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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3 Customer Reviews

  • 293T cells were transfected with Flag-WT-FBW7. Thirty hours post transfection, cells were pretreated with MG132 and various MEK/ERK inhibitors overnight before harvesting. FBW7 phosphorylation status was examined by immunoblot analysis after immunoprecipitation.

    Cell Research, 2015, 25: 561-573. SCH772984 purchased from Selleck.

    K562 cells were exposed to ERK inhibitor SCH772984 (1 uM, 2 uM, 5 uM) for 48 h. Apoptosis was analyzed by Annexin V-APC labeling.

    Leuk Lymphoma 2014 1, 8. SCH772984 purchased from Selleck.

  • ERK1/2 influences the effects of TGF-β1 on Cdk5 and Bax in PC12 cells. A. Original western blot showing the level of Cdk5 and respective Actin in PC12 cells with TGF-β1 (40 ng/ml) treatment in the presence of SCH772984(1 μM) and LY294002(1.5 μM) for 2 h. B. Arithmetic means ± SEM (n = 4) of Cdk5 protein abundance in PC12 cells with TGF-β1 treatment in the presence of SCH772984(1 μM) and LY294002(1.5 μM) for 2 h. C. Original western blot showing the level of Bax and respective Actin in PC12 cells with TGF-β1 (40 ng/ml) treatment in the presence of SCH772984(1 μM) for 2 h. D. Arithmetic means ± SEM (n = 4) of Bax protein abundance in PC12 cells with TGF-β1 treatment in the presence of SCH772984(1 μM) for 2 h. **(p < 0.01), ***(p < 0.001) indicate statistically significant difference.

    Biochem Biophys Res Commun, 2017, 485(4):775-781. SCH772984 purchased from Selleck.

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 MmXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXUTWM2OD1yLkK0JI5O MlTNNlU{PTB7M{G=
WM-266-4 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmLWTWM2OD1{MDDuUS=> MWqyN|YyPDh7OB?=
UACC-62 M{jPdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTNyIH7N M375TFI{PjF2OEm4
Colo-205 NX3hcGZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIPvfHNKSzVyPUO2JI5O M1LkbFI{PjF2OEm4
SK-Mel-1 NGLobJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYXJR|UxRTN5IH7N MXGyN|YyPDh7OB?=
WiDr NEjqVHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTN7IH7N M4Tue|I{PjF2OEm4
M14 M37mOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfPTWM2OD12NzDuUS=> M4DISVI{PjF2OEm4
HT-29 M{HnSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjrZXNKSzVyPUWwJI5O MV:yN|YyPDh7OB?=
8505C MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTVyIH7N M1H6T|I{PjF2OEm4
HT-144 NVnyephxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTZyIH7N NEjobm8zOzZzNEi5PC=>
SK-Mel-5 NXHDT|Z6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTtTWM2OD14NjDuUS=> MoPvNlM3OTR6OUi=
A375-SM MoDQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGD6PFVKSzVyPUe1JI5O MW[yN|YyPDh7OB?=
SK-Mel-28 NGnnVGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlK0TWM2OD16NTDuUS=> MnjCNlM3OTR6OUi=
LOX NUj0cXBPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfuTWM2OD1zMECgcm0> MknHNlM3OTR6OUi=
SK-Mel-3 NX\XNYpIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnL0TWM2OD1zMUigcm0> MlLRNlM3OTR6OUi=
K1 Mlz0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7STWM2OD1zM{Cgcm0> M3rBNVI{PjF2OEm4
Hs-695T M{XTU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\He|dKSzVyPUG2OUBvVQ>? NHr2dowzOzZzNEi5PC=>
BHT-101 MknkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTNVGNKSzVyPUOwNEBvVQ>? NVm5[JgxOjN4MUS4PVg>
RPMI-7951 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXpV29KSzVyPUO0OEBvVQ>? MV:yN|YyPDh7OB?=
A2058 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTN4MDDuUS=> MYSyN|YyPDh7OB?=
SK-Hep-1 MnvSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfLS5ZKSzVyPUG0NlIhdk1? NYDheFJ[OjN4MUS4PVg>
A673 NXrNWJg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnOUYtKSzVyPUOwNFEhdk1? NHnVWJkzOzZzNEi5PC=>
DBTRG-05MG MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nXdGlEPTB;M{CwNUBvVQ>? MXeyN|YyPDh7OB?=
SW-626 NYrZfnlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LLSGlEPTB;M{Ogcm0> MXiyN|YyPDh7OB?=
LoVo NFjpeG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37CbWlEPTB;NEegcm0> M{jDZ|I{PjF2OEm4
MiaPaCa M{nBeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTV|IH7N MVOyN|YyPDh7OB?=
SW-620 NVLoOFQ2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmi4TWM2OD1zMESgcm0> MYeyN|YyPDh7OB?=
CAPAN-1 NFrSTHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTFyNDDuUS=> MUKyN|YyPDh7OB?=
SW-527 NXjEblZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PkPWlEPTB;MUKxJI5O MlLMNlM3OTR6OUi=
HCT-116 NV:0UWE1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fEe2lEPTB;MUK4JI5O MXGyN|YyPDh7OB?=
SW-480 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYqxZZNZUUN3ME2xOlUhdk1? NWm5dmdHOjN4MUS4PVg>
HPAC M1jUWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDXVVFRUUN3ME2xO|Ahdk1? M1\E[FI{PjF2OEm4
OVCAR-5 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvHZ3hbUUN3ME2yNFghdk1? NETZdHYzOzZzNEi5PC=>
AsPc-1 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHjTWM2OD1{N{Cgcm0> M1;nPFI{PjF2OEm4
A549 M4f1T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PQd2lEPTB;M{K2JI5O Ml\VNlM3OTR6OUi=
SNU-1 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2T3fGlEPTB;M{W0JI5O NWqweGRMOjN4MUS4PVg>
HOP62 NU[xNZdOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DKRmlEPTB;Nke2JI5O M4jC[FI{PjF2OEm4
H23 NVO1VmFPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzC[Fl[UUN3ME2xNFAxKG6P MWOyN|YyPDh7OB?=
MB-231 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrtTWM2OD1zMECwJI5O Mm\vNlM3OTR6OUi=
