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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4 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.

    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 NULtSWQ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4K5SWlEPTB;MD6yOEBvVQ>? NV7kPZpoOjV|NUC5N|E>
WM-266-4 NUWz[YJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nyZWlEPTB;MkCgcm0> NI\2cI4zOzZzNEi5PC=>
UACC-62 Mn;HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonaTWM2OD1|MDDuUS=> MnPSNlM3OTR6OUi=
Colo-205 NV3WPJNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmezTWM2OD1|NjDuUS=> MX6yN|YyPDh7OB?=
SK-Mel-1 M2HweGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGL5U2FKSzVyPUO3JI5O NFzMXIczOzZzNEi5PC=>
WiDr MoPSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjZ[5NKSzVyPUO5JI5O NX3Xd2pkOjN4MUS4PVg>
M14 M3zp[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3z2emlEPTB;NEegcm0> MUiyN|YyPDh7OB?=
HT-29 MlXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fQcmlEPTB;NUCgcm0> MkfTNlM3OTR6OUi=
8505C NHPaeYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDhe3U5UUN3ME21NEBvVQ>? MoDQNlM3OTR6OUi=
HT-144 MoLIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDMTWM2OD14MDDuUS=> MkfTNlM3OTR6OUi=
SK-Mel-5 NVezXYlWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTZ4IH7N NHnKNGwzOzZzNEi5PC=>
A375-SM Mny1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTd3IH7N MYiyN|YyPDh7OB?=
SK-Mel-28 Mn3BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPJSYlKSzVyPUi1JI5O Mn;kNlM3OTR6OUi=
LOX M1XFd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nVU2lEPTB;MUCwJI5O MoT5NlM3OTR6OUi=
SK-Mel-3 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1i5d2lEPTB;MUG4JI5O MVqyN|YyPDh7OB?=
K1 NYDDcIZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHiTWM2OD1zM{Cgcm0> NIHJWmszOzZzNEi5PC=>
Hs-695T NYTW[VluT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TIN2lEPTB;MU[1JI5O M3jxbVI{PjF2OEm4
BHT-101 MmHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2L0c2lEPTB;M{CwJI5O M{DaPVI{PjF2OEm4
RPMI-7951 NHHBV|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHpemlKSzVyPUO0OEBvVQ>? M2fGeFI{PjF2OEm4
A2058 M1nmfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPpN4hKSzVyPUO2NEBvVQ>? MmToNlM3OTR6OUi=
SK-Hep-1 M4jjfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTF2MkKgcm0> MofqNlM3OTR6OUi=
A673 NV\YOYJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2jWVGlEPTB;M{CwNUBvVQ>? MkLONlM3OTR6OUi=
DBTRG-05MG MmThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlHTTWM2OD1|MECxJI5O NF36fpMzOzZzNEi5PC=>
SW-626 NIf2[INIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHpT4VtUUN3ME2zN{BvVQ>? MlfXNlM3OTR6OUi=
LoVo Mnz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvxdFVLUUN3ME20O{BvVQ>? M4DGe|I{PjF2OEm4
MiaPaCa M4qze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPsTWM2OD13MzDuUS=> NIKyRVgzOzZzNEi5PC=>
SW-620 M1GwT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVX0O3F6UUN3ME2xNFQhdk1? M4PDZlI{PjF2OEm4
CAPAN-1 NXHONpZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrP[Y5KSzVyPUGwOEBvVQ>? NV3RPVBJOjN4MUS4PVg>
SW-527 M4ri[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TDe2lEPTB;MUKxJI5O MlzvNlM3OTR6OUi=
HCT-116 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTF{ODDuUS=> MkLvNlM3OTR6OUi=
SW-480 M4PjWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjiTWM2OD1zNkWgcm0> NYLOPVlLOjN4MUS4PVg>
HPAC NEXmSnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmG2TWM2OD1zN{Cgcm0> M3vpclI{PjF2OEm4
OVCAR-5 NIHJVGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnGxTWM2OD1{MEigcm0> NHnkN24zOzZzNEi5PC=>
AsPc-1 NITUbYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XzbWlEPTB;MkewJI5O NWHaOmVQOjN4MUS4PVg>
A549 MojXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLsTWM2OD1|Mk[gcm0> MYWyN|YyPDh7OB?=
SNU-1 M1zEVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7GNlFlUUN3ME2zOVQhdk1? MUKyN|YyPDh7OB?=
HOP62 NUHPNoRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLtTWM2OD14N{[gcm0> M1zhNlI{PjF2OEm4
H23 MnHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTFyMECgcm0> MnviNlM3OTR6OUi=
MB-231 NX3wU4RiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlW5TWM2OD1zMECwJI5O NEHUe|EzOzZzNEi5PC=>
SU.86.86 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF75SoxKSzVyPUGwNFEhdk1? NIT4R|YzOzZzNEi5PC=>
CFPAC-1 NIPLXo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX22W3ZLUUN3ME2xNFAyKG6P MWiyN|YyPDh7OB?=
A427 M1LyVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXDWlgxUUN3ME2xOFM{KG6P MWKyN|YyPDh7OB?=
MDAH-2774 NHzPcI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3GTWM2OD1{NkW3JI5O Mn\qNlM3OTR6OUi=
NCI-H157 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYSxXZQzUUN3ME2zNFAxKG6P NIPYeIozOzZzNEi5PC=>
HTB-177 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXNdHRKSzVyPUOwNFAhdk1? MoW3NlM3OTR6OUi=
UM-UC-3 M4j2b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37uc2lEPTB;M{CwNUBvVQ>? MmHRNlM3OTR6OUi=
HCT-8 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\tWWlEPTB;M{CwNUBvVQ>? MnvTNlM3OTR6OUi=
Panc-1 NWnLeVJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTNyMEGgcm0> MWWyN|YyPDh7OB?=
DLD-1 Mm\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvuSmZKSzVyPUOwNFEhdk1? NIjjRVgzOzZzNEi5PC=>
HCT-15 NFTLVJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTNyMEGgcm0> MoHVNlM3OTR6OUi=
HL-60 MmjYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTNyIH7N NV[3Xm1OOjN4MUS4PVg>
SK-Mel-2 M3[xNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXCVYFKSzVyPUO0JI5O Mn;5NlM3OTR6OUi=
RD NF74VlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjhTWM2OD1zMkOgcm0> NUPRXXlKOjN4MUS4PVg>
HT-1197 M2f6b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXMS|dKUUN3ME2zNVYhdk1? NXfMTIlnOjN4MUS4PVg>
Molt-3 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfzNFVRUUN3ME22NFAhdk1? NG\VfVMzOzZzNEi5PC=>
PA-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGO2NphKSzVyPUGwNFEhdk1? NVqwR3hrOjN4MUS4PVg>
Molt-4 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnmwTWM2OD1|MECxJI5O NHjTe3gzOzZzNEi5PC=>
NCI-H292 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;kV2lEPTB;OUCgcm0> NVi0RVlKOjN4MUS4PVg>
A2780 MoDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrpbm1IUUN3ME2xOFMhdk1? MV:yN|YyPDh7OB?=
IGROV-1 NUjTZ3c6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH:yfm1KSzVyPUG0OkBvVQ>? MmHINlM3OTR6OUi=
SK-N-SH M4izSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTF3MDDuUS=> NVHG[m1IOjN4MUS4PVg>
N-87 NGiwRmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHhdYNKSzVyPUOwO{BvVQ>? NGjJSGYzOzZzNEi5PC=>
H322 NVPZXphoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\tfZZKSzVyPUOyOUBvVQ>? NIfiU2wzOzZzNEi5PC=>
H716 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHHlTphKSzVyPUOzOEBvVQ>? MX6yN|YyPDh7OB?=
TT M3zRTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3jU|lKSzVyPUSwOkBvVQ>? MWGyN|YyPDh7OB?=
Caki-1 M1u5bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvlcVNKSzVyPUS1NEBvVQ>? MX6yN|YyPDh7OB?=
5637 NX3IcIN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTZzMDDuUS=> MVyyN|YyPDh7OB?=
MB-453 NHjsfIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlWxTWM2OD14N{Kgcm0> NHLxZpMzOzZzNEi5PC=>
RT-4 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWS4XZI4UUN3ME24NVAhdk1? MmPuNlM3OTR6OUi=
HOP92 NUfQXpVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXReZdKSzVyPUiyNEBvVQ>? NX[zRYVPOjN4MUS4PVg>
KG-1 NVr3OJdiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTlyMDDuUS=> Mki0NlM3OTR6OUi=
Hs-294T M1jQPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLhSphKSzVyPUm0OUBvVQ>? NVLJUVhiOjN4MUS4PVg>
SF-539 MmfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPNTWMzUUN3ME2xNFAxKG6P NYLaZ2JjOjN4MUS4PVg>
U-251 M{XlUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4m5N2lEPTB;MUCwNEBvVQ>? NH3Rb3EzOzZzNEi5PC=>
MB-468 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4C1ZmlEPTB;MUCwNEBvVQ>? Mo[2NlM3OTR6OUi=
HS746T MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHMTYlKSzVyPUGwNFAhdk1? MW[yN|YyPDh7OB?=
SCABER NGHoSWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTFyMECgcm0> MViyN|YyPDh7OB?=
MCF-7 NFW5SXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlntTWM2OD1zMECxJI5O NXzkelhiOjN4MUS4PVg>
CHL-1 NHT5WVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTF2NkCgcm0> MWSyN|YyPDh7OB?=
