SCH772984

For research use only.

Catalog No.S7101

280 publications

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.

Size Price Stock Quantity  
USD 270 In stock
USD 1070 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Selleck's SCH772984 has been cited by 280 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 M17MS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrQSGZKSzVyPUCuNlQhdk1? NUe5dpRSOjV|NUC5N|E>
WM-266-4 M2rHbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfCTWM2OD1{MDDuUS=> M1\1d|I{PjF2OEm4
UACC-62 NVL1cVdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTNyIH7N M2DUO|I{PjF2OEm4
Colo-205 M4HCdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTsNIgzUUN3ME2zOkBvVQ>? NGnMUI8zOzZzNEi5PC=>
SK-Mel-1 M4\QWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\y[GdOUUN3ME2zO{BvVQ>? NXjkXYh1OjN4MUS4PVg>
WiDr M4PpWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7jOllZUUN3ME2zPUBvVQ>? MV[yN|YyPDh7OB?=
M14 M{PST2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrM[G1KSzVyPUS3JI5O NUjK[XN6OjN4MUS4PVg>
HT-29 M3qx[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIW1N3lKSzVyPUWwJI5O M3nFclI{PjF2OEm4
8505C NU\T[JZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1izU2lEPTB;NUCgcm0> M1XXVlI{PjF2OEm4
HT-144 NE\Qc2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzSTWM2OD14MDDuUS=> MV[yN|YyPDh7OB?=
SK-Mel-5 NFL3bHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLO[Y5KSzVyPU[2JI5O NVLuOng1OjN4MUS4PVg>
A375-SM MlXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTd3IH7N MlzkNlM3OTR6OUi=
SK-Mel-28 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXm1c4ZkUUN3ME24OUBvVQ>? MWOyN|YyPDh7OB?=
LOX MlOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITGPWNKSzVyPUGwNEBvVQ>? M1TRdFI{PjF2OEm4
SK-Mel-3 NGHBdmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\4VmlEPTB;MUG4JI5O MYKyN|YyPDh7OB?=
K1 Moe5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XJVWlEPTB;MUOwJI5O NWTJ[YtCOjN4MUS4PVg>
Hs-695T MlTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HvWGlEPTB;MU[1JI5O MWqyN|YyPDh7OB?=
BHT-101 NXTpPY55T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTNyMDDuUS=> MWeyN|YyPDh7OB?=
RPMI-7951 NVflO483T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfWOotKSzVyPUO0OEBvVQ>? MV:yN|YyPDh7OB?=
A2058 NVjFWlhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTN4MDDuUS=> M4nKe|I{PjF2OEm4
SK-Hep-1 NECyO3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPoTWM2OD1zNEKyJI5O NVnzXFZLOjN4MUS4PVg>
A673 M3rK[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHCTWM2OD1|MECxJI5O M2jEflI{PjF2OEm4
DBTRG-05MG M2ryU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWWzdWJ2UUN3ME2zNFAyKG6P NHPKXFMzOzZzNEi5PC=>
SW-626 M121VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn[wTWM2OD1|MzDuUS=> NWKwdJdlOjN4MUS4PVg>
LoVo MlW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\4TWM2OD12NzDuUS=> MoTLNlM3OTR6OUi=
MiaPaCa NVOweVNwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH63S|NKSzVyPUWzJI5O M37nTlI{PjF2OEm4
SW-620 NE\2NY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfzZWpNUUN3ME2xNFQhdk1? MkTxNlM3OTR6OUi=
CAPAN-1 NV61PVRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLmOHlKSzVyPUGwOEBvVQ>? Mmj4NlM3OTR6OUi=
SW-527 NGeyTGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUD0U3c{UUN3ME2xNlEhdk1? NYLBTIp{OjN4MUS4PVg>
HCT-116 M3\XPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTxTWM2OD1zMkigcm0> Mn3rNlM3OTR6OUi=
SW-480 NInV[FZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTF4NTDuUS=> M{O4ZVI{PjF2OEm4
HPAC NWPq[YxlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Hu[mlEPTB;MUewJI5O Mn;PNlM3OTR6OUi=
OVCAR-5 NXTwXZRMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYr6eFJlUUN3ME2yNFghdk1? NGDL[FAzOzZzNEi5PC=>
AsPc-1 NVHBSWZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTJ5MDDuUS=> NYPtTo5vOjN4MUS4PVg>
A549 M13Sc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1O2fWlEPTB;M{K2JI5O NVPQcndtOjN4MUS4PVg>
SNU-1 NVOzO4JDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPUTWM2OD1|NUSgcm0> M2f1blI{PjF2OEm4
HOP62 NUO3dGZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV\UZlhqUUN3ME22O|Yhdk1? Mmj6NlM3OTR6OUi=
H23 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTFyMECgcm0> NH[2SHgzOzZzNEi5PC=>
MB-231 M1j0Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XEUWlEPTB;MUCwNEBvVQ>? MnviNlM3OTR6OUi=
SU.86.86 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTrO21KSzVyPUGwNFEhdk1? Mo\wNlM3OTR6OUi=
CFPAC-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILGUY9KSzVyPUGwNFEhdk1? MVKyN|YyPDh7OB?=
A427 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;tVWlEPTB;MUSzN{BvVQ>? NWH3OWZZOjN4MUS4PVg>
MDAH-2774 NITEUJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nMTmlEPTB;Mk[1O{BvVQ>? MlfyNlM3OTR6OUi=
NCI-H157 NFL4cWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTNyMECgcm0> NFXPWpQzOzZzNEi5PC=>
HTB-177 MoO3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXWbpBKSzVyPUOwNFAhdk1? NH76R|AzOzZzNEi5PC=>
UM-UC-3 M3;2SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTNyMEGgcm0> M3znZVI{PjF2OEm4
HCT-8 M2PiSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTNyMEGgcm0> NXvXdVZpOjN4MUS4PVg>
Panc-1 MoHYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jKN2lEPTB;M{CwNUBvVQ>? NUXMUGhoOjN4MUS4PVg>
DLD-1 NXe0UFU1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NInwdIlKSzVyPUOwNFEhdk1? MYOyN|YyPDh7OB?=
HCT-15 NYqwSXdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTNyMEGgcm0> MXKyN|YyPDh7OB?=
HL-60 MkixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2[0[GlEPTB;M{Cgcm0> MUiyN|YyPDh7OB?=
SK-Mel-2 NGTpdI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\ORlhkUUN3ME2zOEBvVQ>? NWjrdYlCOjN4MUS4PVg>
RD M{T3NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlzITWM2OD1zMkOgcm0> MYeyN|YyPDh7OB?=
HT-1197 NFnhVoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLNN3h{UUN3ME2zNVYhdk1? MmXDNlM3OTR6OUi=
Molt-3 NGflVmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFn2Nm5KSzVyPU[wNEBvVQ>? MlnzNlM3OTR6OUi=
PA-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFSxbopKSzVyPUGwNFEhdk1? MoXGNlM3OTR6OUi=
Molt-4 MoPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTNyMEGgcm0> MUGyN|YyPDh7OB?=
NCI-H292 NV7nV25uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfmTWM2OD17MDDuUS=> MV:yN|YyPDh7OB?=
A2780 M1;mWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LPdWlEPTB;MUSzJI5O NWDQeoM{OjN4MUS4PVg>
IGROV-1 MoO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzvWYRKSzVyPUG0OkBvVQ>? M{O4RVI{PjF2OEm4
SK-N-SH M4\lcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;WZ3g1UUN3ME2xOVAhdk1? NXnBdmJIOjN4MUS4PVg>
N-87 M1:x[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\TdmxKSzVyPUOwO{BvVQ>? MXWyN|YyPDh7OB?=
H322 NVjScVJCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoOyTWM2OD1|MkWgcm0> NH;0UHozOzZzNEi5PC=>
H716 NIPPcm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXmd41pUUN3ME2zN|Qhdk1? MlXJNlM3OTR6OUi=
TT NX7lSoFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3u1U2lEPTB;NEC2JI5O MWSyN|YyPDh7OB?=
Caki-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{H2ZmlEPTB;NEWwJI5O NIDH[XkzOzZzNEi5PC=>
5637 M32wO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjITWM2OD14MUCgcm0> MkK5NlM3OTR6OUi=
MB-453 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnMTZlKSzVyPU[3NkBvVQ>? M1ziVlI{PjF2OEm4
RT-4 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVi5UmRjUUN3ME24NVAhdk1? NH3tZ3gzOzZzNEi5PC=>
HOP92 M3TsV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPoPFhKSzVyPUiyNEBvVQ>? M1L0SlI{PjF2OEm4
KG-1 MkG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfzNYpKSzVyPUmwNEBvVQ>? M2r2fFI{PjF2OEm4
Hs-294T NH;vZ|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13SOGlEPTB;OUS1JI5O M3TnTFI{PjF2OEm4
SF-539 NUnDS|JqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\BTWM2OD1zMECwJI5O MnjJNlM3OTR6OUi=
U-251 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjLVYlCUUN3ME2xNFAxKG6P NE[2RZQzOzZzNEi5PC=>
MB-468 M4PGWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfudJJpUUN3ME2xNFAxKG6P NF3yT5gzOzZzNEi5PC=>
HS746T MkDwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYnmRXJWUUN3ME2xNFAxKG6P NXiwO4ZKOjN4MUS4PVg>
SCABER M3PDV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvCWY5QUUN3ME2xNFAxKG6P NGrCN3czOzZzNEi5PC=>
MCF-7 Mn3sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTFyMEGgcm0> NWH1fohUOjN4MUS4PVg>
CHL-1 Mof3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrxc4VnUUN3ME2xOFYxKG6P NITkfmQzOzZzNEi5PC=>
U87MG M{DjfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTJyMECgcm0> NHixOmMzOzZzNEi5PC=>
SJCRH30 NF6zN3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmm5TWM2OD1{MECyJI5O NUDzSGpiOjN4MUS4PVg>
ES-2 M3nPWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTJ4NUmgcm0> M4jHN|I{PjF2OEm4
HT-1376 M2rrXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTJ6MECgcm0> MWWyN|YyPDh7OB?=
