SCH772984

Catalog No.S7101

SCH772984 Chemical Structure

Molecular Weight(MW): 587.67

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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Cited by 15 Publications

5 Customer Reviews

  • K562 cells were exposed to ERK inhibitor SCH772984 (1 uM, 2 uM, 5 uM) for 48 h. Apoptosis was analyzed by Annexin V-APC labeling.

    Leuk Lymphoma 2014 1, 8. SCH772984 purchased from Selleck.

  • ERK1/2 influences the effects of TGF-β1 on Cdk5 and Bax in PC12 cells. A. Original western blot showing the level of Cdk5 and respective Actin in PC12 cells with TGF-β1 (40 ng/ml) treatment in the presence of SCH772984(1 μM) and LY294002(1.5 μM) for 2 h. B. Arithmetic means ± SEM (n = 4) of Cdk5 protein abundance in PC12 cells with TGF-β1 treatment in the presence of SCH772984(1 μM) and LY294002(1.5 μM) for 2 h. C. Original western blot showing the level of Bax and respective Actin in PC12 cells with TGF-β1 (40 ng/ml) treatment in the presence of SCH772984(1 μM) for 2 h. D. Arithmetic means ± SEM (n = 4) of Bax protein abundance in PC12 cells with TGF-β1 treatment in the presence of SCH772984(1 μM) for 2 h. **(p < 0.01), ***(p < 0.001) indicate statistically significant difference.

    Biochem Biophys Res Commun, 2017, 485(4):775-781. SCH772984 purchased from Selleck.

  • Immunoblot of H23 cells treated with trametinib (25 nM), SCH772984 (500 nM), or their combination for the times shown.

    Nature, 2016, 534(7609):647-51. SCH772984 purchased from Selleck.

  • 293T cells were transfected with Flag-WT-FBW7. Thirty hours post transfection, cells were pretreated with MG132 and various MEK/ERK inhibitors overnight before harvesting. FBW7 phosphorylation status was examined by immunoblot analysis after immunoprecipitation.

    Cell Research, 2015, 25: 561-573. SCH772984 purchased from Selleck.

  • Int J Oncol, 2018, 53(2):750-760. SCH772984 purchased from Selleck.

