SCH772984

For research use only.

Catalog No.S7101

352 publications

SCH772984 Chemical Structure

CAS No. 942183-80-4

SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 values of 4 nM and 1 nM in cell-free assay, respectively, And show robust efficacy in RAS- or BRAF-mutant cancer cells.

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Selleck's SCH772984 has been cited by 352 publications

Purity & Quality Control

Choose Selective ERK Inhibitors

Biological Activity

Description SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 values of 4 nM and 1 nM in cell-free assay, respectively, And show robust efficacy in RAS- or BRAF-mutant cancer cells.
Features Does not directly inhibit MEK1, MEK2, BRAF, or CRAF enzyme activity.
Targets
ERK2 [1]
(Cell-free assay)
ERK1 [1]
(Cell-free assay)
1 nM 4 nM
In vitro

SCH772984 is a novel, selective and ATP competitive inhibitor of ERK1/2. SCH772984 inhibits phosphorylation of the ERK substrate p90 ribosomal S6 kinase (T359/S363 phospho-RSK) in a dose-dependent manner. SCH772984 also inhibits phosphorylation of residues in the activation loop of ERK itself. SCH772984 demonstrates EC50 values <500 nM in approximately 88% and 49% of BRAF-mutant or RAS-mutant tumor lines, respectively. Importantly, SCH772984 effectively inhibited MAPK signaling and cell proliferation in tumor cells resistant to concurrent treatment with BRAF and MEK inhibitors. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
2P-ERK2 NXTDfFZvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWXJR|UxRTBwMkSgcm0> NGe2RmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO1NFk{OSd-MkWzOVA6OzF:L3G+
WM-266-4 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTJyIH7N MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
UACC-62 M4q1Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXPTWM2OD1|MDDuUS=> M2DUOFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
Colo-205 NWfSdVJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTN4IH7N MmHaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
SK-Mel-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnK4TWM2OD1|NzDuUS=> NUXKNIdzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
WiDr Mlm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmT0TWM2OD1|OTDuUS=> NEHk[4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
M14 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoTGTWM2OD12NzDuUS=> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
HT-29 M372e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NViycpJQUUN3ME21NEBvVQ>? NInoUlc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
8505C NHG4TFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHyTWM2OD13MDDuUS=> NGG2bIw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
HT-144 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfveGhKSzVyPU[wJI5O M3;0OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
SK-Mel-5 NVvCOGVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDGUY9YUUN3ME22OkBvVQ>? NWrIb2FPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
A375-SM NUGzSpVPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXHJR|UxRTd3IH7N NIXmbVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
SK-Mel-28 NH\xdpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTh3IH7N MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
LOX MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3H5VWlEPTB;MUCwJI5O NVXaWJMzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
SK-Mel-3 MofFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1u1PGlEPTB;MUG4JI5O MmTmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
K1 NF:4NmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml65TWM2OD1zM{Cgcm0> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
Hs-695T NUP3V|lOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFryVopKSzVyPUG2OUBvVQ>? M2PKdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
BHT-101 NEDrVnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTNyMDDuUS=> M3TENFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
RPMI-7951 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MontTWM2OD1|NESgcm0> NH\CUoQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
A2058 NXHkWnppT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTN4MDDuUS=> Ml;uQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
SK-Hep-1 MmL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4XpSmlEPTB;MUSyNkBvVQ>? M3zNVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
A673 MkT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M134PWlEPTB;M{CwNUBvVQ>? M2roT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
DBTRG-05MG M122fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLkPWF2UUN3ME2zNFAyKG6P MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
SW-626 MkXCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTN|IH7N M4HVZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
LoVo MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2e0emlEPTB;NEegcm0> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
MiaPaCa M3\pbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHLSJhGUUN3ME21N{BvVQ>? MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
SW-620 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnIfJVvUUN3ME2xNFQhdk1? NXnke3Y1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
CAPAN-1 NHPrNm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;SVWpKSzVyPUGwOEBvVQ>? NF3KOHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
SW-527 NE\hcWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnBNlJNUUN3ME2xNlEhdk1? NHzJOZE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
HCT-116 MmnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkX4TWM2OD1zMkigcm0> NVPneHFERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
SW-480 M4fOVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4X3XmlEPTB;MU[1JI5O NYjEXoJtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
HPAC MmnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDtN5VIUUN3ME2xO|Ahdk1? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
OVCAR-5 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTJyODDuUS=> M3TRXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
AsPc-1 NV75ZoRxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPXTWM2OD1{N{Cgcm0> NHr6clI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
A549 MmW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzpVXVtUUN3ME2zNlYhdk1? NYTBeFd6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
SNU-1 NH;2fY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoroTWM2OD1|NUSgcm0> NI\6WIQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
HOP62 NIrZfZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPzfWpQUUN3ME22O|Yhdk1? NXX3WlNCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
H23 NF7sfZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULjO2x5UUN3ME2xNFAxKG6P NUXoWFc4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
MB-231 NH[xXHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlS0TWM2OD1zMECwJI5O MlHTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
SU.86.86 NU\J[GszT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETq[5pKSzVyPUGwNFEhdk1? M2fsXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
CFPAC-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInNc2FKSzVyPUGwNFEhdk1? NFXaSHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
A427 M{XMbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XqRmlEPTB;MUSzN{BvVQ>? NIryXY09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
MDAH-2774 NWTJ[INWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnt[ndKSzVyPUK2OVchdk1? NXq3VGc5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
NCI-H157 NUDsWHZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvvTWM2OD1|MECwJI5O MlvlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
HTB-177 NHfJcnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV:5RZNLUUN3ME2zNFAxKG6P M1;5T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
UM-UC-3 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTNyMEGgcm0> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
HCT-8 M2S0WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\mPVh6UUN3ME2zNFAyKG6P MmHtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
Panc-1 MonHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7HZVlKSzVyPUOwNFEhdk1? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
DLD-1 MkfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDJdJdrUUN3ME2zNFAyKG6P NXnTeHM3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
HCT-15 NVjx[GMzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Oy[GlEPTB;M{CwNUBvVQ>? MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
HL-60 NYPwfYJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTNyIH7N MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
SK-Mel-2 NWj2c|F3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVX2fZRLUUN3ME2zOEBvVQ>? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
RD MkTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7M[YdKSzVyPUGyN{BvVQ>? MoHpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
HT-1197 NV3nN4RxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTNzNjDuUS=> MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
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... 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
In vivo SCH772984 induces tumor regressions in xenograft models at tolerated doses. SCH772984 effectively inhibites MAPK signaling and cell proliferation in BRAF or MEK inhibitor resistant models. [1]