A172 Mn3xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnW3TWM2OD1|MECwJI5O NWPFVWhOOjN4MUS4PVg>
769P NITkNFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTNyMECgcm0> NHzYXG0zOzZzNEi5PC=>
NCI-H520 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TQOWlEPTB;M{CwNEBvVQ>? M1XmOFI{PjF2OEm4
DU145 NYr4U3Q6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTNyMECgcm0> NWftSJV7OjN4MUS4PVg>
K562 M{nLcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHJVIhKSzVyPUOwNFAhdk1? MXmyN|YyPDh7OB?=
U-937 NX:5fGNYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnjTHBKSzVyPUOwNFAhdk1? MlfyNlM3OTR6OUi=
A204 NUTmSJVGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTGPVdKSzVyPUOwNFEhdk1? NHfNdYczOzZzNEi5PC=>
DAOY MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofMTWM2OD1|MECxJI5O M2mzUlI{PjF2OEm4
SF-268 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHG4SIdKSzVyPUOwNFEhdk1? M1POTFI{PjF2OEm4
SF-295 NXrK[2NRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVjHR5FqUUN3ME2zNFAyKG6P M3i0bFI{PjF2OEm4
SNB-19 NU\pcmFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXhTWM2OD1|MECxJI5O MYKyN|YyPDh7OB?=
SNB-75 M1G2Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTNyMEGgcm0> MWmyN|YyPDh7OB?=
U373-MG NGLuSndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnoRYtyUUN3ME2zNFAyKG6P NWHkN2tVOjN4MUS4PVg>
786-O MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2CzVWlEPTB;M{CwNUBvVQ>? Ml\rNlM3OTR6OUi=
A498 NIHQSmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rzeWlEPTB;M{CwNUBvVQ>? MXeyN|YyPDh7OB?=
ACHN NE[1OJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\OelBKSzVyPUOwNFEhdk1? M3TrdVI{PjF2OEm4
EKVX MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjpN4oxUUN3ME2zNFAyKG6P MYWyN|YyPDh7OB?=
H226 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjkbm52UUN3ME2zNFAyKG6P M3y5OFI{PjF2OEm4
H522 NH;EXFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmi5TWM2OD1|MECxJI5O NXnCephMOjN4MUS4PVg>
HeLa MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHe1OoxKSzVyPUOwNFEhdk1? NIDKeHEzOzZzNEi5PC=>
SK-OV-3 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTNyMEGgcm0> NVrKTWJQOjN4MUS4PVg>
Ln Cap M2Htemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2PvW2lEPTB;M{CwNUBvVQ>? NF;2RYkzOzZzNEi5PC=>
PC3 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4mweGlEPTB;M{CwNUBvVQ>? M2\aPVI{PjF2OEm4
SNU-16 M2\IOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTNyMEGgcm0> NV;WcItROjN4MUS4PVg>
FTC-133 NIq1WnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTNyMEGgcm0> MkjpNlM3OTR6OUi=
Ro82-W-1 Mn6wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nkO2lEPTB;M{CwNUBvVQ>? MV[yN|YyPDh7OB?=
Daudi Mk\HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYj0N2h1UUN3ME2zNFAyKG6P NEXvR2czOzZzNEi5PC=>
Jijoye MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTNyMEGgcm0> M3X2S|I{PjF2OEm4
Jurkat Ml3SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTNyMEGgcm0> MVuyN|YyPDh7OB?=
J-82 M3zsZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTNyMEGgcm0> NHqxdo0zOzZzNEi5PC=>
TCC-SUP NVvMVItVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHG3TI9KSzVyPUOwNFEhdk1? MXeyN|YyPDh7OB?=
BT-474 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTNyMEGgcm0> MVGyN|YyPDh7OB?=
ZR-75-1 Mnm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3mTYRKSzVyPUOwNFEhdk1? NETBV3czOzZzNEi5PC=>

... 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]

- Collapse

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]

- Collapse
  • 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]

- Collapse
  • Animal Models: Nude mice
  • 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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
CalculateReset

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.

  • * Indicates a Required Field

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

Tags: buy SCH772984|SCH772984 ic50|SCH772984 price|SCH772984 cost|SCH772984 solubility dmso|SCH772984 purchase|SCH772984 manufacturer|SCH772984 research buy|SCH772984 order|SCH772984 mouse|SCH772984 chemical structure|SCH772984 mw|SCH772984 molecular weight|SCH772984 datasheet|SCH772984 supplier|SCH772984 in vitro|SCH772984 cell line|SCH772984 concentration|SCH772984 nmr|SCH772984 in vivo|SCH772984 clinical trial|SCH772984 inhibitor|SCH772984 MAPK inhibitor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID