SCH772984

For research use only.

Catalog No.S7101

295 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.

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Selleck's SCH772984 has been cited by 295 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 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYi0bVN2UUN3ME2wMlI1KG6P MUCyOVM2ODl|MR?=
WM-266-4 MkfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\MeoJKSzVyPUKwJI5O MkfpNlM3OTR6OUi=
UACC-62 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFW1dZhKSzVyPUOwJI5O NHjGN44zOzZzNEi5PC=>
Colo-205 NWfVc|FKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTN4IH7N MX[yN|YyPDh7OB?=
SK-Mel-1 NVnBUJhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4XpSGlEPTB;M{egcm0> NHH3e2QzOzZzNEi5PC=>
WiDr NYjGbHZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTN7IH7N NF3oS4wzOzZzNEi5PC=>
M14 M4XaNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\hTWM2OD12NzDuUS=> NUfCcXZIOjN4MUS4PVg>
HT-29 NVXTPFZPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{j0OmlEPTB;NUCgcm0> NWjjU45WOjN4MUS4PVg>
8505C MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnrTZNKSzVyPUWwJI5O NF3EN4ozOzZzNEi5PC=>
HT-144 NWTBVGJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PTOWlEPTB;NkCgcm0> M2jYTlI{PjF2OEm4
SK-Mel-5 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonwTWM2OD14NjDuUS=> M4\CflI{PjF2OEm4
A375-SM NH;pZopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPsN4NqUUN3ME23OUBvVQ>? MVeyN|YyPDh7OB?=
SK-Mel-28 NFLuS|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTh3IH7N MnmzNlM3OTR6OUi=
LOX NIO4VIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzOTWM2OD1zMECgcm0> NWm1c|R5OjN4MUS4PVg>
SK-Mel-3 M{XvVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTFzODDuUS=> MX6yN|YyPDh7OB?=
K1 M3vNdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\xemsxUUN3ME2xN|Ahdk1? NXX4eFFSOjN4MUS4PVg>
Hs-695T MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVjiU5lKUUN3ME2xOlUhdk1? M{X3SlI{PjF2OEm4
BHT-101 MornS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWP3ZppHUUN3ME2zNFAhdk1? Mn\PNlM3OTR6OUi=
RPMI-7951 M3y4dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nOdmlEPTB;M{S0JI5O MoX3NlM3OTR6OUi=
A2058 NYXZNpNpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LOdGlEPTB;M{[wJI5O MlvyNlM3OTR6OUi=
SK-Hep-1 M3G3dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYPJR|UxRTF2MkKgcm0> Ml7zNlM3OTR6OUi=
A673 M2DX[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnHNTWM2OD1|MECxJI5O MoLRNlM3OTR6OUi=
DBTRG-05MG Ml\MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHTRYZKSzVyPUOwNFEhdk1? NHzHSpQzOzZzNEi5PC=>
SW-626 NUHSNWxJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Da[mlEPTB;M{Ogcm0> MmnaNlM3OTR6OUi=
LoVo NYqxfpVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTR5IH7N MoHMNlM3OTR6OUi=
MiaPaCa NVLLXWZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXpTWM2OD13MzDuUS=> MXqyN|YyPDh7OB?=
SW-620 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPyNmJKSzVyPUGwOEBvVQ>? MV[yN|YyPDh7OB?=
CAPAN-1 M1jWdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojwTWM2OD1zMESgcm0> NXfVUGw5OjN4MUS4PVg>
SW-527 MkDhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jlWWlEPTB;MUKxJI5O M3TiRlI{PjF2OEm4
HCT-116 NG\rXo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1;kZWlEPTB;MUK4JI5O NGPYfG8zOzZzNEi5PC=>
SW-480 NYXO[HJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2K1XWlEPTB;MU[1JI5O NIjQNHIzOzZzNEi5PC=>
HPAC Ml\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnldXRKSzVyPUG3NEBvVQ>? MmPaNlM3OTR6OUi=
OVCAR-5 NV\SXpdvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLjTWM2OD1{MEigcm0> MWSyN|YyPDh7OB?=
AsPc-1 M3;mdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlO2TWM2OD1{N{Cgcm0> NVvOcVN5OjN4MUS4PVg>
A549 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTN{NjDuUS=> NGXse|EzOzZzNEi5PC=>
SNU-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjE[mpKSzVyPUO1OEBvVQ>? MX2yN|YyPDh7OB?=
HOP62 NH72Z4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4HYWGlEPTB;Nke2JI5O MnrmNlM3OTR6OUi=
H23 NWrrO3ZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTFyMECgcm0> NHX5SFAzOzZzNEi5PC=>
MB-231 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTFyMECgcm0> NIj1O4IzOzZzNEi5PC=>
SU.86.86 M1:4T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzpWnlKSzVyPUGwNFEhdk1? MnzZNlM3OTR6OUi=
CFPAC-1 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{OwdmlEPTB;MUCwNUBvVQ>? MXKyN|YyPDh7OB?=
A427 NXXlOVNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHtfodKSzVyPUG0N|Mhdk1? MkP3NlM3OTR6OUi=
MDAH-2774 NGXP[2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTJ4NUegcm0> NFzyV|kzOzZzNEi5PC=>
NCI-H157 NXS2fnJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmq0TWM2OD1|MECwJI5O M4r1XVI{PjF2OEm4
HTB-177 NI\qflJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTNyMECgcm0> M1[yclI{PjF2OEm4
UM-UC-3 M4XHbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGGyeGVKSzVyPUOwNFEhdk1? MUeyN|YyPDh7OB?=
HCT-8 NI\vNWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUX5TXlpUUN3ME2zNFAyKG6P M1:wV|I{PjF2OEm4
Panc-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlTlTWM2OD1|MECxJI5O NXL2SZdsOjN4MUS4PVg>
DLD-1 M2iwfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGC2R25KSzVyPUOwNFEhdk1? NH21fXAzOzZzNEi5PC=>
HCT-15 NXW4TFRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DTOGlEPTB;M{CwNUBvVQ>? NGSweZMzOzZzNEi5PC=>
HL-60 NWS5TZgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHW5cHZKSzVyPUOwJI5O MlX5NlM3OTR6OUi=
SK-Mel-2 MmH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfHSJpKSzVyPUO0JI5O MnrCNlM3OTR6OUi=
RD M{TvWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlriTWM2OD1zMkOgcm0> NYnMNpp{OjN4MUS4PVg>
HT-1197 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUS4bms1UUN3ME2zNVYhdk1? M{PCNFI{PjF2OEm4
Molt-3 NE\1NHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTZyMDDuUS=> MXmyN|YyPDh7OB?=
PA-1 NUPSfINkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWLNZ2txUUN3ME2xNFAyKG6P NHHwUXQzOzZzNEi5PC=>
Molt-4 M1m3PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTNyMEGgcm0> MYSyN|YyPDh7OB?=
NCI-H292 MoTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF34bZhKSzVyPUmwJI5O NUCwTIVqOjN4MUS4PVg>
A2780 MlTOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{Hqb2lEPTB;MUSzJI5O M1XhTVI{PjF2OEm4
IGROV-1 NHL2eWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4jOd2lEPTB;MUS2JI5O MXqyN|YyPDh7OB?=
SK-N-SH M3fMfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37NZmlEPTB;MUWwJI5O NVLITHBQOjN4MUS4PVg>
N-87 NGLGO3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rsXGlEPTB;M{C3JI5O MWiyN|YyPDh7OB?=
H322 M1fj[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NImzXpJKSzVyPUOyOUBvVQ>? MnHSNlM3OTR6OUi=
H716 NYS2VVA5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnIXnVKSzVyPUOzOEBvVQ>? MXqyN|YyPDh7OB?=
TT MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVG2W3UzUUN3ME20NFYhdk1? NHXPZ|UzOzZzNEi5PC=>
Caki-1 MmnqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX25WIRzUUN3ME20OVAhdk1? NUjs[29XOjN4MUS4PVg>
5637 MnL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmmyTWM2OD14MUCgcm0> NUe5O5lJOjN4MUS4PVg>
MB-453 MnfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\mfYZKSzVyPU[3NkBvVQ>? NIHaR40zOzZzNEi5PC=>
RT-4 MoLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXTbWJqUUN3ME24NVAhdk1? MmmwNlM3OTR6OUi=
HOP92 M2XWcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXK1XINCUUN3ME24NlAhdk1? M1nheVI{PjF2OEm4
KG-1 NV;wWmt6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\CbWlEPTB;OUCwJI5O MVSyN|YyPDh7OB?=
Hs-294T NYH6TFlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\0TWM2OD17NEWgcm0> NGq3T2QzOzZzNEi5PC=>
SF-539 MnW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTFyMECgcm0> M{nURlI{PjF2OEm4
U-251 M2rQXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIq4S4VKSzVyPUGwNFAhdk1? NHXUdIIzOzZzNEi5PC=>
MB-468 M3LvPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTFyMECgcm0> MVGyN|YyPDh7OB?=
HS746T MlLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTFyMECgcm0> NWPabXB6OjN4MUS4PVg>
SCABER MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDTblJmUUN3ME2xNFAxKG6P NXXhelZOOjN4MUS4PVg>
MCF-7 M4LBcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MljyTWM2OD1zMECxJI5O MUeyN|YyPDh7OB?=
CHL-1 M3zlcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rKOWlEPTB;MUS2NEBvVQ>? MnviNlM3OTR6OUi=
U87MG NF\Jc29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHacIlOUUN3ME2yNFAxKG6P MWCyN|YyPDh7OB?=
SJCRH30 M1S3Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mly4TWM2OD1{MECyJI5O MYiyN|YyPDh7OB?=
ES-2 NInydZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvadGxKSzVyPUK2OVkhdk1? MlXyNlM3OTR6OUi=
HT-1376 NHy2UGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M16zVWlEPTB;MkiwNEBvVQ>? MnztNlM3OTR6OUi=
A172 NV;hbpRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rz[WlEPTB;M{CwNEBvVQ>? MmHpNlM3OTR6OUi=
769P MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1jr[GlEPTB;M{CwNEBvVQ>? MUOyN|YyPDh7OB?=
NCI-H520 M{\pN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzQfndKSzVyPUOwNFAhdk1? M3q3dlI{PjF2OEm4
DU145 M{DpcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4iyOWlEPTB;M{CwNEBvVQ>? NYXMNlFlOjN4MUS4PVg>
K562 NXW0UHFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIK4NZdKSzVyPUOwNFAhdk1? NFe5PHEzOzZzNEi5PC=>
U-937 NGjCdXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTNyMECgcm0> M1e3SVI{PjF2OEm4
A204 NYHzZ|NvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHmWFFKSzVyPUOwNFEhdk1? NYLzbI1VOjN4MUS4PVg>
DAOY M2fuemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LJPWlEPTB;M{CwNUBvVQ>? NVyxR3pLOjN4MUS4PVg>
SF-268 NHX4TJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XTeWlEPTB;M{CwNUBvVQ>? MX[yN|YyPDh7OB?=
SF-295 NF\sRodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTNyMEGgcm0> MVWyN|YyPDh7OB?=
SNB-19 NIH3UWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTNyMEGgcm0> NFPtSGQzOzZzNEi5PC=>
SNB-75 MnS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrnTWM2OD1|MECxJI5O NVu4b|ZDOjN4MUS4PVg>
U373-MG MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVLJR|UxRTNyMEGgcm0> MnzrNlM3OTR6OUi=
786-O Ml;rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFq2XZNKSzVyPUOwNFEhdk1? MXeyN|YyPDh7OB?=
A498 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFH4O5dKSzVyPUOwNFEhdk1? M2XUVlI{PjF2OEm4
ACHN M4Lj[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVP4NJRUUUN3ME2zNFAyKG6P NFfDO4ozOzZzNEi5PC=>
EKVX NIjjUGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DsfWlEPTB;M{CwNUBvVQ>? MVqyN|YyPDh7OB?=
H226 M{WwR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MknXTWM2OD1|MECxJI5O NUDO[YFJOjN4MUS4PVg>
H522 MnrOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjD[pAyUUN3ME2zNFAyKG6P NVPUT|lKOjN4MUS4PVg>
HeLa M2PuZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2q0OWlEPTB;M{CwNUBvVQ>? MmOyNlM3OTR6OUi=
SK-OV-3 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfWTWM2OD1|MECxJI5O M1vzWlI{PjF2OEm4
Ln Cap NWnOcGhwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILoXnJKSzVyPUOwNFEhdk1? MWmyN|YyPDh7OB?=
PC3 NHfDNmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTNyMEGgcm0> NH;sfFUzOzZzNEi5PC=>
SNU-16 NE\GWZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXv1UGVJUUN3ME2zNFAyKG6P Mn\4NlM3OTR6OUi=
FTC-133 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LwUmlEPTB;M{CwNUBvVQ>? NFK2ZZUzOzZzNEi5PC=>
Ro82-W-1 Mnm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm[xTWM2OD1|MECxJI5O Mm[3NlM3OTR6OUi=
Daudi M4HrXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIG3b4RKSzVyPUOwNFEhdk1? MXSyN|YyPDh7OB?=
Jijoye NG\GTYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYCzUFIyUUN3ME2zNFAyKG6P MnjQNlM3OTR6OUi=
Jurkat NWfrfVhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{[4e2lEPTB;M{CwNUBvVQ>? NEDWUmYzOzZzNEi5PC=>
J-82 NH\JZlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTNyMEGgcm0> MoS4NlM3OTR6OUi=
TCC-SUP NYDN[It6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTNyMEGgcm0> NY\5PGFVOjN4MUS4PVg>
BT-474 NE\EeJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHftUpJKSzVyPUOwNFEhdk1? NGnTcpYzOzZzNEi5PC=>
ZR-75-1 M3fNcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTNyMEGgcm0> M2DnSFI{PjF2OEm4

... 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