SU.86.86 NWnqV2RvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVriTpZlUUN3ME2xNFAyKG6P MlvuNlM3OTR6OUi=
CFPAC-1 NXv3VIhxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTFyMEGgcm0> NEjyZ4gzOzZzNEi5PC=>
A427 NY\JT|d[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLMT4JKSzVyPUG0N|Mhdk1? MV6yN|YyPDh7OB?=
MDAH-2774 NVTMPWQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTJ4NUegcm0> MnjzNlM3OTR6OUi=
NCI-H157 NIDERmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTNyMECgcm0> NWfKSFBsOjN4MUS4PVg>
HTB-177 NWnPd3d3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDsfnBKSzVyPUOwNFAhdk1? M{jqUVI{PjF2OEm4
UM-UC-3 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3viUmlEPTB;M{CwNUBvVQ>? MWOyN|YyPDh7OB?=
HCT-8 NUfjOWp4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTNyMEGgcm0> NWLwZod1OjN4MUS4PVg>
Panc-1 NIS2e|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmnUTWM2OD1|MECxJI5O NHm4WlUzOzZzNEi5PC=>
DLD-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTNyMEGgcm0> NHjpZ28zOzZzNEi5PC=>
HCT-15 MnPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmK2TWM2OD1|MECxJI5O MWGyN|YyPDh7OB?=
HL-60 Mk\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXIfppKSzVyPUOwJI5O MYqyN|YyPDh7OB?=
SK-Mel-2 NUDI[Zk3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTN2IH7N M17L[|I{PjF2OEm4
RD MoXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrGPVh2UUN3ME2xNlMhdk1? MYSyN|YyPDh7OB?=
HT-1197 M3K4TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWHmbo46UUN3ME2zNVYhdk1? NHPr[ZczOzZzNEi5PC=>
Molt-3 NVuwSmZsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnP1TWM2OD14MECgcm0> MoDnNlM3OTR6OUi=
PA-1 M4e0Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTFyMEGgcm0> NFz3SXAzOzZzNEi5PC=>
Molt-4 M1;w[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4L3dWlEPTB;M{CwNUBvVQ>? NWf4eFJYOjN4MUS4PVg>
NCI-H292 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXHS5ZKSzVyPUmwJI5O NV\mTotxOjN4MUS4PVg>
A2780 MmPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHWycZFKSzVyPUG0N{BvVQ>? M3PUU|I{PjF2OEm4
IGROV-1 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH:2R3ZKSzVyPUG0OkBvVQ>? NFrpbo8zOzZzNEi5PC=>
SK-N-SH NFHCT2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUnuN|JsUUN3ME2xOVAhdk1? MlvhNlM3OTR6OUi=
N-87 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjpOJZKSzVyPUOwO{BvVQ>? MWOyN|YyPDh7OB?=
H322 M13pXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTN{NTDuUS=> Ml\KNlM3OTR6OUi=
H716 NUfmSFY6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7XTWM2OD1|M{Sgcm0> MmDhNlM3OTR6OUi=
TT M37PPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTRyNjDuUS=> NXX0NGNnOjN4MUS4PVg>
Caki-1 NIO5VoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XwU2lEPTB;NEWwJI5O NF7zUIkzOzZzNEi5PC=>
5637 NH\RWHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HYTWlEPTB;NkGwJI5O NIfhN4gzOzZzNEi5PC=>
MB-453 NV:5NZZuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXSO2JEUUN3ME22O|Ihdk1? M1XrdlI{PjF2OEm4
RT-4 Mn;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;mSGlEPTB;OEGwJI5O NXS1fZRYOjN4MUS4PVg>
HOP92 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDoTWM2OD16MkCgcm0> M4DiRVI{PjF2OEm4
KG-1 NGXxdo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\1fXJwUUN3ME25NFAhdk1? NYPPdpJqOjN4MUS4PVg>
Hs-294T Mnr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTl2NTDuUS=> NX;IZ|lXOjN4MUS4PVg>
SF-539 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfVc4VKSzVyPUGwNFAhdk1? MkLFNlM3OTR6OUi=
U-251 MkC2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrpd3RKSzVyPUGwNFAhdk1? M3rONlI{PjF2OEm4
MB-468 NF7UO2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILme|RKSzVyPUGwNFAhdk1? MWKyN|YyPDh7OB?=
HS746T M4rrcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPnSHFKSzVyPUGwNFAhdk1? MXSyN|YyPDh7OB?=
SCABER M2PCVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTFyMECgcm0> M2r4S|I{PjF2OEm4
MCF-7 NUDTe|FvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTFyMEGgcm0> NX;kPFB1OjN4MUS4PVg>
CHL-1 NWXqVmNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTF2NkCgcm0> MlXtNlM3OTR6OUi=
U87MG MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYm5NmgyUUN3ME2yNFAxKG6P M2T0bFI{PjF2OEm4
SJCRH30 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrKcnpKSzVyPUKwNFIhdk1? MYmyN|YyPDh7OB?=
ES-2 NHf3SY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTJ4NUmgcm0> NHrQNFAzOzZzNEi5PC=>
HT-1376 NXPxZ2V7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HsSGlEPTB;MkiwNEBvVQ>? MUGyN|YyPDh7OB?=
A172 M1Kzemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2e0PGlEPTB;M{CwNEBvVQ>? NVTwT2JMOjN4MUS4PVg>
769P M3nteWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnzOIJKSzVyPUOwNFAhdk1? M{njd|I{PjF2OEm4
NCI-H520 NH\kV25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInuboRKSzVyPUOwNFAhdk1? MV6yN|YyPDh7OB?=
DU145 NXiyO|dzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTNyMECgcm0> NF:4[WozOzZzNEi5PC=>
K562 MmXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;mdFZKSzVyPUOwNFAhdk1? NVPEU3Q{OjN4MUS4PVg>
U-937 NV3q[HZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{S5VGlEPTB;M{CwNEBvVQ>? NIrtUoszOzZzNEi5PC=>
A204 M4rleGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjjTWM2OD1|MECxJI5O Mn6xNlM3OTR6OUi=
DAOY MlToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfmZppiUUN3ME2zNFAyKG6P NH7Ib|IzOzZzNEi5PC=>
SF-268 M2T5bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTNyMEGgcm0> NEGwPZkzOzZzNEi5PC=>
SF-295 NIXKUlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEL3XpZKSzVyPUOwNFEhdk1? M2j1OFI{PjF2OEm4
SNB-19 MoG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\FWJZKSzVyPUOwNFEhdk1? M2jlRlI{PjF2OEm4
SNB-75 NWPtdoNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHXTWM2OD1|MECxJI5O MXeyN|YyPDh7OB?=
U373-MG NIDzTo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTNyMEGgcm0> NUnW[4NWOjN4MUS4PVg>
786-O NHLPTFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGn4cmxKSzVyPUOwNFEhdk1? MnPWNlM3OTR6OUi=
A498 NWK2SY5rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTNyMEGgcm0> MmLmNlM3OTR6OUi=
ACHN NED2TIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4j5RmlEPTB;M{CwNUBvVQ>? NVTlfIcxOjN4MUS4PVg>
EKVX M3m1WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHO4cFBKSzVyPUOwNFEhdk1? NE\0RWUzOzZzNEi5PC=>
H226 Mn:zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUHueVM{UUN3ME2zNFAyKG6P NXT0[FZwOjN4MUS4PVg>
H522 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37QdWlEPTB;M{CwNUBvVQ>? NXzKO|NnOjN4MUS4PVg>
HeLa MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPmTWM2OD1|MECxJI5O NGjhZoYzOzZzNEi5PC=>
SK-OV-3 MnTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX:4VYhLUUN3ME2zNFAyKG6P NGXm[pYzOzZzNEi5PC=>
Ln Cap NF3hc25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTNyMEGgcm0> NWfJT45XOjN4MUS4PVg>
PC3 MnPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX[ze|VxUUN3ME2zNFAyKG6P NF3rXYwzOzZzNEi5PC=>
SNU-16 NIryR3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHruVGVKSzVyPUOwNFEhdk1? NYCwRpNzOjN4MUS4PVg>
FTC-133 M3\6[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHVe5htUUN3ME2zNFAyKG6P NWTvO4ZHOjN4MUS4PVg>
Ro82-W-1 MnTtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfzWGZKSzVyPUOwNFEhdk1? NF3uUoYzOzZzNEi5PC=>
Daudi NIXZVIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHJO2xKSzVyPUOwNFEhdk1? MY[yN|YyPDh7OB?=
Jijoye M3\2Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFny[JhKSzVyPUOwNFEhdk1? NE\Le20zOzZzNEi5PC=>
Jurkat NFfyRYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jF[mlEPTB;M{CwNUBvVQ>? NFTGZ2ozOzZzNEi5PC=>
J-82 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHhWmJKSzVyPUOwNFEhdk1? NYLUZ5h{OjN4MUS4PVg>
TCC-SUP MnThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTNyMEGgcm0> NELLSHIzOzZzNEi5PC=>
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... Click to View More Cell Line Experimental Data

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)

  • 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