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)
MEK1 [1]
(Cell-free assay)
1 nM 4 nM >10 μM
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 MkftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXzTWM2OD1yLkK0JI5O MofiNlU{PTB7M{G=
WM-266-4 M1W1RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXLTWM2OD1{MDDuUS=> M3fJblI{PjF2OEm4
UACC-62 M{flcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILydY1KSzVyPUOwJI5O NYKxUVhwOjN4MUS4PVg>
Colo-205 M4\JW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfPTWM2OD1|NjDuUS=> M3TMdlI{PjF2OEm4
SK-Mel-1 NEHSZYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVy4d3hpUUN3ME2zO{BvVQ>? NGTBVIYzOzZzNEi5PC=>
WiDr NXXId|hmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTRNoJEUUN3ME2zPUBvVQ>? MV[yN|YyPDh7OB?=
M14 NGLQbHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPGR2l4UUN3ME20O{BvVQ>? MVqyN|YyPDh7OB?=
HT-29 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF2wUo5KSzVyPUWwJI5O NHO5SWYzOzZzNEi5PC=>
8505C M4TLUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTVyIH7N NHX0XY4zOzZzNEi5PC=>
HT-144 M{LTcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFj6TYNKSzVyPU[wJI5O NF30S2czOzZzNEi5PC=>
SK-Mel-5 MkPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHRU|ZKSzVyPU[2JI5O M1K3eVI{PjF2OEm4
A375-SM MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PUb2lEPTB;N{Wgcm0> NWnuV3Q2OjN4MUS4PVg>
SK-Mel-28 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXBV|hKSzVyPUi1JI5O NEnIenozOzZzNEi5PC=>
LOX M{TNTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnHUGhKSzVyPUGwNEBvVQ>? M4XPXFI{PjF2OEm4
SK-Mel-3 M2rOcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTFzODDuUS=> M1jwZlI{PjF2OEm4
K1 NVTabotvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF[yN4tKSzVyPUGzNEBvVQ>? NYj6PHhpOjN4MUS4PVg>
Hs-695T NXi0[JpqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTF4NTDuUS=> NE\qUIUzOzZzNEi5PC=>
BHT-101 NW[4ZoFST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTNyMDDuUS=> NHzZWpYzOzZzNEi5PC=>
RPMI-7951 NWOyWG4xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnvTWM2OD1|NESgcm0> Mn7wNlM3OTR6OUi=
A2058 NHH4VJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2D1eWlEPTB;M{[wJI5O MU[yN|YyPDh7OB?=
SK-Hep-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDxOmVKSzVyPUG0NlIhdk1? NVrLboNlOjN4MUS4PVg>
A673 NHv0eWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fRWWlEPTB;M{CwNUBvVQ>? NVTQOXFUOjN4MUS4PVg>
DBTRG-05MG NGDNV4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnKzTWM2OD1|MECxJI5O MYiyN|YyPDh7OB?=
SW-626 M4XvTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTN|IH7N M4O5XVI{PjF2OEm4
LoVo MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvjTWM2OD12NzDuUS=> MVyyN|YyPDh7OB?=
MiaPaCa MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPzTWM2OD13MzDuUS=> NHTqeGgzOzZzNEi5PC=>
SW-620 NVz1e4l7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlf3TWM2OD1zMESgcm0> MUmyN|YyPDh7OB?=
CAPAN-1 MlS2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTFyNDDuUS=> NWjk[I1POjN4MUS4PVg>
SW-527 NEG3[HJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTF{MTDuUS=> NV32bI9UOjN4MUS4PVg>
HCT-116 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHQTWM2OD1zMkigcm0> NILldGszOzZzNEi5PC=>
SW-480 NEXFXXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVH2d2htUUN3ME2xOlUhdk1? NXnISIJmOjN4MUS4PVg>
HPAC NGjNdmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jVWGlEPTB;MUewJI5O MmfINlM3OTR6OUi=
OVCAR-5 NF\veGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTJyODDuUS=> NIDmfnQzOzZzNEi5PC=>
AsPc-1 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjpdmFKSzVyPUK3NEBvVQ>? MorlNlM3OTR6OUi=
A549 M3\YfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF65dGxKSzVyPUOyOkBvVQ>? NIC2RXQzOzZzNEi5PC=>
SNU-1 NVrsdVUxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;sN2lEPTB;M{W0JI5O NInQZ4QzOzZzNEi5PC=>
HOP62 NXPTSYZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XoW2lEPTB;Nke2JI5O MVyyN|YyPDh7OB?=
H23 M2\4emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTFyMECgcm0> MnO0NlM3OTR6OUi=
MB-231 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHFSZJHUUN3ME2xNFAxKG6P NITVcIczOzZzNEi5PC=>
