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 MlTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFGzbFdKSzVyPUCuNlQhdk1? NYHtZWZmOjV|NUC5N|E>
WM-266-4 NHLl[GFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTtOopKSzVyPUKwJI5O MmHtNlM3OTR6OUi=
UACC-62 MknJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLPUWVKSzVyPUOwJI5O M1KzUVI{PjF2OEm4
Colo-205 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4m4fWlEPTB;M{[gcm0> MVSyN|YyPDh7OB?=
SK-Mel-1 M13wV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTN5IH7N NHzyc5QzOzZzNEi5PC=>
WiDr NWjudol[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nESmlEPTB;M{mgcm0> MUWyN|YyPDh7OB?=
M14 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmS2TWM2OD12NzDuUS=> NWnHT2pDOjN4MUS4PVg>
HT-29 MnuzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XEOGlEPTB;NUCgcm0> MlSzNlM3OTR6OUi=
8505C NFK2To5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXLOpVKSzVyPUWwJI5O NHrRRWczOzZzNEi5PC=>
HT-144 NWHs[49bT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nXZ2lEPTB;NkCgcm0> MViyN|YyPDh7OB?=
SK-Mel-5 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPLPIpKSzVyPU[2JI5O M3fSclI{PjF2OEm4
A375-SM M2HuVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\kTWM2OD15NTDuUS=> MV2yN|YyPDh7OB?=
SK-Mel-28 M2XQWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnKTWM2OD16NTDuUS=> NFe4NogzOzZzNEi5PC=>
LOX M1PIOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTFyMDDuUS=> NH;XTHEzOzZzNEi5PC=>
SK-Mel-3 NUm2TFM{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLaNldKSzVyPUGxPEBvVQ>? MkPJNlM3OTR6OUi=
K1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvkTWM2OD1zM{Cgcm0> NEfhdFAzOzZzNEi5PC=>
Hs-695T MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPPUY1KSzVyPUG2OUBvVQ>? MojONlM3OTR6OUi=
BHT-101 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTNyMDDuUS=> MlrjNlM3OTR6OUi=
RPMI-7951 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\Sd2lEPTB;M{S0JI5O M{Tx[|I{PjF2OEm4
A2058 NGX3[WpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXMTWM2OD1|NkCgcm0> NWfRXmFnOjN4MUS4PVg>
SK-Hep-1 MljYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTF2MkKgcm0> MmLkNlM3OTR6OUi=
A673 MmfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXOWZhKSzVyPUOwNFEhdk1? NYCwfYZEOjN4MUS4PVg>
DBTRG-05MG M2S3NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHBZ3lKSzVyPUOwNFEhdk1? MkDlNlM3OTR6OUi=
SW-626 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{G0WGlEPTB;M{Ogcm0> NEnM[oEzOzZzNEi5PC=>
LoVo MmX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXK[4NiUUN3ME20O{BvVQ>? MVGyN|YyPDh7OB?=
MiaPaCa MmD0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;GTWM2OD13MzDuUS=> NYnT[FB7OjN4MUS4PVg>
SW-620 M2H5SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4C4cGlEPTB;MUC0JI5O MXOyN|YyPDh7OB?=
CAPAN-1 M1\WRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rEOGlEPTB;MUC0JI5O M2Lr[|I{PjF2OEm4
SW-527 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPhS4pKSzVyPUGyNUBvVQ>? M17OfVI{PjF2OEm4
HCT-116 MmrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrTRYQxUUN3ME2xNlghdk1? M3r5SFI{PjF2OEm4
SW-480 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HuRmlEPTB;MU[1JI5O MmDTNlM3OTR6OUi=
HPAC NYLtTW9CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PIU2lEPTB;MUewJI5O M1r2bVI{PjF2OEm4
OVCAR-5 NVr5N|ZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XQTmlEPTB;MkC4JI5O NX;3S2JTOjN4MUS4PVg>
AsPc-1 MkTVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETTWHlKSzVyPUK3NEBvVQ>? NHHPN3AzOzZzNEi5PC=>
A549 NUS0co94T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XhcmlEPTB;M{K2JI5O NGOz[lgzOzZzNEi5PC=>
SNU-1 MnH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fQUWlEPTB;M{W0JI5O MlP5NlM3OTR6OUi=
HOP62 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo[5TWM2OD14N{[gcm0> M3HnblI{PjF2OEm4
H23 NILkbHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jPWGlEPTB;MUCwNEBvVQ>? NEn0dlgzOzZzNEi5PC=>
MB-231 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTFyMECgcm0> MWqyN|YyPDh7OB?=
SU.86.86 MoDvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTFyMEGgcm0> NWPHXJJoOjN4MUS4PVg>