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 NGTOXJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlnzTWM2OD1yLkK0JI5O M1rifFI2OzVyOUOx
WM-266-4 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTJyIH7N M3W1fVI{PjF2OEm4
UACC-62 M1zBVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnL2TWM2OD1|MDDuUS=> MkL2NlM3OTR6OUi=
Colo-205 NGXUdJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nIb2lEPTB;M{[gcm0> NYXhZ3ZVOjN4MUS4PVg>
SK-Mel-1 NULU[nRKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2SxeGlEPTB;M{egcm0> NFHsV5AzOzZzNEi5PC=>
WiDr MlfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrifXhKSzVyPUO5JI5O MYeyN|YyPDh7OB?=
M14 M4q1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTR5IH7N M1XyWlI{PjF2OEm4
HT-29 M1HLcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTVyIH7N MVqyN|YyPDh7OB?=
8505C MmTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jpNWlEPTB;NUCgcm0> NIDuWmUzOzZzNEi5PC=>
HT-144 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2e0[WlEPTB;NkCgcm0> Mn3rNlM3OTR6OUi=
SK-Mel-5 NEfrTnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3[3NWlEPTB;Nk[gcm0> MoL1NlM3OTR6OUi=
A375-SM MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWi0WWQ4UUN3ME23OUBvVQ>? NIm1eYYzOzZzNEi5PC=>
SK-Mel-28 Mn:4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHvTWM2OD16NTDuUS=> M4nO[lI{PjF2OEm4
LOX MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIC3VnBKSzVyPUGwNEBvVQ>? NXHsc3h4OjN4MUS4PVg>
SK-Mel-3 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NViwbnIzUUN3ME2xNVghdk1? MkHkNlM3OTR6OUi=
K1 M{KxfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjnOIZPUUN3ME2xN|Ahdk1? NGLo[ZczOzZzNEi5PC=>
Hs-695T NH35dnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\DVJlKSzVyPUG2OUBvVQ>? NUe2VII{OjN4MUS4PVg>
BHT-101 NVnidGt7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTNyMDDuUS=> Moj6NlM3OTR6OUi=
RPMI-7951 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\zUmZRUUN3ME2zOFQhdk1? MWSyN|YyPDh7OB?=
A2058 MlKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHNTJdpUUN3ME2zOlAhdk1? MWKyN|YyPDh7OB?=
SK-Hep-1 NX;WS|JkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4K2RWlEPTB;MUSyNkBvVQ>? M{LIT|I{PjF2OEm4
A673 NIO4UlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2SzcmlEPTB;M{CwNUBvVQ>? Mlf2NlM3OTR6OUi=
DBTRG-05MG M2nTW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnyPFRKSzVyPUOwNFEhdk1? MUOyN|YyPDh7OB?=
SW-626 Moj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDD[|dQUUN3ME2zN{BvVQ>? M4nFSlI{PjF2OEm4
LoVo MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrxU3NKSzVyPUS3JI5O NXLZ[GNlOjN4MUS4PVg>
MiaPaCa MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLvS5lKSzVyPUWzJI5O MUWyN|YyPDh7OB?=
SW-620 NVLQbZloT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofJTWM2OD1zMESgcm0> NH:4bZIzOzZzNEi5PC=>
CAPAN-1 NYPuZ21wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEe0OYpKSzVyPUGwOEBvVQ>? M4XyeVI{PjF2OEm4
SW-527 NXnYRlhPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrNW45KSzVyPUGyNUBvVQ>? NIrJeFczOzZzNEi5PC=>
HCT-116 NWfaV4wxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfydGNKSzVyPUGyPEBvVQ>? M3LYW|I{PjF2OEm4
SW-480 NIm2WnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTmTWM2OD1zNkWgcm0> MnjkNlM3OTR6OUi=
HPAC MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrvTWM2OD1zN{Cgcm0> NHXmT5EzOzZzNEi5PC=>
OVCAR-5 NEfTXGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTJyODDuUS=> MnmyNlM3OTR6OUi=
AsPc-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX33eIs1UUN3ME2yO|Ahdk1? NVTxXlZYOjN4MUS4PVg>
A549 NWTPOGtYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3e5TmlEPTB;M{K2JI5O MnrXNlM3OTR6OUi=
SNU-1 NXzBT3FHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTN3NDDuUS=> M{L0NVI{PjF2OEm4
HOP62 NVnuS5VDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTZ5NjDuUS=> NWL3SZhzOjN4MUS4PVg>
H23 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrHTWM2OD1zMECwJI5O NHjtOlMzOzZzNEi5PC=>
MB-231 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXnR3lYUUN3ME2xNFAxKG6P MoHlNlM3OTR6OUi=
SU.86.86 NUC1UW1qT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVS0eWtwUUN3ME2xNFAyKG6P MVWyN|YyPDh7OB?=
CFPAC-1 MoDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYezOGlnUUN3ME2xNFAyKG6P M3:5UFI{PjF2OEm4
