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 74 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 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2WzUmlEPTB;MD6yOEBvVQ>? MmW2NlU{PTB7M{G=
WM-266-4 M1XDSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoW5TWM2OD1{MDDuUS=> NFTFUZQzOzZzNEi5PC=>
UACC-62 MlHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk[4TWM2OD1|MDDuUS=> MoXINlM3OTR6OUi=
Colo-205 Ml[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;pcVFPUUN3ME2zOkBvVQ>? NH\HZ2YzOzZzNEi5PC=>
SK-Mel-1 NXfhWmtGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfwOVhMUUN3ME2zO{BvVQ>? NHr6R|MzOzZzNEi5PC=>
WiDr Mkn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1f0WGlEPTB;M{mgcm0> NWHOfHlqOjN4MUS4PVg>
M14 M2jnU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHu2bmJKSzVyPUS3JI5O MUeyN|YyPDh7OB?=
HT-29 NFvsU|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzsUotzUUN3ME21NEBvVQ>? NGnGeIczOzZzNEi5PC=>
8505C NXviO3RLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFy1V2hKSzVyPUWwJI5O MmHlNlM3OTR6OUi=
HT-144 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTZyIH7N NFXDVpAzOzZzNEi5PC=>
SK-Mel-5 NIWxbFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PiTmlEPTB;Nk[gcm0> NFPVW2UzOzZzNEi5PC=>
A375-SM MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTwSnF4UUN3ME23OUBvVQ>? MnP4NlM3OTR6OUi=
SK-Mel-28 NIDHeXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX35T4hEUUN3ME24OUBvVQ>? NXzySY1VOjN4MUS4PVg>
LOX NVHES5RDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDxTWM2OD1zMECgcm0> NWH1TmhSOjN4MUS4PVg>
SK-Mel-3 NYLKNIw6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHTdoxrUUN3ME2xNVghdk1? NU\s[G53OjN4MUS4PVg>
K1 NEf4NXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrJWnk5UUN3ME2xN|Ahdk1? M4D1Z|I{PjF2OEm4
Hs-695T M1fW[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTF4NTDuUS=> MnrWNlM3OTR6OUi=
BHT-101 NHTuc|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\sdHhKSzVyPUOwNEBvVQ>? M37Fe|I{PjF2OEm4
RPMI-7951 MmG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLWTWM2OD1|NESgcm0> NVOyTJRpOjN4MUS4PVg>
A2058 Mn;JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTN4MDDuUS=> MlX3NlM3OTR6OUi=
SK-Hep-1 NF7YOpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jESGlEPTB;MUSyNkBvVQ>? M1H2U|I{PjF2OEm4
A673 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHISnlKSzVyPUOwNFEhdk1? MkHTNlM3OTR6OUi=
DBTRG-05MG MkTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXBRZBKSzVyPUOwNFEhdk1? NEnJRWgzOzZzNEi5PC=>
SW-626 NE\VVVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTN|IH7N MoDXNlM3OTR6OUi=
LoVo MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTR5IH7N NUTKOYVDOjN4MUS4PVg>
MiaPaCa NUDON4pZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHO3fnNKSzVyPUWzJI5O M3LwUFI{PjF2OEm4
SW-620 NHvSTIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYP5TnVOUUN3ME2xNFQhdk1? M{\wO|I{PjF2OEm4
CAPAN-1 M2DScGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV7rNIJ3UUN3ME2xNFQhdk1? NXPMfo1KOjN4MUS4PVg>
SW-527 MnzOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzVZnM6UUN3ME2xNlEhdk1? MlqwNlM3OTR6OUi=
HCT-116 MmDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTF{ODDuUS=> NUfmToF5OjN4MUS4PVg>
SW-480 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLm[nlKSzVyPUG2OUBvVQ>? M4CzUVI{PjF2OEm4
HPAC M4PVUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLXW3FKSzVyPUG3NEBvVQ>? NWj4SFVEOjN4MUS4PVg>
OVCAR-5 NYfw[m1sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTJyODDuUS=> NXn4PYl5OjN4MUS4PVg>
AsPc-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXrJR|UxRTJ5MDDuUS=> NHewXZIzOzZzNEi5PC=>
A549 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVS5WW5xUUN3ME2zNlYhdk1? NF;nXVAzOzZzNEi5PC=>
SNU-1 Ml7US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHo[XdoUUN3ME2zOVQhdk1? M36zRVI{PjF2OEm4
HOP62 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTZ5NjDuUS=> NUD5fm9jOjN4MUS4PVg>
H23 M1X3SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTFyMECgcm0> NE\F[pEzOzZzNEi5PC=>
MB-231 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoL6TWM2OD1zMECwJI5O MUWyN|YyPDh7OB?=
SU.86.86 M1PPdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\hTWM2OD1zMECxJI5O NX;kcZdlOjN4MUS4PVg>
CFPAC-1 MlnaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XCVGlEPTB;MUCwNUBvVQ>? MkD6NlM3OTR6OUi=
A427 M1fCbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULPNYFTUUN3ME2xOFM{KG6P NGfrVFIzOzZzNEi5PC=>
MDAH-2774 M4jx[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jPUGlEPTB;Mk[1O{BvVQ>? M3LQ[VI{PjF2OEm4
NCI-H157 NVPIU2h{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlziTWM2OD1|MECwJI5O NX3BfWpXOjN4MUS4PVg>
HTB-177 NFrqbGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\QOmRKSzVyPUOwNFAhdk1? M2TtclI{PjF2OEm4
UM-UC-3 NUXWfYMyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fleGlEPTB;M{CwNUBvVQ>? NEnzVI8zOzZzNEi5PC=>
HCT-8 M{e1fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXBSYxKSzVyPUOwNFEhdk1? M2DlTFI{PjF2OEm4
Panc-1 M{DlRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTNyMEGgcm0> MWqyN|YyPDh7OB?=
DLD-1 NHLHS4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3viTGlEPTB;M{CwNUBvVQ>? NWPUd3R2OjN4MUS4PVg>
HCT-15 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPQTWM2OD1|MECxJI5O NUHFS2M3OjN4MUS4PVg>
HL-60 M3HLeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnzZ3ZKSzVyPUOwJI5O Mn\lNlM3OTR6OUi=
SK-Mel-2 NVPw[HN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnOdGx{UUN3ME2zOEBvVQ>? MXWyN|YyPDh7OB?=
RD MlfQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rHc2lEPTB;MUKzJI5O NYjxcG9COjN4MUS4PVg>
HT-1197 M2\zVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkniTWM2OD1|MU[gcm0> M374RVI{PjF2OEm4
Molt-3 MonsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jIemlEPTB;NkCwJI5O M3\DbFI{PjF2OEm4
PA-1 M2L5Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTFyMEGgcm0> MXeyN|YyPDh7OB?=
Molt-4 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIewXlZKSzVyPUOwNFEhdk1? NIPiUpozOzZzNEi5PC=>
NCI-H292 NHvOb4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELpfGFKSzVyPUmwJI5O NEjmR|AzOzZzNEi5PC=>
A2780 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHJVFNKSzVyPUG0N{BvVQ>? MVyyN|YyPDh7OB?=
IGROV-1 MnP1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LWcmlEPTB;MUS2JI5O MXKyN|YyPDh7OB?=
SK-N-SH MkHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jnPGlEPTB;MUWwJI5O NHzie5gzOzZzNEi5PC=>
N-87 M2PDXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHP3[4lKSzVyPUOwO{BvVQ>? MlXZNlM3OTR6OUi=
H322 NFfOVnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoS0TWM2OD1|MkWgcm0> MYOyN|YyPDh7OB?=
H716 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTN|NDDuUS=> NEDsNpozOzZzNEi5PC=>
TT NHm5NldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTRyNjDuUS=> NFyxOVAzOzZzNEi5PC=>
Caki-1 NILRcmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTR3MDDuUS=> MkPwNlM3OTR6OUi=
5637 NEe1S3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTZzMDDuUS=> M2DNclI{PjF2OEm4
MB-453 NFXiPXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XXfGlEPTB;NkeyJI5O MoHVNlM3OTR6OUi=
RT-4 M4\BXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDJS29KSzVyPUixNEBvVQ>? M3rJcVI{PjF2OEm4
HOP92 M4S3PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PhbWlEPTB;OEKwJI5O NFv1c2QzOzZzNEi5PC=>
KG-1 M3vRZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vFfmlEPTB;OUCwJI5O M1vhU|I{PjF2OEm4
Hs-294T MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DWR2lEPTB;OUS1JI5O M17zNFI{PjF2OEm4
SF-539 NEn4b4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nuNmlEPTB;MUCwNEBvVQ>? NF3MPIQzOzZzNEi5PC=>
U-251 M4LPcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFe3cpZKSzVyPUGwNFAhdk1? NX3TPGJtOjN4MUS4PVg>
MB-468 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTFyMECgcm0> M4DlV|I{PjF2OEm4
HS746T NFSy[WVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETsRoNKSzVyPUGwNFAhdk1? NXfBO4NPOjN4MUS4PVg>
SCABER NIDNRWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLp[4xMUUN3ME2xNFAxKG6P NGTwWWYzOzZzNEi5PC=>
MCF-7 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TyOWlEPTB;MUCwNUBvVQ>? Mn7JNlM3OTR6OUi=
CHL-1 NIrzbXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4fySGlEPTB;MUS2NEBvVQ>? M1PSU|I{PjF2OEm4
