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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Cited by 257 Publications

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 NEnYO2NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjXXoJpUUN3ME2wMlI1KG6P MUCyOVM2ODl|MR?=
WM-266-4 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTJyIH7N M3\PblI{PjF2OEm4
UACC-62 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLsTWM2OD1|MDDuUS=> NHz0VngzOzZzNEi5PC=>
Colo-205 Mnm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDnTWM2OD1|NjDuUS=> MXGyN|YyPDh7OB?=
SK-Mel-1 NHuzV|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37Xe2lEPTB;M{egcm0> MoTyNlM3OTR6OUi=
WiDr M1X4Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PvbmlEPTB;M{mgcm0> MmG5NlM3OTR6OUi=
M14 NX7xdIF[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PtbmlEPTB;NEegcm0> NWLWR4tlOjN4MUS4PVg>
HT-29 Mn\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7QZ5dvUUN3ME21NEBvVQ>? MWGyN|YyPDh7OB?=
8505C NGTwdINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\YbYhjUUN3ME21NEBvVQ>? Mn23NlM3OTR6OUi=
HT-144 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDTTWM2OD14MDDuUS=> NH;IVpkzOzZzNEi5PC=>
SK-Mel-5 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\Pc5JxUUN3ME22OkBvVQ>? MWWyN|YyPDh7OB?=
A375-SM MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXCTmtKSzVyPUe1JI5O M33kWFI{PjF2OEm4
SK-Mel-28 NGDUcYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml32TWM2OD16NTDuUS=> NFTWd3EzOzZzNEi5PC=>
LOX MoLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnq4TWM2OD1zMECgcm0> NVfxd3VuOjN4MUS4PVg>
SK-Mel-3 NUSwb4JqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPoTWM2OD1zMUigcm0> NGH5S2kzOzZzNEi5PC=>
K1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXJZ3dKSzVyPUGzNEBvVQ>? NH\WOVczOzZzNEi5PC=>
Hs-695T Mnn3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkSyTWM2OD1zNkWgcm0> MWiyN|YyPDh7OB?=
BHT-101 M2\3e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfJO3pQUUN3ME2zNFAhdk1? Moi3NlM3OTR6OUi=
RPMI-7951 M1P1dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2\ZXGlEPTB;M{S0JI5O MYeyN|YyPDh7OB?=
A2058 NX[xcHlsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnWzTWM2OD1|NkCgcm0> MmXINlM3OTR6OUi=
SK-Hep-1 Ml7vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTF2MkKgcm0> MkjuNlM3OTR6OUi=
A673 M13rPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4f0dmlEPTB;M{CwNUBvVQ>? NEK2N2gzOzZzNEi5PC=>
DBTRG-05MG MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\ETWM2OD1|MECxJI5O M1nkRlI{PjF2OEm4
SW-626 NF3lXJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTN|IH7N MnTyNlM3OTR6OUi=
LoVo NWfafG5LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1;6UWlEPTB;NEegcm0> M3HiO|I{PjF2OEm4
MiaPaCa MlTHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjiTWM2OD13MzDuUS=> MkLPNlM3OTR6OUi=
SW-620 M4TBU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVy2TFR4UUN3ME2xNFQhdk1? Ml;NNlM3OTR6OUi=
CAPAN-1 Ml;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\iXGlEPTB;MUC0JI5O MkjhNlM3OTR6OUi=
SW-527 NE\qWYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3y0dWlEPTB;MUKxJI5O NHTvZYMzOzZzNEi5PC=>
HCT-116 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\JepBKSzVyPUGyPEBvVQ>? MmHtNlM3OTR6OUi=
SW-480 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1[0U2lEPTB;MU[1JI5O Mn7yNlM3OTR6OUi=
HPAC MnL4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTF5MDDuUS=> NH7tOIYzOzZzNEi5PC=>
OVCAR-5 MnLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HyN2lEPTB;MkC4JI5O NF70ZWQzOzZzNEi5PC=>
AsPc-1 M2DJOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTJ5MDDuUS=> NVrMR2Y6OjN4MUS4PVg>
A549 NIfpfWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGPyboNKSzVyPUOyOkBvVQ>? NYnP[5NIOjN4MUS4PVg>
SNU-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrGZpFKSzVyPUO1OEBvVQ>? NHP3c4wzOzZzNEi5PC=>
HOP62 MnG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTZ5NjDuUS=> MX[yN|YyPDh7OB?=
H23 Mm\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3y[IVKSzVyPUGwNFAhdk1? NGnuc40zOzZzNEi5PC=>
MB-231 MnTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrLd3g2UUN3ME2xNFAxKG6P NVfCUHBtOjN4MUS4PVg>
SU.86.86 NV60WGV4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTFyMEGgcm0> MVSyN|YyPDh7OB?=
CFPAC-1 NEjxWlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF35d3dKSzVyPUGwNFEhdk1? M1rRO|I{PjF2OEm4
A427 NXzZT2JRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3m3dmlEPTB;MUSzN{BvVQ>? MnXPNlM3OTR6OUi=
MDAH-2774 NHTTUZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHBfXZqUUN3ME2yOlU4KG6P NH\lOmEzOzZzNEi5PC=>
NCI-H157 NFHZNJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofvTWM2OD1|MECwJI5O MmfkNlM3OTR6OUi=
HTB-177 NHH4WlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXzPVRKSzVyPUOwNFAhdk1? NH;0enQzOzZzNEi5PC=>
UM-UC-3 NYHqblI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTNyMEGgcm0> Mmi1NlM3OTR6OUi=
HCT-8 M1XhVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nJXGlEPTB;M{CwNUBvVQ>? MlfJNlM3OTR6OUi=
Panc-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4i0W2lEPTB;M{CwNUBvVQ>? MkHKNlM3OTR6OUi=
DLD-1 NIm0Zm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTPN5IyUUN3ME2zNFAyKG6P NXjGeml7OjN4MUS4PVg>
HCT-15 MnnoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrWfIxKSzVyPUOwNFEhdk1? MX:yN|YyPDh7OB?=
HL-60 M3rROGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTnU2dKSzVyPUOwJI5O NFrSTGMzOzZzNEi5PC=>
SK-Mel-2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlPrTWM2OD1|NDDuUS=> M{naO|I{PjF2OEm4
RD MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPOeZVKSzVyPUGyN{BvVQ>? M4WyN|I{PjF2OEm4
HT-1197 NILPeZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rwbmlEPTB;M{G2JI5O NXX0b3dNOjN4MUS4PVg>
Molt-3 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jaeGlEPTB;NkCwJI5O M3S4TlI{PjF2OEm4
PA-1 M1exNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LNVGlEPTB;MUCwNUBvVQ>? NYH4d49TOjN4MUS4PVg>
Molt-4 NH7pcm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfKXG5yUUN3ME2zNFAyKG6P NV\E[4pjOjN4MUS4PVg>
NCI-H292 M2DRe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTlyIH7N NV3xOGllOjN4MUS4PVg>
A2780 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTF2MzDuUS=> M2TCcVI{PjF2OEm4
IGROV-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTF2NjDuUS=> MUWyN|YyPDh7OB?=
SK-N-SH MnXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXH1cnlqUUN3ME2xOVAhdk1? M4WwXFI{PjF2OEm4
N-87 MnjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\5UIJKSzVyPUOwO{BvVQ>? MmDLNlM3OTR6OUi=
H322 NWfwWYcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjzWIhKSzVyPUOyOUBvVQ>? MV2yN|YyPDh7OB?=
H716 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrrZmVwUUN3ME2zN|Qhdk1? MWSyN|YyPDh7OB?=
TT NV7vWItzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\YT2NOUUN3ME20NFYhdk1? NHz0WHAzOzZzNEi5PC=>
Caki-1 M2T0W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XESmlEPTB;NEWwJI5O MWmyN|YyPDh7OB?=
5637 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{j5PGlEPTB;NkGwJI5O M37pblI{PjF2OEm4
MB-453 M1fRU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvEWWs4UUN3ME22O|Ihdk1? NVP0O5NlOjN4MUS4PVg>
RT-4 NHLsRoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGCzbY5KSzVyPUixNEBvVQ>? MV[yN|YyPDh7OB?=
HOP92 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofzTWM2OD16MkCgcm0> M4PKOFI{PjF2OEm4
KG-1 NXrublJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTlyMDDuUS=> MWeyN|YyPDh7OB?=
Hs-294T MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTl2NTDuUS=> MnH0NlM3OTR6OUi=
SF-539 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGj0W3JKSzVyPUGwNFAhdk1? MVqyN|YyPDh7OB?=
U-251 NHu4cnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHTZZFKSzVyPUGwNFAhdk1? NELtOogzOzZzNEi5PC=>
MB-468 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PrWWlEPTB;MUCwNEBvVQ>? Ml\qNlM3OTR6OUi=
HS746T MlOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLMV3NKSzVyPUGwNFAhdk1? MkDPNlM3OTR6OUi=
SCABER NHz3fZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWniPIxOUUN3ME2xNFAxKG6P MlG1NlM3OTR6OUi=
MCF-7 M2DSWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXDVlhZUUN3ME2xNFAyKG6P MYOyN|YyPDh7OB?=
CHL-1 MlK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTF2NkCgcm0> MlrnNlM3OTR6OUi=
U87MG MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPJUopnUUN3ME2yNFAxKG6P MWqyN|YyPDh7OB?=
SJCRH30 NWHUVWtGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnKzTWM2OD1{MECyJI5O NVuzWW9LOjN4MUS4PVg>
ES-2 MnrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonnTWM2OD1{NkW5JI5O M4HQR|I{PjF2OEm4
HT-1376 NHXQbWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2r3OmlEPTB;MkiwNEBvVQ>? NUTWOVlEOjN4MUS4PVg>
A172 NXrtcpFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HqZmlEPTB;M{CwNEBvVQ>? M4PnbVI{PjF2OEm4
769P MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTNyMECgcm0> NX30cGM1OjN4MUS4PVg>
NCI-H520 M1n1PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmT3TWM2OD1|MECwJI5O M4W1[|I{PjF2OEm4
DU145 MmnMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXqw[5hDUUN3ME2zNFAxKG6P M4LwOFI{PjF2OEm4
K562 MoO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jJeWlEPTB;M{CwNEBvVQ>? MU[yN|YyPDh7OB?=
U-937 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXvTWM2OD1|MECwJI5O NXz1b5F4OjN4MUS4PVg>
A204 M1zJ[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjDTWM2OD1|MECxJI5O MVuyN|YyPDh7OB?=
DAOY MlOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrNTWM2OD1|MECxJI5O MmCzNlM3OTR6OUi=
SF-268 M2\Xemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnWToFKSzVyPUOwNFEhdk1? M1jTZlI{PjF2OEm4
SF-295 MnjIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jiW2lEPTB;M{CwNUBvVQ>? MWCyN|YyPDh7OB?=
SNB-19 MkXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVWwWI11UUN3ME2zNFAyKG6P NYKxRWpFOjN4MUS4PVg>
SNB-75 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXFVYlKSzVyPUOwNFEhdk1? M1:0T|I{PjF2OEm4
U373-MG M3jNfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHBbW9KSzVyPUOwNFEhdk1? NILhclczOzZzNEi5PC=>
786-O MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTNyMEGgcm0> MVKyN|YyPDh7OB?=
A498 Ml2zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3jb5kzUUN3ME2zNFAyKG6P NGPuXVEzOzZzNEi5PC=>
ACHN MnuyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XKWmlEPTB;M{CwNUBvVQ>? MWiyN|YyPDh7OB?=
EKVX NHjjUplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlf1TWM2OD1|MECxJI5O NXjORmRXOjN4MUS4PVg>
H226 NGrLXohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\Pb5dKSzVyPUOwNFEhdk1? NGjrVlgzOzZzNEi5PC=>
H522 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoCwTWM2OD1|MECxJI5O NHnh[|czOzZzNEi5PC=>
HeLa M1XYPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUnJR|UxRTNyMEGgcm0> NIjSR5QzOzZzNEi5PC=>
SK-OV-3 NG\wV2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;WTWM2OD1|MECxJI5O M2HOVFI{PjF2OEm4
Ln Cap MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjtTWM2OD1|MECxJI5O M4[4NVI{PjF2OEm4
PC3 NXXHVoZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVf1Rmo3UUN3ME2zNFAyKG6P M{Tuc|I{PjF2OEm4
SNU-16 NXP4WVM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH7zNG9KSzVyPUOwNFEhdk1? MVOyN|YyPDh7OB?=
FTC-133 NXG1e3V{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYr0NYJtUUN3ME2zNFAyKG6P MV[yN|YyPDh7OB?=
Ro82-W-1 NHHuNlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV7JR|UxRTNyMEGgcm0> NGjJVoUzOzZzNEi5PC=>
Daudi NEDGSlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPBUmZyUUN3ME2zNFAyKG6P MVuyN|YyPDh7OB?=
Jijoye M2L4Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXRTWM2OD1|MECxJI5O M4D2TlI{PjF2OEm4
Jurkat MknaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrITWM2OD1|MECxJI5O MWGyN|YyPDh7OB?=
J-82 M2\hcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTNyMEGgcm0> MViyN|YyPDh7OB?=
TCC-SUP M2nwcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTNyMEGgcm0> MVGyN|YyPDh7OB?=
BT-474 NIq0bYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTNyMEGgcm0> MXqyN|YyPDh7OB?=
ZR-75-1 MlX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXGSHJKSzVyPUOwNFEhdk1? NV72SXYxOjN4MUS4PVg>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
cyclin B1 / cyclin D1 / p21; 