SU.86.86 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HCeWlEPTB;MUCwNUBvVQ>? MVKyN|YyPDh7OB?=
CFPAC-1 NUfoZmFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTFyMEGgcm0> M2PhfVI{PjF2OEm4
A427 MkfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWH6fWxCUUN3ME2xOFM{KG6P M4nlZVI{PjF2OEm4
MDAH-2774 NFrMSlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2CzTGlEPTB;Mk[1O{BvVQ>? NIPsboIzOzZzNEi5PC=>
NCI-H157 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nDNWlEPTB;M{CwNEBvVQ>? NW\LcZN6OjN4MUS4PVg>
HTB-177 M2TQOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPVXXZKSzVyPUOwNFAhdk1? NIH5NoozOzZzNEi5PC=>
UM-UC-3 MmnDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XYWmlEPTB;M{CwNUBvVQ>? MmPUNlM3OTR6OUi=
HCT-8 NWTnfXJQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml2zTWM2OD1|MECxJI5O M2nSbFI{PjF2OEm4
Panc-1 NF\mRlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXaTWM2OD1|MECxJI5O M2jJTlI{PjF2OEm4
DLD-1 M37Rbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjXRo5KSzVyPUOwNFEhdk1? NGflPZQzOzZzNEi5PC=>
HCT-15 M1LP[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nYWWlEPTB;M{CwNUBvVQ>? MmnyNlM3OTR6OUi=
HL-60 NHTZT3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XyPWlEPTB;M{Cgcm0> M{e0SlI{PjF2OEm4
SK-Mel-2 M2jx[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLvTWM2OD1|NDDuUS=> M3Pm[|I{PjF2OEm4
RD M4GwS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHEcJh4UUN3ME2xNlMhdk1? Mm\QNlM3OTR6OUi=
HT-1197 M4fLemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTNzNjDuUS=> MXyyN|YyPDh7OB?=
Molt-3 NETOOVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\STWM2OD14MECgcm0> NXzpTnpnOjN4MUS4PVg>
PA-1 M1HVS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLpTWM2OD1zMECxJI5O NFXMcnEzOzZzNEi5PC=>
Molt-4 M{nIWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPUTWM2OD1|MECxJI5O M1r5PVI{PjF2OEm4
NCI-H292 NXjrN4R{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\ETWM2OD17MDDuUS=> MmTFNlM3OTR6OUi=
A2780 MkH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTF2MzDuUS=> NV\DNY8zOjN4MUS4PVg>
IGROV-1 NGrve5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTF2NjDuUS=> NFv4[VIzOzZzNEi5PC=>
SK-N-SH M2PhcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTF3MDDuUS=> MoXQNlM3OTR6OUi=
N-87 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnKd3hRUUN3ME2zNFchdk1? MWeyN|YyPDh7OB?=
H322 M1\Wd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\2TWM2OD1|MkWgcm0> MX[yN|YyPDh7OB?=
H716 MnSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;2NoxNUUN3ME2zN|Qhdk1? NInBNIQzOzZzNEi5PC=>
TT MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTRyNjDuUS=> MmHnNlM3OTR6OUi=
Caki-1 M{\OSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTR3MDDuUS=> NEW5UZozOzZzNEi5PC=>
5637 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTZzMDDuUS=> NF3TVlYzOzZzNEi5PC=>
MB-453 MnjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7hTWM2OD14N{Kgcm0> M2\pTlI{PjF2OEm4
RT-4 M37je2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PlfWlEPTB;OEGwJI5O MY[yN|YyPDh7OB?=
HOP92 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPUTWM2OD16MkCgcm0> M1;uZVI{PjF2OEm4
KG-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPleJpKSzVyPUmwNEBvVQ>? MnXXNlM3OTR6OUi=
Hs-294T MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2fj[2lEPTB;OUS1JI5O M2K4UlI{PjF2OEm4
SF-539 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTFyMECgcm0> NXzMbHNzOjN4MUS4PVg>
U-251 NWTwepV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDETWM2OD1zMECwJI5O NGDTVmkzOzZzNEi5PC=>
MB-468 Ml7ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXZSnBKSzVyPUGwNFAhdk1? M1fpfVI{PjF2OEm4
HS746T MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEW0[|RKSzVyPUGwNFAhdk1? M37OdlI{PjF2OEm4
SCABER M2XE[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDneYZKSzVyPUGwNFAhdk1? M{PRcVI{PjF2OEm4
MCF-7 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;qfVRKSzVyPUGwNFEhdk1? MlfNNlM3OTR6OUi=
CHL-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\HTWM2OD1zNE[wJI5O NVj2[HY6OjN4MUS4PVg>
U87MG MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHw[mpKSzVyPUKwNFAhdk1? MoPwNlM3OTR6OUi=
SJCRH30 M3u5emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTJyMEKgcm0> M{Gxe|I{PjF2OEm4
ES-2 NELCXJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3QdZZwUUN3ME2yOlU6KG6P M4\FOVI{PjF2OEm4
HT-1376 MmfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjJTWM2OD1{OECwJI5O NYnJfIx2OjN4MUS4PVg>
A172 NHi4[ZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nVRWlEPTB;M{CwNEBvVQ>? NXjHfY1SOjN4MUS4PVg>
769P M2rIXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLrTWM2OD1|MECwJI5O NHrBRoIzOzZzNEi5PC=>
NCI-H520 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRTNyMECgcm0> NHLlU4QzOzZzNEi5PC=>
DU145 NU\RWY8xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\4OmtKSzVyPUOwNFAhdk1? M2DufFI{PjF2OEm4
K562 M1q4fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTNyMECgcm0> NFnRV2EzOzZzNEi5PC=>
U-937 MkHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTNyMECgcm0> MUWyN|YyPDh7OB?=
A204 Mn7XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFnMRnhKSzVyPUOwNFEhdk1? NWLBN3hrOjN4MUS4PVg>
DAOY NYfJUZN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\H[po1UUN3ME2zNFAyKG6P NVvGeYdsOjN4MUS4PVg>
SF-268 NXjxNpVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfXTWM2OD1|MECxJI5O M2\sbFI{PjF2OEm4
SF-295 Ml3pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPvbIJUUUN3ME2zNFAyKG6P MmC3NlM3OTR6OUi=
SNB-19 NH;EW2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnryTWM2OD1|MECxJI5O NE\mRY0zOzZzNEi5PC=>
SNB-75 NVS5T5kzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTNyMEGgcm0> M4\PUFI{PjF2OEm4
U373-MG MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17OTmlEPTB;M{CwNUBvVQ>? NVrjeldkOjN4MUS4PVg>
786-O MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnPZWt[UUN3ME2zNFAyKG6P NIjxfngzOzZzNEi5PC=>
A498 NHv6VJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\TNJpKSzVyPUOwNFEhdk1? NWXxeJRlOjN4MUS4PVg>
ACHN NYrUfZhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XSR2lEPTB;M{CwNUBvVQ>? NFjOZWEzOzZzNEi5PC=>
EKVX M2PpRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3roZWlEPTB;M{CwNUBvVQ>? NY\yb4NROjN4MUS4PVg>
H226 NFzRdFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTNyMEGgcm0> NXrnNItPOjN4MUS4PVg>
H522 NGPkVm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\kTWM2OD1|MECxJI5O NFPpSWwzOzZzNEi5PC=>
HeLa NX;wW|B2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLQTWM2OD1|MECxJI5O MYqyN|YyPDh7OB?=
SK-OV-3 NYjJfVc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHTfm1KSzVyPUOwNFEhdk1? NEG4PVgzOzZzNEi5PC=>
Ln Cap MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4D3RmlEPTB;M{CwNUBvVQ>? NWTabpREOjN4MUS4PVg>
PC3 NHPsephIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTNyMEGgcm0> NITXbIIzOzZzNEi5PC=>
SNU-16 MknNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTNyMEGgcm0> NXLlWZYzOjN4MUS4PVg>
FTC-133 MmSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHvSI94UUN3ME2zNFAyKG6P MWCyN|YyPDh7OB?=
Ro82-W-1 M37a[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTNyMEGgcm0> M{W3XFI{PjF2OEm4
Daudi MnHQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jz[mlEPTB;M{CwNUBvVQ>? NFuzO4MzOzZzNEi5PC=>
Jijoye MmnuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTNyMEGgcm0> NUnXUGRFOjN4MUS4PVg>
Jurkat M{OwUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrUd|Y2UUN3ME2zNFAyKG6P M1;IVVI{PjF2OEm4
J-82 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LQSmlEPTB;M{CwNUBvVQ>? MoLuNlM3OTR6OUi=
TCC-SUP NFjMNVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTNyMEGgcm0> M4LhU|I{PjF2OEm4
BT-474 NX3mTZBFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUn4[YVsUUN3ME2zNFAyKG6P NWXhd|NWOjN4MUS4PVg>
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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)

Solubility (25°C)

In vitro DMSO 0.1 mg/mL warmed (0.17 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
5% DMSO+30% PEG 300+ddH2O
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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ERK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID