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 NWqweHJ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorOTWM2OD1yLkK0JI5O M2ewVFI2OzVyOUOx
WM-266-4 NWX3XppLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLIU4kzUUN3ME2yNEBvVQ>? M3jm[|I{PjF2OEm4
UACC-62 MkHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4TTdmlEPTB;M{Cgcm0> MYWyN|YyPDh7OB?=
Colo-205 NYq3[XJZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXrLcG91UUN3ME2zOkBvVQ>? M3TVOFI{PjF2OEm4
SK-Mel-1 NFfZb2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3UeG9FUUN3ME2zO{BvVQ>? MX:yN|YyPDh7OB?=
WiDr NHnacWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2W2RmlEPTB;M{mgcm0> NF7YcGEzOzZzNEi5PC=>
M14 NFTNS2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TlbGlEPTB;NEegcm0> MXKyN|YyPDh7OB?=
HT-29 NE\x[I1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHflfmhKSzVyPUWwJI5O M1zIZlI{PjF2OEm4
8505C NWXhNYUzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlniTWM2OD13MDDuUS=> MmXDNlM3OTR6OUi=
HT-144 MkjFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjnZZJKSzVyPU[wJI5O NXnqRoxbOjN4MUS4PVg>
SK-Mel-5 NFflWXVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULme3NvUUN3ME22OkBvVQ>? M{nPVlI{PjF2OEm4
A375-SM NXW5XJBKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFK0fFJKSzVyPUe1JI5O NIWyZ3kzOzZzNEi5PC=>
SK-Mel-28 NH\5fnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjaTWM2OD16NTDuUS=> NFLlW20zOzZzNEi5PC=>
LOX NYXtSnJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTFyMDDuUS=> MXyyN|YyPDh7OB?=
SK-Mel-3 M4PnZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjucFJ2UUN3ME2xNVghdk1? M2f0clI{PjF2OEm4
K1 MmnVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTF|MDDuUS=> MWOyN|YyPDh7OB?=
Hs-695T MlL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTkb2FiUUN3ME2xOlUhdk1? M{jkNlI{PjF2OEm4
BHT-101 NYn4e4VoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\hRmFHUUN3ME2zNFAhdk1? MWqyN|YyPDh7OB?=
RPMI-7951 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLWVppKSzVyPUO0OEBvVQ>? M4j1TlI{PjF2OEm4
A2058 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXIN2hKSzVyPUO2NEBvVQ>? M4Dl[VI{PjF2OEm4
SK-Hep-1 Ml36S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWLJR|UxRTF2MkKgcm0> NVHWOVN{OjN4MUS4PVg>
A673 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrVTWM2OD1|MECxJI5O MVyyN|YyPDh7OB?=
DBTRG-05MG MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWC3OGV6UUN3ME2zNFAyKG6P NWnHb|c{OjN4MUS4PVg>
SW-626 NHexSmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnvV4F7UUN3ME2zN{BvVQ>? MV2yN|YyPDh7OB?=
LoVo NIKzSItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1Xoe2lEPTB;NEegcm0> MXyyN|YyPDh7OB?=
MiaPaCa NHHsXJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljaTWM2OD13MzDuUS=> NYDERWR3OjN4MUS4PVg>
SW-620 Mmf2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\aNXJVUUN3ME2xNFQhdk1? MV:yN|YyPDh7OB?=
CAPAN-1 NEfCRmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTFyNDDuUS=> NGHyVI8zOzZzNEi5PC=>
SW-527 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnxTWM2OD1zMkGgcm0> MUeyN|YyPDh7OB?=
HCT-116 NX7tRYZjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjsTWM2OD1zMkigcm0> MV:yN|YyPDh7OB?=
SW-480 M2TQVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnqVG5rUUN3ME2xOlUhdk1? M1TnNlI{PjF2OEm4
HPAC NGLzNWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPMTWM2OD1zN{Cgcm0> MYGyN|YyPDh7OB?=
OVCAR-5 NVvQR|k3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjUcFdCUUN3ME2yNFghdk1? NFntPHAzOzZzNEi5PC=>
AsPc-1 M1\1SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmKyTWM2OD1{N{Cgcm0> MUOyN|YyPDh7OB?=
A549 NU[2Z2xmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTN{NjDuUS=> NXPVcXRlOjN4MUS4PVg>
SNU-1 MnzZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rMW2lEPTB;M{W0JI5O MVWyN|YyPDh7OB?=
HOP62 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTYT3NKUUN3ME22O|Yhdk1? MnfqNlM3OTR6OUi=
H23 NVXUXGdPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTFyMECgcm0> MWqyN|YyPDh7OB?=
MB-231 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\6TWM2OD1zMECwJI5O M1T5clI{PjF2OEm4