U87MG NF6yeWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17WOWlEPTB;MkCwNEBvVQ>? Mlf2NlM3OTR6OUi=
SJCRH30 NH6xNYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvoSld[UUN3ME2yNFAzKG6P MX6yN|YyPDh7OB?=
ES-2 M{jaPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\sWFhKSzVyPUK2OVkhdk1? M33PSlI{PjF2OEm4
HT-1376 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3\EWmlEPTB;MkiwNEBvVQ>? M1XMfFI{PjF2OEm4
A172 NXjjXWVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DTc2lEPTB;M{CwNEBvVQ>? MX2yN|YyPDh7OB?=
769P M{\CdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPETWM2OD1|MECwJI5O M3S2R|I{PjF2OEm4
NCI-H520 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7GTJNKSzVyPUOwNFAhdk1? MVuyN|YyPDh7OB?=
DU145 NYrCd2c3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4e1WGlEPTB;M{CwNEBvVQ>? NEmzTJczOzZzNEi5PC=>
K562 Mk\XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTNyMECgcm0> NVG0d3RWOjN4MUS4PVg>
U-937 NY\lR5J{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnsW5M3UUN3ME2zNFAxKG6P NVPpbHRnOjN4MUS4PVg>
A204 NYnYWHF6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTNyMEGgcm0> NGLvVHkzOzZzNEi5PC=>
DAOY MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2K5VmlEPTB;M{CwNUBvVQ>? NXLSTnZ{OjN4MUS4PVg>
SF-268 NFn3O5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHr1XJJKSzVyPUOwNFEhdk1? NIPNPJkzOzZzNEi5PC=>
SF-295 NUTwbJJrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX[0T5hrUUN3ME2zNFAyKG6P MUmyN|YyPDh7OB?=
SNB-19 NYm1WFZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTNyMEGgcm0> MXeyN|YyPDh7OB?=
SNB-75 NUPlOJIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\vWXJKSzVyPUOwNFEhdk1? NHi5eIYzOzZzNEi5PC=>
U373-MG MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTNyMEGgcm0> MYqyN|YyPDh7OB?=
786-O MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXRd2pKSzVyPUOwNFEhdk1? NWriUIJ[OjN4MUS4PVg>
A498 NFz6RWNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHHFWZVKSzVyPUOwNFEhdk1? M1O3bVI{PjF2OEm4
ACHN MlL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV75RW9lUUN3ME2zNFAyKG6P M1zsSFI{PjF2OEm4
EKVX Mlf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;hPFIxUUN3ME2zNFAyKG6P MYSyN|YyPDh7OB?=
H226 M2nkTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jLOWlEPTB;M{CwNUBvVQ>? M4WxblI{PjF2OEm4
H522 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmO2TWM2OD1|MECxJI5O Mm\5NlM3OTR6OUi=
HeLa NFPFZXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTNyMEGgcm0> M1fPUFI{PjF2OEm4
SK-OV-3 NVTXO5ZUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVWzXJNNUUN3ME2zNFAyKG6P M{\tRVI{PjF2OEm4
Ln Cap NULRXIkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1X6U2lEPTB;M{CwNUBvVQ>? MljqNlM3OTR6OUi=
PC3 NVK5eHduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWDJR|UxRTNyMEGgcm0> NWH3OY05OjN4MUS4PVg>
SNU-16 NEf1TmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrTWVJKSzVyPUOwNFEhdk1? NX;0TZY3OjN4MUS4PVg>
FTC-133 MlK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHz[VVKSzVyPUOwNFEhdk1? NF7SZnIzOzZzNEi5PC=>
Ro82-W-1 NYq1fnh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTNyMEGgcm0> MoHaNlM3OTR6OUi=
Daudi Mnr4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\0ZlFKSzVyPUOwNFEhdk1? MmLsNlM3OTR6OUi=
Jijoye NEPhSW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUf1R3R4UUN3ME2zNFAyKG6P M3LXVVI{PjF2OEm4
Jurkat NIHUeVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HtcGlEPTB;M{CwNUBvVQ>? M2DFeFI{PjF2OEm4
J-82 Moi1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLkTWM2OD1|MECxJI5O MVKyN|YyPDh7OB?=
TCC-SUP MkTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTNyMEGgcm0> M4nwSVI{PjF2OEm4
BT-474 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTNyMEGgcm0> Ml;qNlM3OTR6OUi=
ZR-75-1 M1TQbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXSzPXRHUUN3ME2zNFAyKG6P NVO3VI43OjN4MUS4PVg>

... 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]

+ 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 (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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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