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 80 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 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTNSJVCUUN3ME2wMlI1KG6P M3n4[lI2OzVyOUOx
WM-266-4 NVT1PYFmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnQfZB7UUN3ME2yNEBvVQ>? NH\hfVgzOzZzNEi5PC=>
UACC-62 NETWUZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\EV2lEPTB;M{Cgcm0> NWTFeHVkOjN4MUS4PVg>
Colo-205 NVHIXopkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTTTWM2OD1|NjDuUS=> MXOyN|YyPDh7OB?=
SK-Mel-1 NFLBVXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1y5[GlEPTB;M{egcm0> MVOyN|YyPDh7OB?=
WiDr M4T1Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrjOFZxUUN3ME2zPUBvVQ>? NWC5UmVQOjN4MUS4PVg>
M14 NYjNOIVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHkToVqUUN3ME20O{BvVQ>? NELm[JozOzZzNEi5PC=>
HT-29 NX7MRnZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3;qR2lEPTB;NUCgcm0> MlzjNlM3OTR6OUi=
8505C NIHEeodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjnOIxQUUN3ME21NEBvVQ>? M3PYc|I{PjF2OEm4
HT-144 M17NZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlryTWM2OD14MDDuUS=> MYCyN|YyPDh7OB?=
SK-Mel-5 M13QRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTZ4IH7N MX6yN|YyPDh7OB?=
A375-SM MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\C[2dKSzVyPUe1JI5O NFTSWngzOzZzNEi5PC=>
SK-Mel-28 M{jxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTh3IH7N M2Xx[VI{PjF2OEm4
LOX NW\ld3l[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWG1eYM3UUN3ME2xNFAhdk1? MlG0NlM3OTR6OUi=
SK-Mel-3 NIDhbWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTFzODDuUS=> NGDBNG4zOzZzNEi5PC=>
K1 Mnq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;QWWlEPTB;MUOwJI5O Mo\kNlM3OTR6OUi=
Hs-695T NXzFZo9tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MU\JR|UxRTF4NTDuUS=> MX2yN|YyPDh7OB?=
BHT-101 M1nFUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlS5TWM2OD1|MECgcm0> MkTxNlM3OTR6OUi=
RPMI-7951 NWHkfIo{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmrFTWM2OD1|NESgcm0> NUW5V2Q3OjN4MUS4PVg>
A2058 NYTwRm5{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTN4MDDuUS=> NV\2Upc1OjN4MUS4PVg>
SK-Hep-1 NVLYdpZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3kTWM2OD1zNEKyJI5O MUSyN|YyPDh7OB?=
A673 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;ZV2lEPTB;M{CwNUBvVQ>? MlTUNlM3OTR6OUi=
DBTRG-05MG M3\OU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;MeWlEPTB;M{CwNUBvVQ>? Mn22NlM3OTR6OUi=
SW-626 M4r1U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[1VmttUUN3ME2zN{BvVQ>? MmXxNlM3OTR6OUi=
LoVo NVrafYhkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorwTWM2OD12NzDuUS=> NIO1SIQzOzZzNEi5PC=>
MiaPaCa M3TlWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHfrcnhKSzVyPUWzJI5O NEfSTVQzOzZzNEi5PC=>
SW-620 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLDTWM2OD1zMESgcm0> NWDxZVBqOjN4MUS4PVg>
CAPAN-1 NX3kTHlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLzZ5NqUUN3ME2xNFQhdk1? NYHqdpFoOjN4MUS4PVg>
SW-527 NWXPToJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHoT3lyUUN3ME2xNlEhdk1? MlP2NlM3OTR6OUi=
HCT-116 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TzcGlEPTB;MUK4JI5O NX\TNWZnOjN4MUS4PVg>
SW-480 M2TPZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF23RXhKSzVyPUG2OUBvVQ>? NIjwWXMzOzZzNEi5PC=>
HPAC MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTF5MDDuUS=> MoXSNlM3OTR6OUi=
OVCAR-5 M2PiN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTL[4NpUUN3ME2yNFghdk1? MoHkNlM3OTR6OUi=
AsPc-1 M{nyUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXFZ|BKSzVyPUK3NEBvVQ>? M4P0fVI{PjF2OEm4
A549 MmfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\SVJN1UUN3ME2zNlYhdk1? MYeyN|YyPDh7OB?=
SNU-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvkfmZKSzVyPUO1OEBvVQ>? MlK5NlM3OTR6OUi=
HOP62 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2L4ZWlEPTB;Nke2JI5O NUnoNnh6OjN4MUS4PVg>
H23 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTpTWM2OD1zMECwJI5O MmnYNlM3OTR6OUi=
MB-231 M{jte2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\LTnR3UUN3ME2xNFAxKG6P NHvWWnMzOzZzNEi5PC=>