A427 MnzjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DaWmlEPTB;MUSzN{BvVQ>? NUHQc2tiOjN4MUS4PVg>
MDAH-2774 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkD5TWM2OD1{NkW3JI5O M3G0[|I{PjF2OEm4
NCI-H157 MkXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvKc4x3UUN3ME2zNFAxKG6P M{XTXFI{PjF2OEm4
HTB-177 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TLU2lEPTB;M{CwNEBvVQ>? M1e1UFI{PjF2OEm4
UM-UC-3 NYPQbG9TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYizT5dwUUN3ME2zNFAyKG6P NXzafVFUOjN4MUS4PVg>
HCT-8 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrmVpRCUUN3ME2zNFAyKG6P NYewUZFROjN4MUS4PVg>
Panc-1 NEXZb|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17KTGlEPTB;M{CwNUBvVQ>? Mom3NlM3OTR6OUi=
DLD-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXG4fnZLUUN3ME2zNFAyKG6P M3nJPFI{PjF2OEm4
HCT-15 NWrrWGdXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUj5dphEUUN3ME2zNFAyKG6P NYTEWmdMOjN4MUS4PVg>
HL-60 M4HTXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYf4bYtEUUN3ME2zNEBvVQ>? NUXnVnJTOjN4MUS4PVg>
SK-Mel-2 M{TZS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXsTWM2OD1|NDDuUS=> MVeyN|YyPDh7OB?=
RD Mlu2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTF{MzDuUS=> MnPVNlM3OTR6OUi=
HT-1197 M3LmbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTNzNjDuUS=> Mn\ONlM3OTR6OUi=
Molt-3 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HJfWlEPTB;NkCwJI5O NIDvWWwzOzZzNEi5PC=>
PA-1 M{e0[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2Dv[WlEPTB;MUCwNUBvVQ>? M2nYcVI{PjF2OEm4
Molt-4 NVnTZ5JvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHT2U5BKSzVyPUOwNFEhdk1? MonPNlM3OTR6OUi=
NCI-H292 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTlyIH7N MX:yN|YyPDh7OB?=
A2780 MlLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfnPItKSzVyPUG0N{BvVQ>? M3KzUlI{PjF2OEm4
IGROV-1 Mn3QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmL1TWM2OD1zNE[gcm0> MnvoNlM3OTR6OUi=
SK-N-SH MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PKRmlEPTB;MUWwJI5O Mn;1NlM3OTR6OUi=
N-87 MmDpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnNdo5DUUN3ME2zNFchdk1? NHXTVGYzOzZzNEi5PC=>
H322 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1zI[GlEPTB;M{K1JI5O NVXyTplVOjN4MUS4PVg>
H716 M{fyXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWn4[FUzUUN3ME2zN|Qhdk1? MkDBNlM3OTR6OUi=
TT NULBUoU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\o[ZlKSzVyPUSwOkBvVQ>? M2PSZVI{PjF2OEm4
Caki-1 NWHHT49ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\sdWlEPTB;NEWwJI5O NVTzTHB5OjN4MUS4PVg>
5637 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3yxN2lEPTB;NkGwJI5O MlPRNlM3OTR6OUi=
MB-453 NUnTblhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHf5fpZKSzVyPU[3NkBvVQ>? MWGyN|YyPDh7OB?=
RT-4 NYjtfZF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUL6b291UUN3ME24NVAhdk1? NEjMcVUzOzZzNEi5PC=>
HOP92 NE[4bHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorNTWM2OD16MkCgcm0> Mo\5NlM3OTR6OUi=
KG-1 M2\KN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPnWo9KSzVyPUmwNEBvVQ>? NGPiSlMzOzZzNEi5PC=>
Hs-294T MorOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzNe4VkUUN3ME25OFUhdk1? NHXoPY8zOzZzNEi5PC=>
SF-539 NH3iZYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnCOHZKSzVyPUGwNFAhdk1? MY[yN|YyPDh7OB?=
U-251 NX33Z4dUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTFyMECgcm0> M4\tWlI{PjF2OEm4
MB-468 M4DQZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTFyMECgcm0> NYXYeox5OjN4MUS4PVg>
HS746T NUH6UpVJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFiyfZVKSzVyPUGwNFAhdk1? MkLhNlM3OTR6OUi=
SCABER MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3HmbmlEPTB;MUCwNEBvVQ>? M2f2[FI{PjF2OEm4
MCF-7 NXvoWVNZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXLTWM2OD1zMECxJI5O M2r2Z|I{PjF2OEm4
CHL-1 NEnNW3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnRN2ozUUN3ME2xOFYxKG6P NFj3S|AzOzZzNEi5PC=>
U87MG MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHH1UZdKSzVyPUKwNFAhdk1? M3jS[VI{PjF2OEm4
SJCRH30 NVnqeFNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWW0Ro45UUN3ME2yNFAzKG6P MoXtNlM3OTR6OUi=
ES-2 NX7jfWI{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmriTWM2OD1{NkW5JI5O NXftR3VFOjN4MUS4PVg>
