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 NWTMZ3N7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfpcY5KSzVyPUCuNlQhdk1? M4XqfFI2OzVyOUOx
WM-266-4 M1vPOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4f1U2lEPTB;MkCgcm0> NGTJXlYzOzZzNEi5PC=>
UACC-62 M1LzUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPaTWM2OD1|MDDuUS=> NVzL[GZuOjN4MUS4PVg>
Colo-205 NEf1eVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1mxcWlEPTB;M{[gcm0> NHnkSmkzOzZzNEi5PC=>
SK-Mel-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPRWHpKSzVyPUO3JI5O NFLad4ozOzZzNEi5PC=>
WiDr NHzmVFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlizTWM2OD1|OTDuUS=> MYSyN|YyPDh7OB?=
M14 NWfZRXZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnDUVJWUUN3ME20O{BvVQ>? NInHeJMzOzZzNEi5PC=>
HT-29 NUXmfW9XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHsPWNbUUN3ME21NEBvVQ>? MXyyN|YyPDh7OB?=
8505C MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUnEXIR2UUN3ME21NEBvVQ>? NFrU[5gzOzZzNEi5PC=>
HT-144 MlXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHf1dYFKSzVyPU[wJI5O NETKc5QzOzZzNEi5PC=>
SK-Mel-5 MmDVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\XUmlEPTB;Nk[gcm0> NXrzPG9DOjN4MUS4PVg>
A375-SM Ml\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTEOINKSzVyPUe1JI5O M1LuSVI{PjF2OEm4
SK-Mel-28 NIK3d3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHlTWM2OD16NTDuUS=> MlTBNlM3OTR6OUi=
LOX Mmi4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnlXIVIUUN3ME2xNFAhdk1? NVO4b5ZkOjN4MUS4PVg>
SK-Mel-3 NIjHeY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkOwTWM2OD1zMUigcm0> MnGwNlM3OTR6OUi=
K1 M4H3c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vUcWlEPTB;MUOwJI5O M2P6S|I{PjF2OEm4
Hs-695T Mn30S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfVZ3BKSzVyPUG2OUBvVQ>? MVqyN|YyPDh7OB?=
BHT-101 NIHXUGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELkXYZKSzVyPUOwNEBvVQ>? MnLyNlM3OTR6OUi=
RPMI-7951 Mn7vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjyTWM2OD1|NESgcm0> MVyyN|YyPDh7OB?=
A2058 M1TSfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknBTWM2OD1|NkCgcm0> NVHsOoJNOjN4MUS4PVg>
SK-Hep-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTF2MkKgcm0> M1\EXFI{PjF2OEm4
A673 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHDT|BKSzVyPUOwNFEhdk1? NUXHbXNWOjN4MUS4PVg>
DBTRG-05MG NV7YVY5jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInmNmxKSzVyPUOwNFEhdk1? MonDNlM3OTR6OUi=
SW-626 NWXnSYhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TCXGlEPTB;M{Ogcm0> MY[yN|YyPDh7OB?=
LoVo NVOzVGg5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFK4V5pKSzVyPUS3JI5O MoT4NlM3OTR6OUi=
MiaPaCa NF:xfZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnVWld2UUN3ME21N{BvVQ>? MkfZNlM3OTR6OUi=
SW-620 MnTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\hTWM2OD1zMESgcm0> M3HlfFI{PjF2OEm4
CAPAN-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLuTXJKSzVyPUGwOEBvVQ>? MX:yN|YyPDh7OB?=
SW-527 NHvES2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTF{MTDuUS=> M1nobFI{PjF2OEm4
HCT-116 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF;qdIJKSzVyPUGyPEBvVQ>? NYHnbWlXOjN4MUS4PVg>
SW-480 M2G2e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPGXHJKSzVyPUG2OUBvVQ>? NVy3[4kyOjN4MUS4PVg>
HPAC NXP2XWNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jnRWlEPTB;MUewJI5O M4nO[FI{PjF2OEm4
OVCAR-5 M2rPPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTLTWM2OD1{MEigcm0> M3vmcFI{PjF2OEm4
AsPc-1 NYfGcZFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHkTWM2OD1{N{Cgcm0> NV;MdHdvOjN4MUS4PVg>
A549 MoK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\CXJpKSzVyPUOyOkBvVQ>? MV:yN|YyPDh7OB?=
SNU-1 NUPDdoZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGr4epRKSzVyPUO1OEBvVQ>? MYSyN|YyPDh7OB?=
HOP62 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;xTWM2OD14N{[gcm0> NF;YPYIzOzZzNEi5PC=>
H23 NWLRdW5mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTFyMECgcm0> M3HWdFI{PjF2OEm4
MB-231 NVztWHV7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1j4d2lEPTB;MUCwNEBvVQ>? MW[yN|YyPDh7OB?=
SU.86.86 MkS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDsN3loUUN3ME2xNFAyKG6P NUjQO2JkOjN4MUS4PVg>
CFPAC-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTFyMEGgcm0> M2r4eVI{PjF2OEm4
A427 M2TZVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLaTWM2OD1zNEOzJI5O NIDvOlAzOzZzNEi5PC=>
MDAH-2774 NYPKUGtWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTJ4NUegcm0> MWCyN|YyPDh7OB?=
NCI-H157 NYXSbXVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HjWWlEPTB;M{CwNEBvVQ>? MkfENlM3OTR6OUi=
HTB-177 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3yc2dwUUN3ME2zNFAxKG6P M33aelI{PjF2OEm4
UM-UC-3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFn1[3lKSzVyPUOwNFEhdk1? MofJNlM3OTR6OUi=
HCT-8 M3LkcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zEeWlEPTB;M{CwNUBvVQ>? NGftU3ozOzZzNEi5PC=>
Panc-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTNyMEGgcm0> MXqyN|YyPDh7OB?=
DLD-1 M4DiSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVzVeHpEUUN3ME2zNFAyKG6P NEDXbYEzOzZzNEi5PC=>
HCT-15 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfLWVlKSzVyPUOwNFEhdk1? M1joOFI{PjF2OEm4
HL-60 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3DTWM2OD1|MDDuUS=> NVTMeZFPOjN4MUS4PVg>
SK-Mel-2 NIXSS4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHf5eFVKSzVyPUO0JI5O M1XMS|I{PjF2OEm4
RD M1zpO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTFTWM2OD1zMkOgcm0> MYiyN|YyPDh7OB?=
HT-1197 Mmn0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYX2Wo8zUUN3ME2zNVYhdk1? M3rsbFI{PjF2OEm4
Molt-3 MoPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTZyMDDuUS=> MoDMNlM3OTR6OUi=
PA-1 NVH6XVc3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjYZ4RKSzVyPUGwNFEhdk1? MmTtNlM3OTR6OUi=
Molt-4 MnvWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HEVWlEPTB;M{CwNUBvVQ>? NIXvbogzOzZzNEi5PC=>
NCI-H292 NGLzNpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfJT|dKSzVyPUmwJI5O NYH3SYFZOjN4MUS4PVg>
A2780 MoTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnl[ldKSzVyPUG0N{BvVQ>? MUWyN|YyPDh7OB?=
IGROV-1 NWTyOGg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIrvWJlKSzVyPUG0OkBvVQ>? M{HWRlI{PjF2OEm4
SK-N-SH M3T6Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTVOGxyUUN3ME2xOVAhdk1? MljoNlM3OTR6OUi=
N-87 NYL4eGNmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7pOWJKSzVyPUOwO{BvVQ>? MlG4NlM3OTR6OUi=
H322 MnHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnO5TWM2OD1|MkWgcm0> NVXXUY5iOjN4MUS4PVg>
H716 M17rWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DGZWlEPTB;M{O0JI5O NGS0TGgzOzZzNEi5PC=>
TT NHzEbmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlW2TWM2OD12ME[gcm0> MkLyNlM3OTR6OUi=
Caki-1 Ml30S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjrTWM2OD12NUCgcm0> NGHW[mkzOzZzNEi5PC=>
5637 NIDJfZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPOTWM2OD14MUCgcm0> MnjJNlM3OTR6OUi=
MB-453 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGCyS|ZKSzVyPU[3NkBvVQ>? MnftNlM3OTR6OUi=
RT-4 NVO5WG5ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{D0PWlEPTB;OEGwJI5O MV6yN|YyPDh7OB?=
HOP92 NEPR[nZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUj1[lZWUUN3ME24NlAhdk1? MlvHNlM3OTR6OUi=
KG-1 MlrES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPoTWM2OD17MECgcm0> NHv6TYIzOzZzNEi5PC=>
Hs-294T M2X3Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTl2NTDuUS=> MUGyN|YyPDh7OB?=
SF-539 M2D0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHL3dZdKSzVyPUGwNFAhdk1? MYGyN|YyPDh7OB?=
U-251 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfUZpZKSzVyPUGwNFAhdk1? NHzGOG0zOzZzNEi5PC=>
MB-468 MorZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mor0TWM2OD1zMECwJI5O NGHSbWQzOzZzNEi5PC=>
HS746T MnnBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGizVYdKSzVyPUGwNFAhdk1? NV\PfpJoOjN4MUS4PVg>
SCABER MnHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LTemlEPTB;MUCwNEBvVQ>? NH3LUXEzOzZzNEi5PC=>
MCF-7 NVTwb2hKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zEb2lEPTB;MUCwNUBvVQ>? MUWyN|YyPDh7OB?=
CHL-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nWNmlEPTB;MUS2NEBvVQ>? NHriXlYzOzZzNEi5PC=>
U87MG NIrN[G1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmmyTWM2OD1{MECwJI5O M2LKVlI{PjF2OEm4
SJCRH30 NXjWRZNqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LFVWlEPTB;MkCwNkBvVQ>? M3:0SlI{PjF2OEm4
ES-2 MnThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknHTWM2OD1{NkW5JI5O MWeyN|YyPDh7OB?=
HT-1376 NGP6U2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTJ6MECgcm0> NVPtNFR7OjN4MUS4PVg>
A172 NHWwdHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIezUJRKSzVyPUOwNFAhdk1? NFjrWmQzOzZzNEi5PC=>
769P NEnR[YFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7WTWM2OD1|MECwJI5O M4jNcVI{PjF2OEm4
NCI-H520 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTNyMECgcm0> MV2yN|YyPDh7OB?=
DU145 NFHldGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnBZotKSzVyPUOwNFAhdk1? NUGxPIIzOjN4MUS4PVg>
K562 M4DPTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnKxTWM2OD1|MECwJI5O M1vXZlI{PjF2OEm4
U-937 NIrKeIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW[3OJp{UUN3ME2zNFAxKG6P NWOzV5BZOjN4MUS4PVg>
A204 M{nFNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkW5TWM2OD1|MECxJI5O Mon4NlM3OTR6OUi=
DAOY MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{m5NWlEPTB;M{CwNUBvVQ>? MlXxNlM3OTR6OUi=
SF-268 NX3BU3VmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MonkTWM2OD1|MECxJI5O MViyN|YyPDh7OB?=
SF-295 M2n3dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfmR4JNUUN3ME2zNFAyKG6P MV6yN|YyPDh7OB?=
SNB-19 NFjKUG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTNyMEGgcm0> MVyyN|YyPDh7OB?=
SNB-75 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37oRmlEPTB;M{CwNUBvVQ>? Mn:5NlM3OTR6OUi=
U373-MG NXLlUWwzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XDbWlEPTB;M{CwNUBvVQ>? MknnNlM3OTR6OUi=
786-O M1W0WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI[zPIJKSzVyPUOwNFEhdk1? MYGyN|YyPDh7OB?=
A498 NVr6S|lpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3q4N2lEPTB;M{CwNUBvVQ>? M{fNZ|I{PjF2OEm4
ACHN NILQcVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXOxdnlMUUN3ME2zNFAyKG6P Mnn2NlM3OTR6OUi=
EKVX MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTDTWM2OD1|MECxJI5O M3GwZVI{PjF2OEm4
H226 MoHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTNyMEGgcm0> M4e3b|I{PjF2OEm4
H522 Mk\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoT4TWM2OD1|MECxJI5O MkHZNlM3OTR6OUi=
HeLa M3PUU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TCXGlEPTB;M{CwNUBvVQ>? NFTz[JUzOzZzNEi5PC=>
SK-OV-3 Mn7JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTNyMEGgcm0> NH6xN5ozOzZzNEi5PC=>
Ln Cap MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTNyMEGgcm0> NGjCc4EzOzZzNEi5PC=>
PC3 M1\Zbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTNyMEGgcm0> MnvGNlM3OTR6OUi=
SNU-16 NEfRZnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVO5bY1wUUN3ME2zNFAyKG6P NH7SdFYzOzZzNEi5PC=>
FTC-133 M1HwNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFe4Z3ZKSzVyPUOwNFEhdk1? M174dFI{PjF2OEm4
Ro82-W-1 Mn\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\TTWM2OD1|MECxJI5O NITsUG0zOzZzNEi5PC=>
Daudi NIS3XlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUe0WJhzUUN3ME2zNFAyKG6P MmfINlM3OTR6OUi=
Jijoye MkXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\VcGlEPTB;M{CwNUBvVQ>? M2XPdFI{PjF2OEm4
Jurkat NX\sS40yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTNyMEGgcm0> MWiyN|YyPDh7OB?=
J-82 NITyXm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPWV4pKSzVyPUOwNFEhdk1? NX[xNWxQOjN4MUS4PVg>
TCC-SUP NESwcFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfMTWM2OD1|MECxJI5O M4\6dlI{PjF2OEm4
BT-474 MmmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTNyMEGgcm0> NX;QZZZ6OjN4MUS4PVg>
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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 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
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