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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3 Customer Reviews

  • 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.

    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.. 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 MkPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLNTWM2OD1yLkK0JI5O NVLHdHFnOjV|NUC5N|E>
WM-266-4 NEP2OYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XFNWlEPTB;MkCgcm0> NVHyeZp{OjN4MUS4PVg>
UACC-62 NGnrdW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPRZ5o4UUN3ME2zNEBvVQ>? NYnRc4xyOjN4MUS4PVg>
Colo-205 M3;seGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHRR|lzUUN3ME2zOkBvVQ>? M3f0S|I{PjF2OEm4
SK-Mel-1 M{fmV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGW4WGdKSzVyPUO3JI5O MkHWNlM3OTR6OUi=
WiDr M3GwfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUL3dWRWUUN3ME2zPUBvVQ>? MmjhNlM3OTR6OUi=
M14 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnZToRKSzVyPUS3JI5O Ml\1NlM3OTR6OUi=
HT-29 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrsXXpKSzVyPUWwJI5O MkDnNlM3OTR6OUi=
8505C MkW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4S4UGlEPTB;NUCgcm0> NEPabXMzOzZzNEi5PC=>
HT-144 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2e3TGlEPTB;NkCgcm0> NEPrbY8zOzZzNEi5PC=>
SK-Mel-5 NGfRUIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTZ4IH7N NULiPFREOjN4MUS4PVg>
A375-SM NFHHboVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjWRmFKSzVyPUe1JI5O NEDtTWUzOzZzNEi5PC=>
SK-Mel-28 Mm\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jKVmlEPTB;OEWgcm0> MVuyN|YyPDh7OB?=
LOX NXf5TmVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHlPJJKSzVyPUGwNEBvVQ>? NVfuV5NJOjN4MUS4PVg>
SK-Mel-3 NELTSnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrieItKSzVyPUGxPEBvVQ>? Ml7ENlM3OTR6OUi=
K1 NIfCWGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWS1[|AyUUN3ME2xN|Ahdk1? M1;EbFI{PjF2OEm4
Hs-695T M3PySWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXiSIdCUUN3ME2xOlUhdk1? M3y2XFI{PjF2OEm4
BHT-101 MmjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPBVoZKSzVyPUOwNEBvVQ>? MkexNlM3OTR6OUi=
RPMI-7951 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFyxe|BKSzVyPUO0OEBvVQ>? NInwWGwzOzZzNEi5PC=>
A2058 NH\LNGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTN4MDDuUS=> NHzZNmIzOzZzNEi5PC=>
SK-Hep-1 NVmw[Y03T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvESFNKSzVyPUG0NlIhdk1? NXfGV4lHOjN4MUS4PVg>
A673 NVPiPFc1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTNyMEGgcm0> NXzoTHJkOjN4MUS4PVg>
DBTRG-05MG M{ezRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTOTWM2OD1|MECxJI5O MkfLNlM3OTR6OUi=
SW-626 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTN|IH7N M2jT[VI{PjF2OEm4
LoVo Mo\aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTNTWM2OD12NzDuUS=> NV;ke|Q2OjN4MUS4PVg>
MiaPaCa M3jC[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTV|IH7N NEXwU|EzOzZzNEi5PC=>
SW-620 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1frWWlEPTB;MUC0JI5O MlrJNlM3OTR6OUi=
CAPAN-1 MnvyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;3UmFVUUN3ME2xNFQhdk1? MViyN|YyPDh7OB?=
SW-527 M4\YUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHvTWM2OD1zMkGgcm0> MUSyN|YyPDh7OB?=
HCT-116 M3L0U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYji[IpWUUN3ME2xNlghdk1? MUSyN|YyPDh7OB?=
SW-480 M1jlfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofzTWM2OD1zNkWgcm0> MkjVNlM3OTR6OUi=
HPAC NEXHXGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;IfJRKSzVyPUG3NEBvVQ>? NGHBZW4zOzZzNEi5PC=>
OVCAR-5 NXHiTVNMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn23TWM2OD1{MEigcm0> MXiyN|YyPDh7OB?=
AsPc-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3npbGlEPTB;MkewJI5O M1jMZlI{PjF2OEm4
A549 M3LOXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;2T2lEPTB;M{K2JI5O NYH5OVVLOjN4MUS4PVg>
SNU-1 MnvuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1H3N2lEPTB;M{W0JI5O M2PnN|I{PjF2OEm4
HOP62 M{K0RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfaTWM2OD14N{[gcm0> NUDDeJhxOjN4MUS4PVg>
H23 Mm\LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTFyMECgcm0> NYHRZ3hsOjN4MUS4PVg>
MB-231 NEjoN4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjtPYpXUUN3ME2xNFAxKG6P MVqyN|YyPDh7OB?=
SU.86.86 NFzFeZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XkTmlEPTB;MUCwNUBvVQ>? NV\DVmN2OjN4MUS4PVg>
CFPAC-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTFyMEGgcm0> Mnm2NlM3OTR6OUi=
A427 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWKxflZHUUN3ME2xOFM{KG6P NWH4W2wyOjN4MUS4PVg>
MDAH-2774 NXXpOGo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13m[2lEPTB;Mk[1O{BvVQ>? MmrQNlM3OTR6OUi=
NCI-H157 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\J[mlEPTB;M{CwNEBvVQ>? MWGyN|YyPDh7OB?=
HTB-177 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfrTpA2UUN3ME2zNFAxKG6P M3PiXVI{PjF2OEm4
UM-UC-3 MmjES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPJblN5UUN3ME2zNFAyKG6P NWLENJR2OjN4MUS4PVg>
HCT-8 Mn7SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLDbFdHUUN3ME2zNFAyKG6P MkLyNlM3OTR6OUi=
Panc-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYWx[XB5UUN3ME2zNFAyKG6P MX2yN|YyPDh7OB?=
DLD-1 M{H3ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HsTGlEPTB;M{CwNUBvVQ>? MonTNlM3OTR6OUi=
HCT-15 M3TDfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTNyMEGgcm0> NIXFdGkzOzZzNEi5PC=>
HL-60 NIXudWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTpTWM2OD1|MDDuUS=> Ml7JNlM3OTR6OUi=
SK-Mel-2 NYDlNZRMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmP2TWM2OD1|NDDuUS=> NFewblkzOzZzNEi5PC=>
RD MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TQNGlEPTB;MUKzJI5O M1fWNVI{PjF2OEm4
HT-1197 NEnJcZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\5fINXUUN3ME2zNVYhdk1? MlXGNlM3OTR6OUi=
Molt-3 MnnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTZyMDDuUS=> NVTyRnBxOjN4MUS4PVg>
PA-1 NWjEVIRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTDTWM2OD1zMECxJI5O NYm2SZlUOjN4MUS4PVg>
Molt-4 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PhUGlEPTB;M{CwNUBvVQ>? MXqyN|YyPDh7OB?=
NCI-H292 NEixfldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF61cHlKSzVyPUmwJI5O NIfGXpMzOzZzNEi5PC=>
A2780 M130c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zvZmlEPTB;MUSzJI5O M{LDWVI{PjF2OEm4
IGROV-1 NFfKXVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWrJR|UxRTF2NjDuUS=> NVLSOHRyOjN4MUS4PVg>
SK-N-SH M1KyUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTF3MDDuUS=> NGm5[2UzOzZzNEi5PC=>
N-87 M{Syemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPIUodKSzVyPUOwO{BvVQ>? NHXJNogzOzZzNEi5PC=>
H322 M4PXWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{T0TWlEPTB;M{K1JI5O MnzLNlM3OTR6OUi=
H716 NYTjc4ZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4P2fWlEPTB;M{O0JI5O NFnhbYMzOzZzNEi5PC=>
TT MnrxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTTfoxsUUN3ME20NFYhdk1? MWWyN|YyPDh7OB?=
Caki-1 NU\u[lY{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLoTWM2OD12NUCgcm0> M1;UelI{PjF2OEm4
5637 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXq1WVdVUUN3ME22NVAhdk1? NFrFOGczOzZzNEi5PC=>
MB-453 NIHGO5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzITWM2OD14N{Kgcm0> NGT5dpQzOzZzNEi5PC=>
RT-4 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRThzMDDuUS=> MYGyN|YyPDh7OB?=
HOP92 M4\6b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYnoRWtQUUN3ME24NlAhdk1? MXuyN|YyPDh7OB?=
KG-1 NEfCN5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVu0[|dnUUN3ME25NFAhdk1? MUiyN|YyPDh7OB?=
Hs-294T MkjnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvrVplKSzVyPUm0OUBvVQ>? MoTJNlM3OTR6OUi=
SF-539 NIrvVm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1j3S2lEPTB;MUCwNEBvVQ>? NUe3fJp5OjN4MUS4PVg>
U-251 NHrnRpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPoTWM2OD1zMECwJI5O NVT2TFM6OjN4MUS4PVg>
MB-468 MoX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLSTWM2OD1zMECwJI5O M33ZXVI{PjF2OEm4
HS746T M{W5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPW[mxkUUN3ME2xNFAxKG6P MYWyN|YyPDh7OB?=
SCABER M3TlTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;He4xFUUN3ME2xNFAxKG6P NHLWfm4zOzZzNEi5PC=>
MCF-7 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jreGlEPTB;MUCwNUBvVQ>? MUWyN|YyPDh7OB?=
CHL-1 M3n3Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnzPFJKSzVyPUG0OlAhdk1? NF3KS4czOzZzNEi5PC=>
U87MG M4HqWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTJyMECgcm0> M1LlNFI{PjF2OEm4
SJCRH30 MkTjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPLTWM2OD1{MECyJI5O M4fHXlI{PjF2OEm4
ES-2 MlTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTJ4NUmgcm0> MW[yN|YyPDh7OB?=
HT-1376 NYXIRmMxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\ISnZKSzVyPUK4NFAhdk1? MlT1NlM3OTR6OUi=
A172 NUXXdoZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzkSVBKSzVyPUOwNFAhdk1? M2G5bVI{PjF2OEm4
769P MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLGVYNKSzVyPUOwNFAhdk1? MXWyN|YyPDh7OB?=
NCI-H520 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTNyMECgcm0> MlWwNlM3OTR6OUi=
DU145 NVL5dZNHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXmTWM2OD1|MECwJI5O NGrROlEzOzZzNEi5PC=>
K562 MkDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvaTWM2OD1|MECwJI5O NE\ybVYzOzZzNEi5PC=>
U-937 NVrkeFQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnUTWM2OD1|MECwJI5O NYroRYQ6OjN4MUS4PVg>
A204 NYTsc|FqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVOyTpBKUUN3ME2zNFAyKG6P MmjJNlM3OTR6OUi=
DAOY M3HLPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\hbYRKSzVyPUOwNFEhdk1? MWOyN|YyPDh7OB?=
SF-268 Ml7lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\WXo9SUUN3ME2zNFAyKG6P M4T3N|I{PjF2OEm4
SF-295 NF6xVotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTNyMEGgcm0> NWPwdIJvOjN4MUS4PVg>
SNB-19 MofnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlv1TWM2OD1|MECxJI5O M3jKfFI{PjF2OEm4
SNB-75 M{jqNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHO3ZY5KSzVyPUOwNFEhdk1? MXqyN|YyPDh7OB?=
U373-MG MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfyfodMUUN3ME2zNFAyKG6P M{\lT|I{PjF2OEm4
786-O NW\1d2pbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnITWM2OD1|MECxJI5O MormNlM3OTR6OUi=
A498 NIXQbWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PEdmlEPTB;M{CwNUBvVQ>? NVHSNJFnOjN4MUS4PVg>
ACHN M3\DWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTNyMEGgcm0> NXS5Uo5xOjN4MUS4PVg>
EKVX MkSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXUTWM2OD1|MECxJI5O MlnrNlM3OTR6OUi=
H226 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHzVFBIUUN3ME2zNFAyKG6P NHj2c5EzOzZzNEi5PC=>
H522 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXIfJhWUUN3ME2zNFAyKG6P NGD5ZlIzOzZzNEi5PC=>
HeLa M4f0XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDZTWM2OD1|MECxJI5O M1;LTFI{PjF2OEm4
SK-OV-3 NGjwZ4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\nSmlEPTB;M{CwNUBvVQ>? NH\mWYUzOzZzNEi5PC=>
Ln Cap MmHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTNyMEGgcm0> M4nNSlI{PjF2OEm4
PC3 NU\kZVVkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTNyMEGgcm0> NFy2UFAzOzZzNEi5PC=>
SNU-16 M33US2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVn0Nm5yUUN3ME2zNFAyKG6P MnvNNlM3OTR6OUi=
FTC-133 NYLOfHFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTNyMEGgcm0> NVPkZYtyOjN4MUS4PVg>
Ro82-W-1 NWTCZVg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3n0RmlEPTB;M{CwNUBvVQ>? MVGyN|YyPDh7OB?=
Daudi NUnv[3pET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmLhTWM2OD1|MECxJI5O MorjNlM3OTR6OUi=
Jijoye NV3ieWpWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTNyMEGgcm0> MYqyN|YyPDh7OB?=
Jurkat NH3tVmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NESwTHlKSzVyPUOwNFEhdk1? NVf6cGtWOjN4MUS4PVg>
J-82 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1vPNWlEPTB;M{CwNUBvVQ>? NHf5Xm4zOzZzNEi5PC=>
TCC-SUP MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrQZ5VKSzVyPUOwNFEhdk1? NFzWdXIzOzZzNEi5PC=>
BT-474 NHfJXlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmf6TWM2OD1|MECxJI5O NFK1bZMzOzZzNEi5PC=>
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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]

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  • 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:
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.

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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