SU.86.86 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTFyMEGgcm0> NGrnXJgzOzZzNEi5PC=>
CFPAC-1 NFftfYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTFyMEGgcm0> MlLhNlM3OTR6OUi=
A427 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33GbWlEPTB;MUSzN{BvVQ>? MUKyN|YyPDh7OB?=
MDAH-2774 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUGzN2RCUUN3ME2yOlU4KG6P MUiyN|YyPDh7OB?=
NCI-H157 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFW3bmFKSzVyPUOwNFAhdk1? MkCzNlM3OTR6OUi=
HTB-177 M{iyZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVPJR|UxRTNyMECgcm0> Mnm3NlM3OTR6OUi=
UM-UC-3 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrUcohZUUN3ME2zNFAyKG6P NUHOTYlrOjN4MUS4PVg>
HCT-8 NF\F[FJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\iSmlEPTB;M{CwNUBvVQ>? MVeyN|YyPDh7OB?=
Panc-1 M3ftfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTNyMEGgcm0> M1fIRlI{PjF2OEm4
DLD-1 M4i0OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7ZcJpSUUN3ME2zNFAyKG6P MkfXNlM3OTR6OUi=
HCT-15 NXP0PIpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlfQTWM2OD1|MECxJI5O MUSyN|YyPDh7OB?=
HL-60 M2TDTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDXWI1nUUN3ME2zNEBvVQ>? NYKwbYxIOjN4MUS4PVg>
SK-Mel-2 NVrXcHo2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTN2IH7N NYjCOnkzOjN4MUS4PVg>
RD NGLGWGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2X6fGlEPTB;MUKzJI5O NFrUTnUzOzZzNEi5PC=>
HT-1197 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTNzNjDuUS=> NEnlUHgzOzZzNEi5PC=>
Molt-3 NIq5WWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnZO5pTUUN3ME22NFAhdk1? MkmxNlM3OTR6OUi=
PA-1 M1TTc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jTcmlEPTB;MUCwNUBvVQ>? MV6yN|YyPDh7OB?=
Molt-4 M33JTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rpd2lEPTB;M{CwNUBvVQ>? M2G4SVI{PjF2OEm4
NCI-H292 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmDUTWM2OD17MDDuUS=> MXmyN|YyPDh7OB?=
A2780 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jQb2lEPTB;MUSzJI5O MUSyN|YyPDh7OB?=
IGROV-1 M4LFPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV73e4VvUUN3ME2xOFYhdk1? NXHPVVZjOjN4MUS4PVg>
SK-N-SH Ml7sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjaTWM2OD1zNUCgcm0> NXnqV4pCOjN4MUS4PVg>
N-87 M1vvcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLH[3hKSzVyPUOwO{BvVQ>? M2PIRlI{PjF2OEm4
H322 NY\PPFYzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTN{NTDuUS=> NX34VGtVOjN4MUS4PVg>
H716 MlftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3qS5RDUUN3ME2zN|Qhdk1? NYTNRWE4OjN4MUS4PVg>
TT MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7PcJVKSzVyPUSwOkBvVQ>? M1;EOFI{PjF2OEm4
Caki-1 Mkj0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXrmUnZrUUN3ME20OVAhdk1? NUDGZ45ZOjN4MUS4PVg>
5637 M4jWfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jwTWlEPTB;NkGwJI5O M3fZN|I{PjF2OEm4
MB-453 NVXRUJB3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTZ5MjDuUS=> NXTwOXA6OjN4MUS4PVg>
RT-4 NHzFWJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFG4eYJKSzVyPUixNEBvVQ>? NEPnSHgzOzZzNEi5PC=>
HOP92 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3G1UmlEPTB;OEKwJI5O MVGyN|YyPDh7OB?=
KG-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnXcmFkUUN3ME25NFAhdk1? M4WwdVI{PjF2OEm4
Hs-294T MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3PlS2lEPTB;OUS1JI5O MnLZNlM3OTR6OUi=
SF-539 M2jabGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDMfng3UUN3ME2xNFAxKG6P M{\1[VI{PjF2OEm4
U-251 NFLHZpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTFyMECgcm0> MmHHNlM3OTR6OUi=
MB-468 NIHRWmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTFyMECgcm0> MUGyN|YyPDh7OB?=
HS746T NGfHS|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLxTWM2OD1zMECwJI5O M2jDcFI{PjF2OEm4
SCABER NX60RnFKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm[yTWM2OD1zMECwJI5O NWXINoxlOjN4MUS4PVg>
MCF-7 MmPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkC1TWM2OD1zMECxJI5O MkjRNlM3OTR6OUi=
CHL-1 Mmf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTF2NkCgcm0> NVnoWVk3OjN4MUS4PVg>
U87MG NH3lSWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTJyMECgcm0> MVWyN|YyPDh7OB?=
SJCRH30 NIH0[mlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPYNlNKSzVyPUKwNFIhdk1? MWCyN|YyPDh7OB?=
ES-2 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{S4OWlEPTB;Mk[1PUBvVQ>? M37jV|I{PjF2OEm4
HT-1376 M{H5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHwTWM2OD1{OECwJI5O NGLnOXMzOzZzNEi5PC=>
A172 NV6zdXRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHviWZFKSzVyPUOwNFAhdk1? MVSyN|YyPDh7OB?=
769P MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTNyMECgcm0> MXGyN|YyPDh7OB?=
NCI-H520 NInySlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4PWWmlEPTB;M{CwNEBvVQ>? MUOyN|YyPDh7OB?=
DU145 NIezbIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTVO5VKSzVyPUOwNFAhdk1? MYGyN|YyPDh7OB?=
K562 M2LsNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDKTVNtUUN3ME2zNFAxKG6P MlnTNlM3OTR6OUi=
U-937 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTNyMECgcm0> MnHONlM3OTR6OUi=
A204 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3WyU2lEPTB;M{CwNUBvVQ>? NXLWcGRpOjN4MUS4PVg>
DAOY NGT0cphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILhcY5KSzVyPUOwNFEhdk1? MmL0NlM3OTR6OUi=
SF-268 NIm4co5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTNyMEGgcm0> NUTPTndROjN4MUS4PVg>
SF-295 Mly1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHzrS|NKSzVyPUOwNFEhdk1? Mkj1NlM3OTR6OUi=
SNB-19 M1vIWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2D2UmlEPTB;M{CwNUBvVQ>? MWKyN|YyPDh7OB?=
SNB-75 NHvGWGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;1PGlEPTB;M{CwNUBvVQ>? Moe2NlM3OTR6OUi=
U373-MG NYTFOGVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTNyMEGgcm0> MVuyN|YyPDh7OB?=
786-O M3SwU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHSe253UUN3ME2zNFAyKG6P M1L4flI{PjF2OEm4
A498 NGfDeHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTDZYFsUUN3ME2zNFAyKG6P MXqyN|YyPDh7OB?=
ACHN MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEmwUohKSzVyPUOwNFEhdk1? M2OwUlI{PjF2OEm4
EKVX MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHHTWM2OD1|MECxJI5O M4[xcFI{PjF2OEm4
H226 MkCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1naT2lEPTB;M{CwNUBvVQ>? NUPLTVBPOjN4MUS4PVg>
H522 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfZTWM2OD1|MECxJI5O M1zndVI{PjF2OEm4
HeLa NHTSToZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1KxOGlEPTB;M{CwNUBvVQ>? MYWyN|YyPDh7OB?=
SK-OV-3 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HhfGlEPTB;M{CwNUBvVQ>? MonlNlM3OTR6OUi=
Ln Cap MlWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zPSWlEPTB;M{CwNUBvVQ>? NUf3VXdlOjN4MUS4PVg>
PC3 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIj6eopKSzVyPUOwNFEhdk1? MUWyN|YyPDh7OB?=
SNU-16 M2Hy[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1L5T2lEPTB;M{CwNUBvVQ>? MmL2NlM3OTR6OUi=
FTC-133 NYfUWW1YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HNU2lEPTB;M{CwNUBvVQ>? NGm1O5YzOzZzNEi5PC=>
Ro82-W-1 M1HPV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTlXGVKSzVyPUOwNFEhdk1? MVWyN|YyPDh7OB?=
Daudi M4fLOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTNyMEGgcm0> MWeyN|YyPDh7OB?=
Jijoye MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGC1TVJKSzVyPUOwNFEhdk1? MV2yN|YyPDh7OB?=
Jurkat NFK3WJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTNyMEGgcm0> MUCyN|YyPDh7OB?=
J-82 MnPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTNyMEGgcm0> MlrLNlM3OTR6OUi=
TCC-SUP M2jMOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDScXlKUUN3ME2zNFAyKG6P MoH6NlM3OTR6OUi=
BT-474 M3Xw[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrPTWM2OD1|MECxJI5O MXWyN|YyPDh7OB?=
ZR-75-1 NGDFWHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjHZppqUUN3ME2zNFAyKG6P NF;KPI0zOzZzNEi5PC=>

... 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]

+ Expand

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]

+ Expand
  • 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]

+ Expand
  • 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
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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):
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    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