Protocol

Kinase Assay:

[1]

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ERK2 IMAP enzymatic assay:

SCH772984 is tested in 8 point dilution curves in duplicate against purified ERK2 or ERK1. The enzyme is added to the reaction plate. and incubated with the compound before adding a solution of substrate peptide and ATP. 14μl of diluted enzyme (0.3ng active ERK2 per reaction) is added to each well of a 384-well plate. The plates are gently shaken to mix the reagents and incubated for 45 minutes at room temperature. The reaction is stopped with 60μl of IMAP Binding Solution (1:2200 dilutions of IMAP beads in 1X Binding Buffer). The plates are incubated at room temperature for an additional 0.5 hours to allow complete binding of phosphopeptides to the IMAP beads. Plates are read on the LJL Analyst.
Cell Research:

[1]

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  • Cell lines: BRAF-mutant or RAS-mutant tumor lines
  • Concentrations: ~10 μM
  • Incubation Time: 5 days
  • Method:

    Cell proliferation experiments are performed in a 96-well format (six replicates), and cells are plated at 4,000/well density. At 24 h after cell seeding, cells are treated with DMSO or 9 point IC50 dilution (0.001-10 μM) at 1% DMSO final for all concentrations. Viability is assayed on 5 days after dosing using ViaLight luminescence kit following the manufacturer’s recommendations. For cell line panel viability assay, cells are treated with SCH772984 for 4 days and assayed by CellTiterGlo luminescent cell viability assay.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Nude mice
  • Dosages: 12.5 mg/kg, 25 mg/kg, 50 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 14 mg/mL warmed (23.82 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.
0.6mg/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 587.67
Formula

C33H33N9O2

CAS No. 942183-80-4
Storage powder
in solvent
Synonyms N/A
Smiles C1CN(CC1C(=O)NC2=CC3=C(C=C2)NN=C3C4=CC=NC=C4)CC(=O)N5CCN(CC5)C6=CC=C(C=C6)C7=NC=CC=N7

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • 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

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 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?

  • Answer:

    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