SCH772984

For research use only.

Catalog No.S7101

307 publications

SCH772984 Chemical Structure

CAS No. 942183-80-4

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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Selleck's SCH772984 has been cited by 307 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 NG\iXoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fwT2lEPTB;MD6yOEBvVQ>? NGGzN40zPTN3MEmzNS=>
WM-266-4 NYjKSYF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITiWpBKSzVyPUKwJI5O MXuyN|YyPDh7OB?=
UACC-62 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjXdm92UUN3ME2zNEBvVQ>? M2TNO|I{PjF2OEm4
Colo-205 M1LzVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDWVIhvUUN3ME2zOkBvVQ>? MV6yN|YyPDh7OB?=
SK-Mel-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml34TWM2OD1|NzDuUS=> NFXzNoEzOzZzNEi5PC=>
WiDr MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfLN3BKSzVyPUO5JI5O M3jrTFI{PjF2OEm4
M14 M3jEfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml[zTWM2OD12NzDuUS=> MoP2NlM3OTR6OUi=
HT-29 MkTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPLbmt[UUN3ME21NEBvVQ>? MYWyN|YyPDh7OB?=
8505C MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTVyIH7N NWXmS|BPOjN4MUS4PVg>
HT-144 NG[zVItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPUTWM2OD14MDDuUS=> M176SVI{PjF2OEm4
SK-Mel-5 NYXGU4xGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUDyTo9yUUN3ME22OkBvVQ>? NXzNZWxlOjN4MUS4PVg>
A375-SM MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo[3TWM2OD15NTDuUS=> NI\UTIgzOzZzNEi5PC=>
SK-Mel-28 NFf4dIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3iy[2lEPTB;OEWgcm0> NFzFSFgzOzZzNEi5PC=>
LOX MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrzVmNKSzVyPUGwNEBvVQ>? MnKxNlM3OTR6OUi=
SK-Mel-3 NVzxTXZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3PW4pbUUN3ME2xNVghdk1? NVHIZlZPOjN4MUS4PVg>
K1 Mn3TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTF|MDDuUS=> M3O0SVI{PjF2OEm4
Hs-695T M1v6SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3v1WGlEPTB;MU[1JI5O NXPoOGxsOjN4MUS4PVg>
BHT-101 M3\FOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTNyMDDuUS=> MUWyN|YyPDh7OB?=
RPMI-7951 NHTmXZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTN2NDDuUS=> NWm5UnBnOjN4MUS4PVg>
A2058 M320cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTN4MDDuUS=> MkjkNlM3OTR6OUi=
SK-Hep-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfScFBKSzVyPUG0NlIhdk1? MnLwNlM3OTR6OUi=
A673 NGrCS2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4LoT2lEPTB;M{CwNUBvVQ>? MYOyN|YyPDh7OB?=
DBTRG-05MG MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17mfWlEPTB;M{CwNUBvVQ>? M{[0TVI{PjF2OEm4
SW-626 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTN|IH7N M1;TRVI{PjF2OEm4
LoVo MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;6cZhzUUN3ME20O{BvVQ>? MXOyN|YyPDh7OB?=
MiaPaCa NXLXUmp1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEK5[2hKSzVyPUWzJI5O NX;nZVVYOjN4MUS4PVg>
SW-620 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGCxeoNKSzVyPUGwOEBvVQ>? MoS2NlM3OTR6OUi=
CAPAN-1 NH7oUHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTyTWM2OD1zMESgcm0> NUSzcWV2OjN4MUS4PVg>
SW-527 NX\ZUJlZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\kPJNKSzVyPUGyNUBvVQ>? MVKyN|YyPDh7OB?=
HCT-116 M2DXfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;HTWM2OD1zMkigcm0> MU[yN|YyPDh7OB?=
SW-480 Mnf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NViwZWVtUUN3ME2xOlUhdk1? NHHX[G4zOzZzNEi5PC=>
HPAC NWq4[XdET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XrbWlEPTB;MUewJI5O NVzTRopIOjN4MUS4PVg>
OVCAR-5 MnvGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzIeoxtUUN3ME2yNFghdk1? NXnXeG9bOjN4MUS4PVg>
AsPc-1 NEX2UYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrIVpVKSzVyPUK3NEBvVQ>? NIfXN3MzOzZzNEi5PC=>
A549 MorQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEO3WYlKSzVyPUOyOkBvVQ>? NHn3cFIzOzZzNEi5PC=>
SNU-1 NYHQbW9DT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;peWlEPTB;M{W0JI5O MXKyN|YyPDh7OB?=
HOP62 NUO5UpZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPvRY1KSzVyPU[3OkBvVQ>? NG\IOnQzOzZzNEi5PC=>
H23 NXTGR4RCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTFyMECgcm0> MoH2NlM3OTR6OUi=