CFPAC-1 NHXRWoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTFyMEGgcm0> NH7NNokzOzZzNEi5PC=>
A427 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfxbZRQUUN3ME2xOFM{KG6P NF3kRmEzOzZzNEi5PC=>
MDAH-2774 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTJ4NUegcm0> MkXZNlM3OTR6OUi=
NCI-H157 NX7JeHNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTNyMECgcm0> NYD3enJCOjN4MUS4PVg>
HTB-177 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTNyMECgcm0> MVOyN|YyPDh7OB?=
UM-UC-3 NEHWeG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjDcGNKSzVyPUOwNFEhdk1? Mn:1NlM3OTR6OUi=
HCT-8 NXvsW4E1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlexTWM2OD1|MECxJI5O NXLpcYF[OjN4MUS4PVg>
Panc-1 NYG4WnVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYriTotVUUN3ME2zNFAyKG6P NE\DflYzOzZzNEi5PC=>
DLD-1 NGfXXFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXYTWM2OD1|MECxJI5O M1vidFI{PjF2OEm4
HCT-15 NIrHOopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\pTmN1UUN3ME2zNFAyKG6P NFPOb2QzOzZzNEi5PC=>
HL-60 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{T0OGlEPTB;M{Cgcm0> MVKyN|YyPDh7OB?=
SK-Mel-2 M3u3fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXzTWM2OD1|NDDuUS=> NH\ocHUzOzZzNEi5PC=>
RD MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInvWZlKSzVyPUGyN{BvVQ>? MkTGNlM3OTR6OUi=
HT-1197 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nwTGlEPTB;M{G2JI5O NHm3dHIzOzZzNEi5PC=>
Molt-3 NGTxO|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\DfIp3UUN3ME22NFAhdk1? NYDDcVdjOjN4MUS4PVg>
PA-1 NGLKb4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2SwZWlEPTB;MUCwNUBvVQ>? NFnHdI8zOzZzNEi5PC=>
Molt-4 NX\CboV2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HBZWlEPTB;M{CwNUBvVQ>? NWLBepdIOjN4MUS4PVg>
NCI-H292 MkjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTlyIH7N NFL4ZoQzOzZzNEi5PC=>
A2780 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTF2MzDuUS=> MnXsNlM3OTR6OUi=
IGROV-1 M1rXV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFn0N4tKSzVyPUG0OkBvVQ>? MVGyN|YyPDh7OB?=
SK-N-SH M{PtcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTwfoFsUUN3ME2xOVAhdk1? NFjFW3YzOzZzNEi5PC=>
N-87 NEnkXFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3m1[mlEPTB;M{C3JI5O NIPEfoczOzZzNEi5PC=>
H322 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LqbGlEPTB;M{K1JI5O MkjBNlM3OTR6OUi=
H716 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3V[49CUUN3ME2zN|Qhdk1? M1G0clI{PjF2OEm4
TT MmXFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2npVWlEPTB;NEC2JI5O M{\2S|I{PjF2OEm4
Caki-1 M1XJR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPWTWM2OD12NUCgcm0> NXHCbGk4OjN4MUS4PVg>
5637 NHnMUXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITtSHJKSzVyPU[xNEBvVQ>? NEDLc2QzOzZzNEi5PC=>
MB-453 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHRTWM2OD14N{Kgcm0> NF;pPHQzOzZzNEi5PC=>
RT-4 NFj1TWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRThzMDDuUS=> Ml3NNlM3OTR6OUi=
HOP92 NVjWdJFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDhWpFCUUN3ME24NlAhdk1? M2S5elI{PjF2OEm4
KG-1 MkX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTlyMDDuUS=> NWTVVJRwOjN4MUS4PVg>
Hs-294T M{\PWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmj2TWM2OD17NEWgcm0> MXWyN|YyPDh7OB?=
SF-539 NVH6VVByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTrTWM2OD1zMECwJI5O MXKyN|YyPDh7OB?=
U-251 NEHvOZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\ETWM2OD1zMECwJI5O NFHYfFQzOzZzNEi5PC=>
MB-468 NFHhWlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XR[mlEPTB;MUCwNEBvVQ>? NFq5NnozOzZzNEi5PC=>
HS746T MkXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2jNOGlEPTB;MUCwNEBvVQ>? M1;2ZlI{PjF2OEm4
SCABER NFroc4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIX6WYVKSzVyPUGwNFAhdk1? NX7VO45[OjN4MUS4PVg>
MCF-7 M{jJOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXTRmpKSzVyPUGwNFEhdk1? MYeyN|YyPDh7OB?=
CHL-1 M3m0d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLBTWM2OD1zNE[wJI5O NXPjZZBMOjN4MUS4PVg>
U87MG MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfHPG1KSzVyPUKwNFAhdk1? MnPSNlM3OTR6OUi=
SJCRH30 MnrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTJyMEKgcm0> MWWyN|YyPDh7OB?=
ES-2 NUm3WlNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPqdlRoUUN3ME2yOlU6KG6P NWnXdm02OjN4MUS4PVg>
HT-1376 NX;hSGtyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnmyTWM2OD1{OECwJI5O MVuyN|YyPDh7OB?=
A172 NXTqOFd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{iycWlEPTB;M{CwNEBvVQ>? MmjxNlM3OTR6OUi=
769P NXL3XnBZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPzc4plUUN3ME2zNFAxKG6P NIXUW3QzOzZzNEi5PC=>
NCI-H520 NWDEVZZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTTVlI1UUN3ME2zNFAxKG6P M3jPeVI{PjF2OEm4
DU145 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;pe2lEPTB;M{CwNEBvVQ>? NULqRXJrOjN4MUS4PVg>
K562 NGTiVWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTqVHNJUUN3ME2zNFAxKG6P NXO2T3pwOjN4MUS4PVg>
U-937 MnjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDoTWM2OD1|MECwJI5O NWj6XW9kOjN4MUS4PVg>
A204 M3rzPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTNyMEGgcm0> NEnqcJozOzZzNEi5PC=>
DAOY MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTNyMEGgcm0> M4fQS|I{PjF2OEm4
SF-268 MlrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3Sxb2lEPTB;M{CwNUBvVQ>? MWCyN|YyPDh7OB?=
SF-295 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnETWM2OD1|MECxJI5O NXnneHNvOjN4MUS4PVg>
SNB-19 M4DsfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPzfVlKSzVyPUOwNFEhdk1? NVnQR|RXOjN4MUS4PVg>
SNB-75 NFvUZ5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHXZVhXUUN3ME2zNFAyKG6P MWOyN|YyPDh7OB?=
U373-MG NVO1[lZET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTNyMEGgcm0> NEG4emUzOzZzNEi5PC=>
786-O MnLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHWTWM2OD1|MECxJI5O M2LXSFI{PjF2OEm4
A498 NXm2RpdIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTNyMEGgcm0> MVGyN|YyPDh7OB?=
ACHN MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzVd2xKSzVyPUOwNFEhdk1? M2js[lI{PjF2OEm4
EKVX MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml30TWM2OD1|MECxJI5O MV:yN|YyPDh7OB?=
H226 NU\xc3hNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPDXFFzUUN3ME2zNFAyKG6P M1P6eVI{PjF2OEm4
H522 NUfqXlZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHPRb|BKSzVyPUOwNFEhdk1? MYiyN|YyPDh7OB?=
HeLa NEXSXolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLhW4hKSzVyPUOwNFEhdk1? NYD0ZWREOjN4MUS4PVg>
SK-OV-3 NEDte3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fxfGlEPTB;M{CwNUBvVQ>? M1z5T|I{PjF2OEm4
Ln Cap MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTNyMEGgcm0> NVrxR2JjOjN4MUS4PVg>
PC3 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHr5T3VKSzVyPUOwNFEhdk1? MXGyN|YyPDh7OB?=
SNU-16 MnHFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTNyMEGgcm0> NXX0dnRwOjN4MUS4PVg>
FTC-133 NW\GOGZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWOxVHFOUUN3ME2zNFAyKG6P MUKyN|YyPDh7OB?=
Ro82-W-1 MmDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXiyTVFnUUN3ME2zNFAyKG6P NWi4SFBPOjN4MUS4PVg>
Daudi NVvxOG41T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrMeWJ[UUN3ME2zNFAyKG6P M2O5bFI{PjF2OEm4
Jijoye NX7lTJpRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrHRXVSUUN3ME2zNFAyKG6P Mn3QNlM3OTR6OUi=
Jurkat NHLtVJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vZWGlEPTB;M{CwNUBvVQ>? M3ftZVI{PjF2OEm4
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TCC-SUP NWDwU2k2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTNyMEGgcm0> MkXnNlM3OTR6OUi=
BT-474 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLITWM2OD1|MECxJI5O NH:wUWUzOzZzNEi5PC=>
ZR-75-1 M{nPVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTNyMEGgcm0> M4LXXVI{PjF2OEm4

... 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 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)

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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
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* 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

Related Antibodies

ERK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID