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

  • 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.

    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.

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 NFnYR5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rQ[mlEPTB;MD6yOEBvVQ>? NW\pUFFuOjV|NUC5N|E>
WM-266-4 MnfzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnzJTWM2OD1{MDDuUS=> NF7kPGIzOzZzNEi5PC=>
UACC-62 M3eyTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTNyIH7N NYrtdYRTOjN4MUS4PVg>
Colo-205 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEn5bXdKSzVyPUO2JI5O Mke4NlM3OTR6OUi=
SK-Mel-1 NELhfolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LpRWlEPTB;M{egcm0> MXuyN|YyPDh7OB?=
WiDr NGrkVHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XmbmlEPTB;M{mgcm0> NXvEUY8{OjN4MUS4PVg>
M14 MoTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLvWFRLUUN3ME20O{BvVQ>? M{O4OVI{PjF2OEm4
HT-29 M4jrd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjSPWFqUUN3ME21NEBvVQ>? Mnz4NlM3OTR6OUi=
8505C MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTVyIH7N MYmyN|YyPDh7OB?=
HT-144 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LiUWlEPTB;NkCgcm0> NInRTpMzOzZzNEi5PC=>
SK-Mel-5 NH;KPZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHqzRndKSzVyPU[2JI5O MlHVNlM3OTR6OUi=
A375-SM M4XUO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTNVXZKSzVyPUe1JI5O M1LSc|I{PjF2OEm4
SK-Mel-28 MljTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4ruOGlEPTB;OEWgcm0> MXOyN|YyPDh7OB?=
LOX NGLvZVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTFyMDDuUS=> NXLKPYpWOjN4MUS4PVg>
SK-Mel-3 NFHhXVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4n4RWlEPTB;MUG4JI5O NHfu[ZUzOzZzNEi5PC=>
K1 M4i0V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvwN|FKSzVyPUGzNEBvVQ>? M2XDclI{PjF2OEm4
Hs-695T M4LqZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX:1RY5wUUN3ME2xOlUhdk1? M3fqSlI{PjF2OEm4
BHT-101 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\nOXVKSzVyPUOwNEBvVQ>? MmrPNlM3OTR6OUi=
RPMI-7951 M1vI[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HmXmlEPTB;M{S0JI5O NEfaSHYzOzZzNEi5PC=>
A2058 MnW2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13T[mlEPTB;M{[wJI5O MXmyN|YyPDh7OB?=
SK-Hep-1 M{W1XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\2TWM2OD1zNEKyJI5O NEXLTIgzOzZzNEi5PC=>
A673 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlW1TWM2OD1|MECxJI5O NIDsTnQzOzZzNEi5PC=>
DBTRG-05MG M4Lr[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\ZTWM2OD1|MECxJI5O MV6yN|YyPDh7OB?=
SW-626 NIGxeY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDkOHZ4UUN3ME2zN{BvVQ>? M{XRUlI{PjF2OEm4
LoVo M2rIS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTR5IH7N M37sc|I{PjF2OEm4
MiaPaCa Ml3zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWm4SmwzUUN3ME21N{BvVQ>? MWmyN|YyPDh7OB?=
SW-620 NVnMZpFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPhTWM2OD1zMESgcm0> NXXZ[Y1pOjN4MUS4PVg>
CAPAN-1 M161W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzxUolEUUN3ME2xNFQhdk1? MlWwNlM3OTR6OUi=
SW-527 NVzYV4FJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHn0XopKSzVyPUGyNUBvVQ>? NHTh[WEzOzZzNEi5PC=>
HCT-116 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU[2d5VqUUN3ME2xNlghdk1? M{jQc|I{PjF2OEm4
SW-480 M2LqV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTF4NTDuUS=> M4\kZlI{PjF2OEm4
HPAC MnTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEm1OmlKSzVyPUG3NEBvVQ>? NEXFXnEzOzZzNEi5PC=>
OVCAR-5 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\aTWM2OD1{MEigcm0> M3;lcFI{PjF2OEm4
AsPc-1 NW\FSJhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTJ5MDDuUS=> NFzsVZYzOzZzNEi5PC=>
A549 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LscGlEPTB;M{K2JI5O NX7IT4VZOjN4MUS4PVg>
SNU-1 M4XWWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfhNHdHUUN3ME2zOVQhdk1? MYCyN|YyPDh7OB?=
HOP62 M1f6Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnqSHJKSzVyPU[3OkBvVQ>? MYiyN|YyPDh7OB?=
H23 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\obZBKSzVyPUGwNFAhdk1? M3XWcFI{PjF2OEm4
MB-231 Mk\JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTFyMECgcm0> MoW2NlM3OTR6OUi=
SU.86.86 NFK0UGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1X6fGlEPTB;MUCwNUBvVQ>? NGOxVVEzOzZzNEi5PC=>
CFPAC-1 NFTxOINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzOTWM2OD1zMECxJI5O NX3D[5lVOjN4MUS4PVg>
A427 M1rGS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV36Z41yUUN3ME2xOFM{KG6P NH\LO3IzOzZzNEi5PC=>
MDAH-2774 NWDidZh6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTJ4NUegcm0> NWf3Rpc{OjN4MUS4PVg>
NCI-H157 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nZeWlEPTB;M{CwNEBvVQ>? NEi4PVEzOzZzNEi5PC=>
HTB-177 MoTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTNyMECgcm0> M1fiNVI{PjF2OEm4
UM-UC-3 NUTqN5gxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{H1ZWlEPTB;M{CwNUBvVQ>? NIXMWXYzOzZzNEi5PC=>
HCT-8 NGTVflBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLmclVKSzVyPUOwNFEhdk1? NUH4SpVHOjN4MUS4PVg>
Panc-1 MorxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTNyMEGgcm0> MlrTNlM3OTR6OUi=
DLD-1 M2PIXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnz2TWM2OD1|MECxJI5O M2Dxe|I{PjF2OEm4
HCT-15 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHi5fo1KSzVyPUOwNFEhdk1? MoDONlM3OTR6OUi=
HL-60 NGq3NpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[xe4JqUUN3ME2zNEBvVQ>? MoHmNlM3OTR6OUi=
SK-Mel-2 MlTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTN2IH7N MXqyN|YyPDh7OB?=
RD MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTF{MzDuUS=> Mk\1NlM3OTR6OUi=
HT-1197 NYLIUnFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTNzNjDuUS=> M2PFV|I{PjF2OEm4
Molt-3 M2TlOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXpcYFXUUN3ME22NFAhdk1? M4T3T|I{PjF2OEm4
PA-1 M4nHOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTFyMEGgcm0> MkD5NlM3OTR6OUi=
Molt-4 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYPJR|UxRTNyMEGgcm0> MX:yN|YyPDh7OB?=
NCI-H292 NVP3bo5NT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHYTWM2OD17MDDuUS=> NF\mXGIzOzZzNEi5PC=>
A2780 NULvSlduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Lq[mlEPTB;MUSzJI5O NVj5PItoOjN4MUS4PVg>
IGROV-1 NFLyXZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NED2RYpKSzVyPUG0OkBvVQ>? NVqxemtSOjN4MUS4PVg>
SK-N-SH Mnv5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTF3MDDuUS=> MmWyNlM3OTR6OUi=
N-87 NFfUNHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nhZ2lEPTB;M{C3JI5O NE\tU|QzOzZzNEi5PC=>
H322 NHWx[oNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTN{NTDuUS=> M4X1VVI{PjF2OEm4
H716 NXLjfHI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTN|NDDuUS=> MkG3NlM3OTR6OUi=
TT NIDzRZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYKzS5hmUUN3ME20NFYhdk1? M4SzXVI{PjF2OEm4
Caki-1 Mo\RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTYPIZmUUN3ME20OVAhdk1? MUmyN|YyPDh7OB?=
5637 NHG5RXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnvqTWM2OD14MUCgcm0> NYK2T|ROOjN4MUS4PVg>
MB-453 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTuTWM2OD14N{Kgcm0> MV2yN|YyPDh7OB?=
RT-4 NVTaWFlUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mof3TWM2OD16MUCgcm0> M4Hlc|I{PjF2OEm4
HOP92 NVLDcGRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHX3TWFKSzVyPUiyNEBvVQ>? MYCyN|YyPDh7OB?=
KG-1 MlXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7Sc2FKSzVyPUmwNEBvVQ>? NHLaOXEzOzZzNEi5PC=>
Hs-294T NX;ZenBrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17qV2lEPTB;OUS1JI5O M2LOOlI{PjF2OEm4
SF-539 MmXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITqS5hKSzVyPUGwNFAhdk1? Mn7CNlM3OTR6OUi=
U-251 NUfGblZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV7HSJl{UUN3ME2xNFAxKG6P NE\WOY4zOzZzNEi5PC=>
MB-468 M4TIXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NED5eY5KSzVyPUGwNFAhdk1? MmfwNlM3OTR6OUi=
HS746T MknSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1S4O2lEPTB;MUCwNEBvVQ>? MWSyN|YyPDh7OB?=
SCABER M3fPOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlywTWM2OD1zMECwJI5O Ml7rNlM3OTR6OUi=
MCF-7 NIj6[WNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mkf5TWM2OD1zMECxJI5O MoHWNlM3OTR6OUi=
CHL-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfLTWM2OD1zNE[wJI5O MoryNlM3OTR6OUi=
U87MG NIS2eYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1T6e2lEPTB;MkCwNEBvVQ>? NELufHIzOzZzNEi5PC=>
SJCRH30 Mlu1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTJyMEKgcm0> NIXBSZMzOzZzNEi5PC=>
ES-2 NETmcGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLiTWM2OD1{NkW5JI5O NYLD[|F5OjN4MUS4PVg>
HT-1376 M2fDeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTJ6MECgcm0> NFPRd2kzOzZzNEi5PC=>
A172 NYHIb4FrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jNNmlEPTB;M{CwNEBvVQ>? M{naXVI{PjF2OEm4
769P M4jEUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHzU|ZIUUN3ME2zNFAxKG6P NUXqXJlpOjN4MUS4PVg>
NCI-H520 NEO0ZWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTNyMECgcm0> NVrqPZhHOjN4MUS4PVg>
DU145 M{LFXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PDOGlEPTB;M{CwNEBvVQ>? M2j0W|I{PjF2OEm4
K562 NV6xUWN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTNyMECgcm0> NWLpV3hjOjN4MUS4PVg>
U-937 NETMc2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33MXWlEPTB;M{CwNEBvVQ>? NVfvcIJrOjN4MUS4PVg>
A204 NUTzVGk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LtPWlEPTB;M{CwNUBvVQ>? MkfZNlM3OTR6OUi=
DAOY M{PEUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInNXolKSzVyPUOwNFEhdk1? NGXhWVQzOzZzNEi5PC=>
SF-268 NFzr[XZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTNNok{UUN3ME2zNFAyKG6P Ml\JNlM3OTR6OUi=
SF-295 MlrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTNyMEGgcm0> NXy2XpdrOjN4MUS4PVg>
SNB-19 M4PrV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3u4ZWlEPTB;M{CwNUBvVQ>? NGDXfHIzOzZzNEi5PC=>
SNB-75 NIPre3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTBTWM2OD1|MECxJI5O M2fpR|I{PjF2OEm4
U373-MG NXWxV3NqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\Rd2lEPTB;M{CwNUBvVQ>? Mo\uNlM3OTR6OUi=
786-O MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{faRmlEPTB;M{CwNUBvVQ>? NWD3NFhTOjN4MUS4PVg>
A498 MmLFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTNyMEGgcm0> MkP0NlM3OTR6OUi=
ACHN MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXq2dFFzUUN3ME2zNFAyKG6P M4TvUlI{PjF2OEm4
EKVX MlnSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTNyMEGgcm0> NEm3TGszOzZzNEi5PC=>
H226 NHjnbohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDpTWM2OD1|MECxJI5O M1LoZlI{PjF2OEm4
H522 M2e1S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmTDTWM2OD1|MECxJI5O M36wSFI{PjF2OEm4
HeLa NY\Me4tUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFTmWlhKSzVyPUOwNFEhdk1? M1LHdFI{PjF2OEm4
SK-OV-3 Mm\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\qTWM2OD1|MECxJI5O NVr6VGE5OjN4MUS4PVg>
Ln Cap NFu1dmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3BTWM2OD1|MECxJI5O MnnwNlM3OTR6OUi=
PC3 NHvhc5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTNyMEGgcm0> NUTVc4FxOjN4MUS4PVg>
SNU-16 NV;4co51T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVj5dlM5UUN3ME2zNFAyKG6P MlrHNlM3OTR6OUi=
FTC-133 NEXuXplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTNyMEGgcm0> MmX0NlM3OTR6OUi=
Ro82-W-1 NFTiXZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;neGlEPTB;M{CwNUBvVQ>? MljjNlM3OTR6OUi=
Daudi NESxb3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7rXpV5UUN3ME2zNFAyKG6P NVnHToFwOjN4MUS4PVg>
Jijoye NYDObnBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHCTWM2OD1|MECxJI5O M2\FblI{PjF2OEm4
Jurkat MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLlenVRUUN3ME2zNFAyKG6P NWT5SlZHOjN4MUS4PVg>
J-82 NUS2[nhDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTNyMEGgcm0> NGHNSZEzOzZzNEi5PC=>
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... Click to View More Cell Line Experimental Data

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]

+ 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)

  • 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