PubMed: 26725216     


Cells treated as above were collected for western blot for total cyclin B1, cyclin D1 and p21, and of phosphorylated, inactivated RB (S807/811; pRB). Western blot for pERK was done to verify SCH772984 inhibition; β-actin was the loading control.

pRSK / pERK / pAKT / pMEK; 

PubMed: 26725216     


Cells were treated for 4 or 24 hr with DMSO vehicle or SCH772984, then evaluated by western blot with phospho-specific antibodies for RSK (T395/S363; pRSK), MEK1/2 (S217/221; pMEK), AKT (S473; pAKT), and ERK (T202/Y204; pERK). Total RSK, ERK, AKT, MEK and β-actin were also analyzed. Data are representative of three independent experiments.

DUSP1 / DUSP4 / DUSP6; 

PubMed: 26725216     


Cells were treated for 4 or 24 hr with DMSO vehicle or SCH772984 for 72 hr and evaluated by western blot for DUSP1, DUSP4, DUSP6 and β-actin.

pCRAF(S338, S289, S296, S301); 

PubMed: 26725216     


Cells were treated for 4 or 24 hr with DMSO vehicle or SCH772984 for 72 hr and evaluated by western blot for pCRAF (S338), pCRAF (S289/296/301), total CRAF and β-actin.

Aurora B / ETS1 / ETS2; 

PubMed: 26725216     


Cells were treated with vehicle or SCH772984 for 7 days, then immunoblotted for Aurora B, MYC, ETS1 or ETS2, and β-actin. Data are representative of three independent experiments.

26725216
Growth inhibition assay
Cell viability; 

PubMed: 30118499     


NCI-H747, SW837, SW480, and SW620 cells were treated with the ERK inhibitor SCH772984 at indicated concentrations for 72 hours. Dimethyl sulfoxide (DMSO) (0.01%) was used as the control treatment. Each data point represents the mean of five replicates; error bars indicate one SD.

30118499
Immunofluorescence
TOMM20; 

PubMed: 30833752     


Mitochondrial morphologies of PDAC cells treated with SCH772984 (ERKi, 1 µM) for 24 h. Green, Anti-TOMM20; blue, DAPI; scale bar, 20 μm.

pERK1/2; 

PubMed: 30213106     


After treatment with 10 µM of the ERIK1/2 inhibitors, the expression of p-ERK1/2 protein in HeLa cells was detected using immunofluorescence (400×), bar = 50 μm.

30833752 30213106
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 (mg) = Concentration (mM) × Volume (mL) × 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