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, 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 MnjDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTBwMkSgcm0> MYiyOVM2ODl|MR?=
WM-266-4 NE\6dllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLqTWM2OD1{MDDuUS=> NIfDVVQzOzZzNEi5PC=>
UACC-62 M3jndmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTNyIH7N NGXh[mEzOzZzNEi5PC=>
Colo-205 MlPZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TpeGlEPTB;M{[gcm0> NWTZZ4tzOjN4MUS4PVg>
SK-Mel-1 NEDsZmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rWbGlEPTB;M{egcm0> MkOyNlM3OTR6OUi=
WiDr MnXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTN7IH7N MmDiNlM3OTR6OUi=
M14 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfkTWM2OD12NzDuUS=> NIC1elYzOzZzNEi5PC=>
HT-29 NY[5SGU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX;JR|UxRTVyIH7N M4ja[FI{PjF2OEm4
8505C NHHld3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLEcpZKSzVyPUWwJI5O MUCyN|YyPDh7OB?=
HT-144 MoTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\x[JdKSzVyPU[wJI5O NE\FZXMzOzZzNEi5PC=>
SK-Mel-5 NH7KcY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTZ4IH7N NEi3SW4zOzZzNEi5PC=>
A375-SM Mo\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTd3IH7N M2fIblI{PjF2OEm4
SK-Mel-28 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPWfopKSzVyPUi1JI5O Ml;tNlM3OTR6OUi=
LOX NGnBSHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVnJR|UxRTFyMDDuUS=> NFrNRpYzOzZzNEi5PC=>
SK-Mel-3 M4rPUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPPTWM2OD1zMUigcm0> M1jFdVI{PjF2OEm4
K1 MkLoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLOXHdWUUN3ME2xN|Ahdk1? MljmNlM3OTR6OUi=
Hs-695T MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnXNVZKSzVyPUG2OUBvVQ>? Mn62NlM3OTR6OUi=
BHT-101 MnfSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLUTWM2OD1|MECgcm0> Mn3ONlM3OTR6OUi=
RPMI-7951 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\6TWM2OD1|NESgcm0> NXfie5dTOjN4MUS4PVg>
A2058 Ml7LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUjhXWttUUN3ME2zOlAhdk1? NXz4bJdvOjN4MUS4PVg>
SK-Hep-1 MmO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTF2MkKgcm0> MmnSNlM3OTR6OUi=
A673 MmPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HxRWlEPTB;M{CwNUBvVQ>? MnTXNlM3OTR6OUi=
DBTRG-05MG NHfD[JlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17Ne2lEPTB;M{CwNUBvVQ>? NVPRN4ROOjN4MUS4PVg>
SW-626 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoHjTWM2OD1|MzDuUS=> MnzZNlM3OTR6OUi=
LoVo NIjP[GtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DZUmlEPTB;NEegcm0> NV3LflVXOjN4MUS4PVg>
MiaPaCa M37qb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{O1[WlEPTB;NUOgcm0> M2DBR|I{PjF2OEm4
SW-620 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;PdWlEPTB;MUC0JI5O NGTlNlEzOzZzNEi5PC=>
CAPAN-1 M2X5SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLITWM2OD1zMESgcm0> MXWyN|YyPDh7OB?=
SW-527 NUDLOW1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlzVTWM2OD1zMkGgcm0> MY[yN|YyPDh7OB?=
HCT-116 MnPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\ub4ZvUUN3ME2xNlghdk1? M2XOblI{PjF2OEm4
SW-480 NW\KdW9mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vE[GlEPTB;MU[1JI5O MXuyN|YyPDh7OB?=
HPAC NG\jOVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmj2TWM2OD1zN{Cgcm0> NX7zUFhJOjN4MUS4PVg>
OVCAR-5 NFLmVYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTJyODDuUS=> Ml;VNlM3OTR6OUi=
AsPc-1 M4\mb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jaNmlEPTB;MkewJI5O NWLp[FBvOjN4MUS4PVg>
A549 NX\3ZplCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjwNo5KSzVyPUOyOkBvVQ>? MoH2NlM3OTR6OUi=
SNU-1 NYjDdpllT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEmxcHRKSzVyPUO1OEBvVQ>? M17ERlI{PjF2OEm4
HOP62 NH7Q[nhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGD0WYdKSzVyPU[3OkBvVQ>? NVrsXoZwOjN4MUS4PVg>
H23 NFXsT5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTFyMECgcm0> MYmyN|YyPDh7OB?=
MB-231 NGq5O|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13OVWlEPTB;MUCwNEBvVQ>? MY[yN|YyPDh7OB?=
SU.86.86 MkDTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2X3U2lEPTB;MUCwNUBvVQ>? NXnQb3pEOjN4MUS4PVg>
CFPAC-1 NHzlWpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEnHVlRKSzVyPUGwNFEhdk1? MkWxNlM3OTR6OUi=
A427 NGrITWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknRTWM2OD1zNEOzJI5O NYH0T4xzOjN4MUS4PVg>
MDAH-2774 NILOOY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVrqV|A{UUN3ME2yOlU4KG6P MnHXNlM3OTR6OUi=
NCI-H157 NXTlZmx4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2LjNWlEPTB;M{CwNEBvVQ>? NX\seVh4OjN4MUS4PVg>
HTB-177 NEGwfopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlrsTWM2OD1|MECwJI5O MoLjNlM3OTR6OUi=
UM-UC-3 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDzSoZKSzVyPUOwNFEhdk1? MojGNlM3OTR6OUi=
HCT-8 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULiPWxFUUN3ME2zNFAyKG6P NVj3NIRQOjN4MUS4PVg>
Panc-1 M3vKWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2W1[GlEPTB;M{CwNUBvVQ>? NYrqb2ZYOjN4MUS4PVg>
DLD-1 M3;3emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PQUGlEPTB;M{CwNUBvVQ>? NYfTdG5iOjN4MUS4PVg>
HCT-15 M4rCZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTNyMEGgcm0> MU[yN|YyPDh7OB?=
HL-60 NVizOnB7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLROo9KSzVyPUOwJI5O NHzRc5YzOzZzNEi5PC=>
SK-Mel-2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTN2IH7N M1z5V|I{PjF2OEm4
RD NYXGWohRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTF{MzDuUS=> MX6yN|YyPDh7OB?=
HT-1197 M4HDeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3ydpc4UUN3ME2zNVYhdk1? NHjvXYMzOzZzNEi5PC=>
Molt-3 M3HhTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3hUmdKSzVyPU[wNEBvVQ>? NWKwOodXOjN4MUS4PVg>
PA-1 Mn;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TzWmlEPTB;MUCwNUBvVQ>? NITjS2ozOzZzNEi5PC=>
Molt-4 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1W0UmlEPTB;M{CwNUBvVQ>? MnnRNlM3OTR6OUi=
NCI-H292 NVi2Z|JzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXsTWM2OD17MDDuUS=> Mle5NlM3OTR6OUi=
A2780 NGHCfIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7rbWFEUUN3ME2xOFMhdk1? M2T4VlI{PjF2OEm4
IGROV-1 MlzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\Zd3JKSzVyPUG0OkBvVQ>? NUHCZ4hPOjN4MUS4PVg>
SK-N-SH MoLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfZTWM2OD1zNUCgcm0> NHLYUYEzOzZzNEi5PC=>
N-87 NF\QN45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDoU48zUUN3ME2zNFchdk1? M4XGdVI{PjF2OEm4
H322 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnmwTWM2OD1|MkWgcm0> MljRNlM3OTR6OUi=
H716 MmjpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HUc2lEPTB;M{O0JI5O Mo\JNlM3OTR6OUi=
TT MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPQOFZKSzVyPUSwOkBvVQ>? NUKwXHVXOjN4MUS4PVg>
Caki-1 MkCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTR3MDDuUS=> NIWzSVczOzZzNEi5PC=>
5637 MnrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIThS2hKSzVyPU[xNEBvVQ>? NFr0XJYzOzZzNEi5PC=>
MB-453 NX\qW5pJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoG4TWM2OD14N{Kgcm0> NIr6NHIzOzZzNEi5PC=>
RT-4 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTMc4o4UUN3ME24NVAhdk1? NX20d5lmOjN4MUS4PVg>
HOP92 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{Xa[2lEPTB;OEKwJI5O M1LhV|I{PjF2OEm4
KG-1 NFKwVW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIHJcpBKSzVyPUmwNEBvVQ>? MYOyN|YyPDh7OB?=
Hs-294T NUDMd2p{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4S3bGlEPTB;OUS1JI5O M3nIblI{PjF2OEm4
SF-539 NXHDb|dDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXrT45OUUN3ME2xNFAxKG6P MX6yN|YyPDh7OB?=
U-251 NWPNZ2hPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWK4R25PUUN3ME2xNFAxKG6P M37GblI{PjF2OEm4
MB-468 Mk\rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHX6PHZKSzVyPUGwNFAhdk1? MY[yN|YyPDh7OB?=
HS746T MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTFyMECgcm0> NUf1VYdKOjN4MUS4PVg>
SCABER M3Xoc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTFyMECgcm0> NEfGS5czOzZzNEi5PC=>
MCF-7 Mn7BS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXpUXQ5UUN3ME2xNFAyKG6P M1GzNVI{PjF2OEm4
CHL-1 MmjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13nTmlEPTB;MUS2NEBvVQ>? M3LTUVI{PjF2OEm4
U87MG MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1naN2lEPTB;MkCwNEBvVQ>? NViyPJI5OjN4MUS4PVg>
SJCRH30 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIjTSo5KSzVyPUKwNFIhdk1? M4PPbFI{PjF2OEm4
ES-2 Mn7QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfxUolKSzVyPUK2OVkhdk1? MV:yN|YyPDh7OB?=
HT-1376 NGXzV|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3yVZFoUUN3ME2yPFAxKG6P NWHD[m5COjN4MUS4PVg>
A172 MkO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\KdWlEPTB;M{CwNEBvVQ>? NFjE[5IzOzZzNEi5PC=>
769P M4D4TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nKdmlEPTB;M{CwNEBvVQ>? NV\pT4JJOjN4MUS4PVg>
NCI-H520 MnnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTNyMECgcm0> M2[5clI{PjF2OEm4
DU145 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEexbGVKSzVyPUOwNFAhdk1? M1TpXVI{PjF2OEm4
K562 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7ne4RZUUN3ME2zNFAxKG6P NFHOV2ozOzZzNEi5PC=>
U-937 Mn:3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHxbXNZUUN3ME2zNFAxKG6P MkXENlM3OTR6OUi=
A204 M37iNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvnT|JKSzVyPUOwNFEhdk1? NVzWbYVMOjN4MUS4PVg>
DAOY NX\neoFTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mke0TWM2OD1|MECxJI5O MWeyN|YyPDh7OB?=
SF-268 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LRVWlEPTB;M{CwNUBvVQ>? NYPG[JpTOjN4MUS4PVg>
SF-295 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI[5ZXdKSzVyPUOwNFEhdk1? M3\0SVI{PjF2OEm4
SNB-19 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPIRZFPUUN3ME2zNFAyKG6P NEXXflIzOzZzNEi5PC=>
SNB-75 MnnhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTNyMEGgcm0> MYOyN|YyPDh7OB?=
U373-MG MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofzTWM2OD1|MECxJI5O NVr2dphOOjN4MUS4PVg>
786-O NGLMb3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoH4TWM2OD1|MECxJI5O NVq3O5h5OjN4MUS4PVg>
A498 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4flWmlEPTB;M{CwNUBvVQ>? M{\SW|I{PjF2OEm4
ACHN NVz5[GNmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVnsU4xJUUN3ME2zNFAyKG6P MoraNlM3OTR6OUi=
EKVX MljNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWT1eI1[UUN3ME2zNFAyKG6P NG\NUoszOzZzNEi5PC=>
H226 NV23d|lZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTNyMEGgcm0> M1vXeVI{PjF2OEm4
H522 NYP0cYlHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTNyMEGgcm0> MYWyN|YyPDh7OB?=
HeLa M4H0eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETqfVZKSzVyPUOwNFEhdk1? NUDCVlZ1OjN4MUS4PVg>
SK-OV-3 NGrrZ21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7xTWM2OD1|MECxJI5O MV:yN|YyPDh7OB?=
Ln Cap M4ewcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\yTWM2OD1|MECxJI5O Ml;hNlM3OTR6OUi=
PC3 NW\OXlJFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXLJR|UxRTNyMEGgcm0> M3;Je|I{PjF2OEm4
SNU-16 NV;QU|lMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHiZZJ3UUN3ME2zNFAyKG6P M{LndVI{PjF2OEm4
FTC-133 Mn3FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2fCbGlEPTB;M{CwNUBvVQ>? NG\VdoYzOzZzNEi5PC=>
Ro82-W-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7WeGhvUUN3ME2zNFAyKG6P NUHYcYN[OjN4MUS4PVg>
Daudi NEjVSVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTNyMEGgcm0> MUGyN|YyPDh7OB?=
Jijoye MnvwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTNyMEGgcm0> M17CRVI{PjF2OEm4
Jurkat NGjyZnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\ScGlEPTB;M{CwNUBvVQ>? NYPpfZQ6OjN4MUS4PVg>
J-82 NV3mVlJTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLqfYxrUUN3ME2zNFAyKG6P NXe5fpNvOjN4MUS4PVg>
TCC-SUP M3LWSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTNyMEGgcm0> MoXyNlM3OTR6OUi=
BT-474 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTNyMEGgcm0> Mne0NlM3OTR6OUi=
ZR-75-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTNyMEGgcm0> NXT2fnZHOjN4MUS4PVg>

... 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
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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