U87MG NW\3fnE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn:5TWM2OD1{MECwJI5O MYWyN|YyPDh7OB?=
SJCRH30 NEDFTJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorJTWM2OD1{MECyJI5O NWGwWJBrOjN4MUS4PVg>
ES-2 M{nVWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfP[mNKSzVyPUK2OVkhdk1? NV6xb2hpOjN4MUS4PVg>
HT-1376 NFTwToRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfQeZR[UUN3ME2yPFAxKG6P MYGyN|YyPDh7OB?=
A172 NFrIOW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXuTWM2OD1|MECwJI5O M1vX[FI{PjF2OEm4
769P MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTNyMECgcm0> M2m3TVI{PjF2OEm4
NCI-H520 NVHiSHpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfSd5JPUUN3ME2zNFAxKG6P NIHOWYUzOzZzNEi5PC=>
DU145 M1TURWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEL4fFNKSzVyPUOwNFAhdk1? MX:yN|YyPDh7OB?=
K562 NUOyVm9KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjPbo9KSzVyPUOwNFAhdk1? M3vETlI{PjF2OEm4
U-937 NYTpPHJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXsZ5pKSzVyPUOwNFAhdk1? M2nIdVI{PjF2OEm4
A204 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILYZXNKSzVyPUOwNFEhdk1? Mm[2NlM3OTR6OUi=
DAOY MoL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\aWotKSzVyPUOwNFEhdk1? NEnmXGgzOzZzNEi5PC=>
SF-268 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXIV5lNUUN3ME2zNFAyKG6P NVflTJpLOjN4MUS4PVg>
SF-295 NIjQdXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\3XGlEPTB;M{CwNUBvVQ>? NVzPbldyOjN4MUS4PVg>
SNB-19 NFi0O2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fO[WlEPTB;M{CwNUBvVQ>? M3z2UVI{PjF2OEm4
SNB-75 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\5RmlEPTB;M{CwNUBvVQ>? NVfRPIVPOjN4MUS4PVg>
U373-MG M1n4U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFX0RVFKSzVyPUOwNFEhdk1? NEfhPI8zOzZzNEi5PC=>
786-O M1e4[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTNyMEGgcm0> MWSyN|YyPDh7OB?=
A498 M1fN[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3He2xYUUN3ME2zNFAyKG6P M3;EdVI{PjF2OEm4
ACHN MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTNyMEGgcm0> MmLYNlM3OTR6OUi=
EKVX MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{W3UGlEPTB;M{CwNUBvVQ>? M3HuW|I{PjF2OEm4
H226 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTNyMEGgcm0> NVmwNlBkOjN4MUS4PVg>
H522 MnjiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TDPWlEPTB;M{CwNUBvVQ>? MXKyN|YyPDh7OB?=
HeLa NWnyT4dTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXH4fGtlUUN3ME2zNFAyKG6P MYSyN|YyPDh7OB?=
SK-OV-3 NYTJdlAyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXS[ZdKSzVyPUOwNFEhdk1? NG\QUZgzOzZzNEi5PC=>
Ln Cap Ml;BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3IOnVnUUN3ME2zNFAyKG6P M4fOWVI{PjF2OEm4
PC3 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHflfYZKSzVyPUOwNFEhdk1? NHTiT|czOzZzNEi5PC=>
SNU-16 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3QUoNKSzVyPUOwNFEhdk1? NHH5OZEzOzZzNEi5PC=>
FTC-133 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTNyMEGgcm0> NX\0VVFSOjN4MUS4PVg>
Ro82-W-1 M2TUWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{C4TWlEPTB;M{CwNUBvVQ>? MmjjNlM3OTR6OUi=
Daudi NV3mS|ZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzvTWM2OD1|MECxJI5O MWmyN|YyPDh7OB?=
Jijoye NEfOWXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULIbplWUUN3ME2zNFAyKG6P M1q0fFI{PjF2OEm4
Jurkat M{DafWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHDfJc{UUN3ME2zNFAyKG6P MVGyN|YyPDh7OB?=
J-82 NHrvWnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIT1VpdKSzVyPUOwNFEhdk1? MoO4NlM3OTR6OUi=
TCC-SUP M{juSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTNyMEGgcm0> NY\qbIxHOjN4MUS4PVg>
BT-474 NFjhV3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTNyMEGgcm0> M1XiW|I{PjF2OEm4
ZR-75-1 NULTZ4VvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLRNlNtUUN3ME2zNFAyKG6P NETTUJczOzZzNEi5PC=>

... 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(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
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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):
    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