MB-231 M4jzbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPhTWM2OD1zMECwJI5O NHfBdmkzOzZzNEi5PC=>
SU.86.86 MoTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPITWM2OD1zMECxJI5O M1\QflI{PjF2OEm4
CFPAC-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXOwdJVHUUN3ME2xNFAyKG6P NEK4Nm8zOzZzNEi5PC=>
A427 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTF2M{Ogcm0> MljCNlM3OTR6OUi=
MDAH-2774 MnLTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mme2TWM2OD1{NkW3JI5O M2PWdVI{PjF2OEm4
NCI-H157 NYXrdHNIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnETWM2OD1|MECwJI5O MlvRNlM3OTR6OUi=
HTB-177 NELmNpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjUTnZKSzVyPUOwNFAhdk1? NETDe|MzOzZzNEi5PC=>
UM-UC-3 NGOwcWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrweWluUUN3ME2zNFAyKG6P NV3XSI4xOjN4MUS4PVg>
HCT-8 NXrIcZBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mki4TWM2OD1|MECxJI5O NGrwe4kzOzZzNEi5PC=>
Panc-1 MlX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWj0S5J{UUN3ME2zNFAyKG6P MXGyN|YyPDh7OB?=
DLD-1 NGPTNo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHBTWM2OD1|MECxJI5O NVvp[2NiOjN4MUS4PVg>
HCT-15 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1izfGlEPTB;M{CwNUBvVQ>? MUmyN|YyPDh7OB?=
HL-60 NF7hbJFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnCXVRYUUN3ME2zNEBvVQ>? NFjmeWkzOzZzNEi5PC=>
SK-Mel-2 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\lTWlEPTB;M{Sgcm0> NEHwR5IzOzZzNEi5PC=>
RD Mlf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\ZO|d6UUN3ME2xNlMhdk1? M4r0WFI{PjF2OEm4
HT-1197 MkCyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHn5WoVKSzVyPUOxOkBvVQ>? Mmi3NlM3OTR6OUi=
Molt-3 NX;uOFhIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDobXdKSzVyPU[wNEBvVQ>? MYeyN|YyPDh7OB?=
PA-1 NYPVOpN5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Moe5TWM2OD1zMECxJI5O MmPkNlM3OTR6OUi=
Molt-4 M3i5ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPSd3VRUUN3ME2zNFAyKG6P NID3ToozOzZzNEi5PC=>
NCI-H292 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonrTWM2OD17MDDuUS=> MWCyN|YyPDh7OB?=
A2780 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nNe2lEPTB;MUSzJI5O NGjyVpUzOzZzNEi5PC=>
IGROV-1 NUew[2hjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvDWnJNUUN3ME2xOFYhdk1? NGrHbXYzOzZzNEi5PC=>
SK-N-SH NXjSRo1XT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjDXVlLUUN3ME2xOVAhdk1? NFTT[XozOzZzNEi5PC=>
N-87 MmTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHXWZZKSzVyPUOwO{BvVQ>? MlnBNlM3OTR6OUi=
H322 NX7te3RkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLubnlKSzVyPUOyOUBvVQ>? MWWyN|YyPDh7OB?=
H716 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTN|NDDuUS=> NYPLb3dXOjN4MUS4PVg>
TT NWPyUXROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTRyNjDuUS=> NH3mPWczOzZzNEi5PC=>
Caki-1 M3HSO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXSwSIJXUUN3ME20OVAhdk1? MkTSNlM3OTR6OUi=
5637 NFXG[VJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPzTWM2OD14MUCgcm0> M33CeFI{PjF2OEm4
MB-453 M2fpfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3tVZhKSzVyPU[3NkBvVQ>? MWiyN|YyPDh7OB?=
RT-4 NVvlVHVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF7RVXJKSzVyPUixNEBvVQ>? NH7HW4QzOzZzNEi5PC=>
HOP92 MmXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7EOFlOUUN3ME24NlAhdk1? M3ju[VI{PjF2OEm4
KG-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjDUI9KSzVyPUmwNEBvVQ>? NVq5Z4llOjN4MUS4PVg>
Hs-294T NH;Efo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTrTWM2OD17NEWgcm0> MVOyN|YyPDh7OB?=
SF-539 NVXkO5JPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTITWM2OD1zMECwJI5O NEfRXlIzOzZzNEi5PC=>
U-251 M4XiUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HCZ2lEPTB;MUCwNEBvVQ>? NHnlTZMzOzZzNEi5PC=>
MB-468 NIXScoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnNSXZ1UUN3ME2xNFAxKG6P MX6yN|YyPDh7OB?=
HS746T M4nOVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDrToFKSzVyPUGwNFAhdk1? MYCyN|YyPDh7OB?=
SCABER MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XwfmlEPTB;MUCwNEBvVQ>? NYrMS4lUOjN4MUS4PVg>
MCF-7 M4XoUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmG2TWM2OD1zMECxJI5O NG[zdVYzOzZzNEi5PC=>
CHL-1 NHHUTZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHCTWM2OD1zNE[wJI5O NEHIfHgzOzZzNEi5PC=>
U87MG NHqzbGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTJyMECgcm0> MYGyN|YyPDh7OB?=
SJCRH30 MkLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTJyMEKgcm0> NV;mdWdTOjN4MUS4PVg>
ES-2 MkTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFW4RYlKSzVyPUK2OVkhdk1? M4[2Z|I{PjF2OEm4
HT-1376 M3TIRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTLcFJnUUN3ME2yPFAxKG6P MX:yN|YyPDh7OB?=
A172 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLqTWM2OD1|MECwJI5O MWiyN|YyPDh7OB?=
769P MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTNyMECgcm0> MY[yN|YyPDh7OB?=
NCI-H520 M3jmUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fOPWlEPTB;M{CwNEBvVQ>? M4T5ZVI{PjF2OEm4
DU145 NEezVpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLHTWM2OD1|MECwJI5O NFnrUYYzOzZzNEi5PC=>
K562 NE\sfoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXT4T|E{UUN3ME2zNFAxKG6P NGHIRVgzOzZzNEi5PC=>
U-937 MoXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHT3OY5KSzVyPUOwNFAhdk1? M2LnOFI{PjF2OEm4
A204 M3jR[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTob5hKSzVyPUOwNFEhdk1? MoXTNlM3OTR6OUi=
DAOY NVnVZplwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPpOm5KSzVyPUOwNFEhdk1? NWTMOHYxOjN4MUS4PVg>
SF-268 MnX3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XHZWlEPTB;M{CwNUBvVQ>? M3faZ|I{PjF2OEm4
SF-295 NYLJdlRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XENWlEPTB;M{CwNUBvVQ>? NI\Ie4szOzZzNEi5PC=>
SNB-19 Mn7MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\VTWM2OD1|MECxJI5O M1TIfFI{PjF2OEm4
SNB-75 MlXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTNyMEGgcm0> MV[yN|YyPDh7OB?=
U373-MG NVfWc|FPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYWyOGhJUUN3ME2zNFAyKG6P MUOyN|YyPDh7OB?=
786-O MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnuTWM2OD1|MECxJI5O NV\vR2V5OjN4MUS4PVg>
A498 MlGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4PhfWlEPTB;M{CwNUBvVQ>? NEfXO4UzOzZzNEi5PC=>
ACHN NIX2eWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTNyMEGgcm0> MYeyN|YyPDh7OB?=
EKVX NVvje2twT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TB[mlEPTB;M{CwNUBvVQ>? M4HIUFI{PjF2OEm4
H226 NWLORmVWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2j1SmlEPTB;M{CwNUBvVQ>? M37LOVI{PjF2OEm4
H522 NEnzRnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmT4TWM2OD1|MECxJI5O NYG3UGlZOjN4MUS4PVg>
HeLa NEnDSFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTNyMEGgcm0> MoH6NlM3OTR6OUi=
SK-OV-3 MlfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDYc4xiUUN3ME2zNFAyKG6P M{XPb|I{PjF2OEm4
Ln Cap M{PaTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfsfIdoUUN3ME2zNFAyKG6P NHe2T4QzOzZzNEi5PC=>
PC3 NFXxW3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnq3TWM2OD1|MECxJI5O NYjEfWZ5OjN4MUS4PVg>
SNU-16 NEHkWYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fPd2lEPTB;M{CwNUBvVQ>? MoP2NlM3OTR6OUi=
FTC-133 NF36SVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTNyMEGgcm0> M4HFVVI{PjF2OEm4
Ro82-W-1 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTOTWM2OD1|MECxJI5O MmOxNlM3OTR6OUi=
Daudi Mn\vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTNyMEGgcm0> M3v3WFI{PjF2OEm4
Jijoye MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDKdG1KSzVyPUOwNFEhdk1? M2nqPFI{PjF2OEm4
Jurkat NXzwPFNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3q5OGlEPTB;M{CwNUBvVQ>? M{nwSlI{PjF2OEm4
J-82 MlS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1u2bmlEPTB;M{CwNUBvVQ>? Mn;sNlM3OTR6OUi=
TCC-SUP MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1q5cGlEPTB;M{CwNUBvVQ>? NYfyV2MzOjN4MUS4PVg>
BT-474 NEHSSnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTNyMEGgcm0> MXOyN|YyPDh7OB?=
ZR-75-1 M2HaRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDBTWM2OD1|MECxJI5O MnP1NlM3OTR6OUi=

... 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
  • 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
Smiles C1CN(CC1C(=O)NC2=CC3=C(C=C2)NN=C3C4=CC=NC=C4)CC(=O)N5CCN(CC5)C6=CC=C(C=C6)C7=NC=CC=N7

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 ()
% 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.

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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