HT-1376 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDkWotKSzVyPUK4NFAhdk1? NYn4XZBkOjN4MUS4PVg>
A172 NH;nTYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTwTWM2OD1|MECwJI5O NULPPJh{OjN4MUS4PVg>
769P MoO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTNyMECgcm0> NWjFbFdvOjN4MUS4PVg>
NCI-H520 MkC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjFVJpKSzVyPUOwNFAhdk1? NWDzO2tVOjN4MUS4PVg>
DU145 MmHyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV3JR|UxRTNyMECgcm0> NWrHW|ZHOjN4MUS4PVg>
K562 MoLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fxZmlEPTB;M{CwNEBvVQ>? NFPYSlkzOzZzNEi5PC=>
U-937 NE\5cGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTNyMECgcm0> Mn;pNlM3OTR6OUi=
A204 M4L1fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjmOpRKSzVyPUOwNFEhdk1? NVnoVYRwOjN4MUS4PVg>
DAOY NG[zeGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfvSXh6UUN3ME2zNFAyKG6P M2XyZVI{PjF2OEm4
SF-268 NV;xfHhjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M134TmlEPTB;M{CwNUBvVQ>? NGnRU5IzOzZzNEi5PC=>
SF-295 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHv6S4ZKSzVyPUOwNFEhdk1? MkXNNlM3OTR6OUi=
SNB-19 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4\hNmlEPTB;M{CwNUBvVQ>? MmXnNlM3OTR6OUi=
SNB-75 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVL6TWpjUUN3ME2zNFAyKG6P MkXSNlM3OTR6OUi=
U373-MG NUHzSoFLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17pWmlEPTB;M{CwNUBvVQ>? NFruZ2IzOzZzNEi5PC=>
786-O M1TGfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7LOpJKSzVyPUOwNFEhdk1? MViyN|YyPDh7OB?=
A498 M1n2NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjVeWNWUUN3ME2zNFAyKG6P MUiyN|YyPDh7OB?=
ACHN M4\Ye2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXPeoRiUUN3ME2zNFAyKG6P NYPCR2VOOjN4MUS4PVg>
EKVX NIrXepFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHp[|Y2UUN3ME2zNFAyKG6P MWSyN|YyPDh7OB?=
H226 MmHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfvUpZKSzVyPUOwNFEhdk1? NGr1TnIzOzZzNEi5PC=>
H522 M{XyWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\xOGlEPTB;M{CwNUBvVQ>? M4HlTFI{PjF2OEm4
HeLa MmTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jWTGlEPTB;M{CwNUBvVQ>? MmDXNlM3OTR6OUi=
SK-OV-3 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnrTWM2OD1|MECxJI5O NGT0dlMzOzZzNEi5PC=>
Ln Cap NX[1OJdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTQTWM2OD1|MECxJI5O MmDGNlM3OTR6OUi=
PC3 NG\2WHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX35cGwyUUN3ME2zNFAyKG6P Mn7HNlM3OTR6OUi=
SNU-16 M3qy[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHDVXczUUN3ME2zNFAyKG6P NXWxVFRQOjN4MUS4PVg>
FTC-133 M3XsdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHxbZpKSzVyPUOwNFEhdk1? NVv3[pJLOjN4MUS4PVg>
Ro82-W-1 NHnufFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDNSo1KSzVyPUOwNFEhdk1? M3XTNVI{PjF2OEm4
Daudi M4HzZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1O4WGlEPTB;M{CwNUBvVQ>? NV;Hb4tlOjN4MUS4PVg>
Jijoye MnmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTNyMEGgcm0> MV6yN|YyPDh7OB?=
Jurkat M13PWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTNyMEGgcm0> NFWzNZozOzZzNEi5PC=>
J-82 M4m1b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;QR4NLUUN3ME2zNFAyKG6P NGnNXWczOzZzNEi5PC=>
TCC-SUP NGDrRmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTNyMEGgcm0> MUOyN|YyPDh7OB?=
BT-474 NHLNdpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfnTWM2OD1|MECxJI5O NF21TYkzOzZzNEi5PC=>
ZR-75-1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTNyMEGgcm0> M{H3e|I{PjF2OEm4

... 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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • Animal Models: Nude mice
  • Formulation: --
  • 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

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 (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*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
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    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):
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    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.

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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