWM2OD1|NDDuUS=> M3n2SlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
RD NGfYOpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWmzdVdwUUN3ME2xNlMhdk1? M3\tPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
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J-82 M1n1S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzV[4szUUN3ME2zNFAyKG6P M{fONlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
TCC-SUP MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXiU|JKSzVyPUOwNFEhdk1? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
BT-474 NUOxZnNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{O4OGlEPTB;M{CwNUBvVQ>? MkX2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
ZR-75-1 NF\hcllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILHdHpKSzVyPUOwNFEhdk1? NXjsPWw1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
A375 NVLMdHVoTnWwY4Tpc44h[XO|YYm= NGPHdYkzKGi{cx?= Mo\aTY5pcWKrdHnvckBw\iCHUluyJIlvKGi3bXHuJGE{PzViY3XscJMhcGG{Yn;ybY5oKEJvUlHGJHY3ODCHIH31eIFvfCCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBxcG:|cHjvMWVTUzJibHX2[Ywh[W[2ZYKgNkBpenNiYomgR4VtdG:vaXPzJGFzemG7U3PhcnROKF[WSTDpcYFocW6pIHHuZYx6e2m|LDDJR|UxKD1iMD6wNFQh|ryPLh?= M2iyO|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUe3PVgyLz5{NUm3O|k5OTxxYU6=
A375 MYrGeY5kfGmxbjDhd5NigQ>? Mn3RTY5pcWKrdHnvckBw\iCHUluyJIlvKGi3bXHuJGE{PzViY3XscJMhcGG{Yn;ybY5oKEKUQV[gWlYxOEVibYX0ZY51KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJJBpd3OyaH;yfYxifGWmIFXST|IhdGW4ZXzzMEBKSzVyIE2gNE4xODRizszNMi=> NIT2PVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEO3OlMxPid-MkizO|Y{ODZ:L3G+
COLO205 NYLoc4N3SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MmrJOEBl[Xm| MkPpRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFT1zPNlA2KGOnbHzzJIhiemKxcnnu[{BDWkGIIG[2NFBGN0RibYX0ZY51KG2nYYP1doVlKGGodHXyJFQh\GG7czygTWM2OCB;IECuNFE3KM7:TT6= NEjWXHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MECzOFYyPSd-M{CwN|Q3OTV:L3G+
A375 NViwTmNiTnWwY4Tpc44h[XO|YYm= NXXUU29MOiCqcoO= M{T1UmlvcGmkaYTpc44hd2ZiRWLLNU8zKGmwIHj1cYFvKEF|N{WgZ4VtdHNiaHHyZo9zcW6pIFKtVmFHKFZ4MEDFJI12fGGwdDDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCyaH;zdIhwNVKVSzDs[ZZmdCCjZoTldkAzKGi{czDifUBE\Wyub33pZ5MhSXK{YYnTZ4FvXE1iVmTJJIlu[WerbnegZY5idHm|aYOsJGlEPTBiPTCwMlAzKM7:TT6= M4PmPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUe3PVgyLz5{NUm3O|k5OTxxYU6=
A375 NVjWWldxTnWwY4Tpc44h[XO|YYm= M4jPVlIhcHK| M2e1OmlvcGmkaYTpc44hd2ZiRWLLNU8zKGmwIHj1cYFvKEF|N{WgZ4VtdHNiaHHyZo9zcW6pIFKtVmFHKFZ4MEDFJI12fGGwdDDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCyaH;zdIhwNVKVSzDs[ZZmdCCjZoTldkAzKGi{czDifUBE\Wyub33pZ5MhSXK{YYnTZ4FvXE1iVmTJJIlu[WerbnegZY5idHm|aYOsJGlEPTBiPTCwMlAzKM7:TT6= NWDQT|QzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5O|c6QDFpPkK1PVc4QThzPD;hQi=>
A375 NFTWdZRHfW6ldHnvckBie3OjeR?= NXTkWXB7UW6qaXLpeIlwdiCxZjDFVmszKGmwIHj1cYFvKEF|N{WgZ4VtdHNiaHHyZo9zcW6pIFLSRWYhXjZyMFWgcZV1[W62IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKHCqb4PwbI9zgWyjdHXkJHJUUyCuZY\lcJMtKEmFNUCgQUAxNjB{IN88UU4> M1fTfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6M{e2N|A3Lz5{OEO3OlMxPjxxYU6=
HT-29 NGjXVoNCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NX7sUFZLPCCmYYnz NHPJeJNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUMVI6KGOnbHzzJIhiemKxcnnu[{BDWkGIIG[2NFBGN0RibYX0ZY51KG2nYYP1doVlKGGodHXyJFQh\GG7czygTWM2OCB;IECuNFU6KM7:TT6= M1PXPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMEO0OlE2Lz5|MECzOFYyPTxxYU6=
HT-29 M2nYSGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MkGzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDoZZJjd3KrbnegRnJCTi:NUlHTJI12fGGwdDygTWM2OCB;IECuNFU6KM7:TT6= MmPrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl5NEiwOVEoRjJ7N{S4NFUyRC:jPh?=
A375 NGjVVmpCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MXe3NkBpenN? NXjtS|BoSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBN|c2KGOnbHzzJIhiemKxcnnu[{BDNVKDRjDWOlAxTSCvdYThcpQh[W[2ZYKgO|IhcHK|IHL5JGNmdGyxbXnjd{BCenKjeWPjZY5VVSCYVFmgbY1i\2mwZzDhcoFtgXOrczygTWM2OCB;IECuNFch|ryPLh?= M1TEPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OUe3PVgyLz5{NUm3O|k5OTxxYU6=
HT-29 M332dWFxd3C2b4Ppd{Bie3OjeR?= MnvkTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKVD2yPUBk\WyuczDoZZJjd3KrbnegRnJCTi:NUlHTJI12fGGwdDDifUBk[XOyYYPlJIFkfGm4YYTpc44h[XO|YYmsJGlEPTBiPTCwMlA6PiEQvF2u NIC1eVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUe0PFA2OSd-Mkm3OFgxPTF:L3G+

... 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(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、SDS / 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、SDS / 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