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 15 Publications

5 Customer Reviews

  • Immunoblot of H23 cells treated with trametinib (25 nM), SCH772984 (500 nM), or their combination for the times shown.

    Nature, 2016, 534(7609):647-51. SCH772984 purchased from Selleck.

    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.

  • Int J Oncol, 2018, 53(2):750-760. 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 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPQboNEUUN3ME2wMlI1KG6P NH7aeY4zPTN3MEmzNS=>
WM-266-4 M1y4Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jzWGlEPTB;MkCgcm0> MorHNlM3OTR6OUi=
UACC-62 MkLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTLbWlCUUN3ME2zNEBvVQ>? MljJNlM3OTR6OUi=
Colo-205 NFPY[pNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkXPTWM2OD1|NjDuUS=> M3\JUVI{PjF2OEm4
SK-Mel-1 M1ywSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTlfWhKSzVyPUO3JI5O MV2yN|YyPDh7OB?=
WiDr MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnPeWdyUUN3ME2zPUBvVQ>? NFP0fFUzOzZzNEi5PC=>
M14 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIG3c5VKSzVyPUS3JI5O Mo\KNlM3OTR6OUi=
HT-29 MmrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1r0eGlEPTB;NUCgcm0> NF;HOIszOzZzNEi5PC=>
8505C MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjKPYlKSzVyPUWwJI5O M{HzUFI{PjF2OEm4
HT-144 M2HJW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHm2VZdKSzVyPU[wJI5O MmHkNlM3OTR6OUi=
SK-Mel-5 NUOwUmRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTZ4IH7N M2jWSVI{PjF2OEm4
A375-SM MmfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXTTWM2OD15NTDuUS=> MWOyN|YyPDh7OB?=
SK-Mel-28 NVfve3R{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTh3IH7N NUXJZZZwOjN4MUS4PVg>
LOX MoDRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTFyMDDuUS=> M{PjNlI{PjF2OEm4
SK-Mel-3 NHf4WlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVLBXZVHUUN3ME2xNVghdk1? NFPLSIgzOzZzNEi5PC=>
K1 MoD0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrIT2hnUUN3ME2xN|Ahdk1? M1XQcVI{PjF2OEm4
Hs-695T NYH4PWxiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\vPXJKSzVyPUG2OUBvVQ>? NIXBW|MzOzZzNEi5PC=>
BHT-101 NGDTNWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTNyMDDuUS=> M4nnUFI{PjF2OEm4
RPMI-7951 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPSTWM2OD1|NESgcm0> NX\YRYNnOjN4MUS4PVg>
A2058 M3LtPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M175dWlEPTB;M{[wJI5O NXe2bmhGOjN4MUS4PVg>
SK-Hep-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm\BTWM2OD1zNEKyJI5O NWLUdYJ6OjN4MUS4PVg>
A673 M2C4dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHy5XIJKSzVyPUOwNFEhdk1? M1i4T|I{PjF2OEm4
DBTRG-05MG M2i3XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7BTWM2OD1|MECxJI5O NEm3eHUzOzZzNEi5PC=>
SW-626 NV71fHJIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIS4enJKSzVyPUOzJI5O MlHuNlM3OTR6OUi=
LoVo NEPHTY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrPTWM2OD12NzDuUS=> MYqyN|YyPDh7OB?=
MiaPaCa NVPsU2l6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHrTWM2OD13MzDuUS=> MU[yN|YyPDh7OB?=
SW-620 NFG2PYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInsdIVKSzVyPUGwOEBvVQ>? MlrDNlM3OTR6OUi=
CAPAN-1 M4jqRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGO4PFRKSzVyPUGwOEBvVQ>? M3HvcFI{PjF2OEm4
SW-527 M3y0Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHMWmZrUUN3ME2xNlEhdk1? MWSyN|YyPDh7OB?=
HCT-116 MmOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkDMTWM2OD1zMkigcm0> NX[5eoxVOjN4MUS4PVg>
SW-480 MoLsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1v3W2lEPTB;MU[1JI5O NWDsVHFiOjN4MUS4PVg>
HPAC NFSyfFJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTF5MDDuUS=> MmO4NlM3OTR6OUi=
OVCAR-5 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\3flU6UUN3ME2yNFghdk1? M1\PWFI{PjF2OEm4
AsPc-1 NWnLXnhKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HmXWlEPTB;MkewJI5O MmDHNlM3OTR6OUi=
A549 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3kflhKSzVyPUOyOkBvVQ>? NVjM[HcyOjN4MUS4PVg>
SNU-1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGf6PIhKSzVyPUO1OEBvVQ>? MWKyN|YyPDh7OB?=
HOP62 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHM[ZlKSzVyPU[3OkBvVQ>? MUKyN|YyPDh7OB?=
H23 NFu4NI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHO3NYxKSzVyPUGwNFAhdk1? MXyyN|YyPDh7OB?=
MB-231 M1zlXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIr3[mtKSzVyPUGwNFAhdk1? Ml;VNlM3OTR6OUi=
SU.86.86 Mnm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTFyMEGgcm0> NWfHeFRyOjN4MUS4PVg>
CFPAC-1 M3TPO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTFyMEGgcm0> MliwNlM3OTR6OUi=
A427 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfte2JKSzVyPUG0N|Mhdk1? MXyyN|YyPDh7OB?=
MDAH-2774 M17r[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fQd2lEPTB;Mk[1O{BvVQ>? NGjTNYkzOzZzNEi5PC=>
NCI-H157 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrHSo9HUUN3ME2zNFAxKG6P NVnKN4tjOjN4MUS4PVg>
HTB-177 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTNyMECgcm0> MlS3NlM3OTR6OUi=
UM-UC-3 M3;5RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoTXTWM2OD1|MECxJI5O Mnz4NlM3OTR6OUi=
HCT-8 NHPVO|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTNyMEGgcm0> NIjFPHozOzZzNEi5PC=>
Panc-1 NFzGfnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWSwSo91UUN3ME2zNFAyKG6P MmLYNlM3OTR6OUi=
DLD-1 NWHUWXNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXSTWM2OD1|MECxJI5O NFfSbYIzOzZzNEi5PC=>
HCT-15 M1LU[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn7xTWM2OD1|MECxJI5O NH:3eW0zOzZzNEi5PC=>
HL-60 Mly2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2nzSWlEPTB;M{Cgcm0> NH3WcnUzOzZzNEi5PC=>
SK-Mel-2 NY\5UHJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYWx[oQ3UUN3ME2zOEBvVQ>? MVSyN|YyPDh7OB?=
RD M{TZc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlG2TWM2OD1zMkOgcm0> M{XldFI{PjF2OEm4
HT-1197 M2SxVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPBb5R7UUN3ME2zNVYhdk1? NV3LOopTOjN4MUS4PVg>
Molt-3 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGi0PVBKSzVyPU[wNEBvVQ>? NYXTT5U3OjN4MUS4PVg>
PA-1 M1f6[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTFyMEGgcm0> NETjVFQzOzZzNEi5PC=>
Molt-4 NYHaOmVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PsZmlEPTB;M{CwNUBvVQ>? M3y3b|I{PjF2OEm4
NCI-H292 M2\EOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2m4S2lEPTB;OUCgcm0> MmnUNlM3OTR6OUi=
A2780 M3G0cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7sRmxKSzVyPUG0N{BvVQ>? NI\qXnYzOzZzNEi5PC=>
IGROV-1 M3ntXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDacFJKSzVyPUG0OkBvVQ>? MUOyN|YyPDh7OB?=
SK-N-SH NGrWXWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33uS2lEPTB;MUWwJI5O MV6yN|YyPDh7OB?=
N-87 NGjQdJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULNNXdIUUN3ME2zNFchdk1? MUSyN|YyPDh7OB?=
H322 M3j0SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYKyUo1JUUN3ME2zNlUhdk1? MUCyN|YyPDh7OB?=
H716 NFSyS4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTjWoZKSzVyPUOzOEBvVQ>? NWTzWFZ1OjN4MUS4PVg>
TT MkfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTRyNjDuUS=> NGTPOYYzOzZzNEi5PC=>
Caki-1 M4[1d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV;kWXJqUUN3ME20OVAhdk1? MnzXNlM3OTR6OUi=
5637 NIf6NIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWrDS|VWUUN3ME22NVAhdk1? M{XTclI{PjF2OEm4
MB-453 NF3MbHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnm5TWM2OD14N{Kgcm0> M2XUZVI{PjF2OEm4
RT-4 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rCOGlEPTB;OEGwJI5O MYiyN|YyPDh7OB?=
HOP92 MlnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnS5TWM2OD16MkCgcm0> MkHBNlM3OTR6OUi=
KG-1 M2Xod2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHSTHdKSzVyPUmwNEBvVQ>? NYr5RVNDOjN4MUS4PVg>
Hs-294T NWjlWXBHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XxOWlEPTB;OUS1JI5O MljFNlM3OTR6OUi=
SF-539 MmTTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGX6fnlKSzVyPUGwNFAhdk1? MnLXNlM3OTR6OUi=
U-251 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7qcIpKSzVyPUGwNFAhdk1? MljqNlM3OTR6OUi=
MB-468 M1P4SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3v0UGlEPTB;MUCwNEBvVQ>? Mk\FNlM3OTR6OUi=
HS746T MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TnNmlEPTB;MUCwNEBvVQ>? NFXHWoYzOzZzNEi5PC=>
SCABER NGPCWXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVqwe3hSUUN3ME2xNFAxKG6P MlvUNlM3OTR6OUi=
MCF-7 NVPQSld6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTFyMEGgcm0> NWPNbndmOjN4MUS4PVg>
CHL-1 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnXdYZKSzVyPUG0OlAhdk1? M4OxelI{PjF2OEm4
U87MG NInCd2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvLPVVbUUN3ME2yNFAxKG6P MUOyN|YyPDh7OB?=
SJCRH30 M3TwXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\z[WVKSzVyPUKwNFIhdk1? NYHvbFhTOjN4MUS4PVg>
ES-2 NGTlSoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPyOWgzUUN3ME2yOlU6KG6P MVuyN|YyPDh7OB?=
HT-1376 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33DfGlEPTB;MkiwNEBvVQ>? NV7S[JFoOjN4MUS4PVg>
A172 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVj4UndNUUN3ME2zNFAxKG6P M37oPVI{PjF2OEm4
769P NHL3T5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjjXWRWUUN3ME2zNFAxKG6P NYjrRXl4OjN4MUS4PVg>
NCI-H520 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrsfZZCUUN3ME2zNFAxKG6P NEfRSFYzOzZzNEi5PC=>
DU145 MnzvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn22TWM2OD1|MECwJI5O MXyyN|YyPDh7OB?=
K562 MmrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TLbGlEPTB;M{CwNEBvVQ>? MVSyN|YyPDh7OB?=
U-937 M1H3e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTNyMECgcm0> NEG3N48zOzZzNEi5PC=>
A204 NYHMTHp2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPRcFdKSzVyPUOwNFEhdk1? Mmf1NlM3OTR6OUi=
DAOY MmPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF:5Z49KSzVyPUOwNFEhdk1? NWjweVNXOjN4MUS4PVg>
SF-268 MmryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGT0cXlKSzVyPUOwNFEhdk1? MUGyN|YyPDh7OB?=
SF-295 NVfw[4JtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;DTWM2OD1|MECxJI5O M3LSVFI{PjF2OEm4
SNB-19 M4fIfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XwXmlEPTB;M{CwNUBvVQ>? MYSyN|YyPDh7OB?=
SNB-75 NIH4R25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTNyMEGgcm0> M4PpPVI{PjF2OEm4
U373-MG MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTNyMEGgcm0> NX60Wo9WOjN4MUS4PVg>
786-O MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTNyMEGgcm0> MXWyN|YyPDh7OB?=
A498 M3TYN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\qT2lEPTB;M{CwNUBvVQ>? NYfESpkxOjN4MUS4PVg>
ACHN MnqzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTNyMEGgcm0> MYiyN|YyPDh7OB?=
EKVX M2XGTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jxdWlEPTB;M{CwNUBvVQ>? NWTIU|J7OjN4MUS4PVg>
H226 M3TNdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4GxO2lEPTB;M{CwNUBvVQ>? M{nnW|I{PjF2OEm4
H522 M1jiOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTC[G5FUUN3ME2zNFAyKG6P NUXRelIzOjN4MUS4PVg>
HeLa NYLZbXNJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fEe2lEPTB;M{CwNUBvVQ>? MnG1NlM3OTR6OUi=
SK-OV-3 M2TWeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnT4TWM2OD1|MECxJI5O MlezNlM3OTR6OUi=
Ln Cap NF61UFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TCPGlEPTB;M{CwNUBvVQ>? M3vJTlI{PjF2OEm4
PC3 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4KwVGlEPTB;M{CwNUBvVQ>? NYi4O5hLOjN4MUS4PVg>
SNU-16 MnfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\oN2N7UUN3ME2zNFAyKG6P M3viZlI{PjF2OEm4
FTC-133 NI[1T4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfaOGJKSzVyPUOwNFEhdk1? NUjGboVMOjN4MUS4PVg>
Ro82-W-1 M4GweWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\CV3F3UUN3ME2zNFAyKG6P NFL0VYMzOzZzNEi5PC=>
Daudi MkjJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTaOZpMUUN3ME2zNFAyKG6P MVWyN|YyPDh7OB?=
Jijoye M4LwVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrIW3FKSzVyPUOwNFEhdk1? M2C2SlI{PjF2OEm4
Jurkat MnPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3qc4FxUUN3ME2zNFAyKG6P M1rnUVI{PjF2OEm4
J-82 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonzTWM2OD1|MECxJI5O MUKyN|YyPDh7OB?=
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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]

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  • 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
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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):
    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