SU.86.86 M2PpfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTFyMEGgcm0> NFe3fWEzOzZzNEi5PC=>
CFPAC-1 NEPtbYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFu5[odKSzVyPUGwNFEhdk1? MV6yN|YyPDh7OB?=
A427 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGr0OnNKSzVyPUG0N|Mhdk1? MY[yN|YyPDh7OB?=
MDAH-2774 Mn\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTJ4NUegcm0> Ml\QNlM3OTR6OUi=
NCI-H157 NX60bXRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\wW2lEPTB;M{CwNEBvVQ>? NHuwXJIzOzZzNEi5PC=>
HTB-177 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{[0R2lEPTB;M{CwNEBvVQ>? MkX1NlM3OTR6OUi=
UM-UC-3 M{fMNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjSSFZpUUN3ME2zNFAyKG6P NHvIOXozOzZzNEi5PC=>
HCT-8 MlezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTNyMEGgcm0> NUT4ZZYyOjN4MUS4PVg>
Panc-1 MknPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTNyMEGgcm0> NWfJR5RSOjN4MUS4PVg>
DLD-1 M4DRemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGLlPFFKSzVyPUOwNFEhdk1? NHH0SoYzOzZzNEi5PC=>
HCT-15 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TuemlEPTB;M{CwNUBvVQ>? MXeyN|YyPDh7OB?=
HL-60 NWnZd4RyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHryW|dKSzVyPUOwJI5O MYeyN|YyPDh7OB?=
SK-Mel-2 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF[3U3BKSzVyPUO0JI5O NWj4[m8zOjN4MUS4PVg>
RD NIjEPVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3nTWM2OD1zMkOgcm0> NV;6VFM1OjN4MUS4PVg>
HT-1197 NEHIWHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;LZoRKSzVyPUOxOkBvVQ>? M{XO[lI{PjF2OEm4
Molt-3 M2XITmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTZyMDDuUS=> NHfhfFEzOzZzNEi5PC=>
PA-1 NIixU|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TRdGlEPTB;MUCwNUBvVQ>? NXy1dJQ6OjN4MUS4PVg>
Molt-4 Mkm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTNyMEGgcm0> NHf1N|UzOzZzNEi5PC=>
NCI-H292 NF63c5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrUcXRKSzVyPUmwJI5O NULPOpozOjN4MUS4PVg>
A2780 MmjhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTF2MzDuUS=> M3\OU|I{PjF2OEm4
IGROV-1 MnmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTF2NjDuUS=> MY[yN|YyPDh7OB?=
SK-N-SH NULsOZJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3i5ZmlEPTB;MUWwJI5O M3nlWlI{PjF2OEm4
N-87 NI\uc21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13ZTGlEPTB;M{C3JI5O M1v0eFI{PjF2OEm4
H322 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPnbWJKSzVyPUOyOUBvVQ>? MnLLNlM3OTR6OUi=
H716 M2ftR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfVTWM2OD1|M{Sgcm0> M2W4cVI{PjF2OEm4
TT Mn:5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWm0XINlUUN3ME20NFYhdk1? M2HzXFI{PjF2OEm4
Caki-1 MkDoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vFVGlEPTB;NEWwJI5O MXuyN|YyPDh7OB?=
5637 NXqzdIVUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVzJR|UxRTZzMDDuUS=> NGPmeoozOzZzNEi5PC=>
MB-453 M1LMW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTZ5MjDuUS=> MVyyN|YyPDh7OB?=
RT-4 M2r1bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHZTWM2OD16MUCgcm0> MYiyN|YyPDh7OB?=
HOP92 NF64NnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M374SGlEPTB;OEKwJI5O MVyyN|YyPDh7OB?=
KG-1 MonWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTlyMDDuUS=> NWjMUVJtOjN4MUS4PVg>
Hs-294T NYLETJN7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXP4bIsxUUN3ME25OFUhdk1? Mli1NlM3OTR6OUi=
SF-539 NGLBO3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTFyMECgcm0> MYWyN|YyPDh7OB?=
U-251 NELWb4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjTRmJ3UUN3ME2xNFAxKG6P MXGyN|YyPDh7OB?=
MB-468 Mm\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFqxfVJKSzVyPUGwNFAhdk1? MXuyN|YyPDh7OB?=
HS746T Mli1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1noVWlEPTB;MUCwNEBvVQ>? M{LhO|I{PjF2OEm4
SCABER MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXqTWM2OD1zMECwJI5O MnHUNlM3OTR6OUi=
MCF-7 MojhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoX6TWM2OD1zMECxJI5O NGH5eJMzOzZzNEi5PC=>
CHL-1 M4TQ[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrEUWFpUUN3ME2xOFYxKG6P Ml7PNlM3OTR6OUi=
U87MG NYSwRmxqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rBV2lEPTB;MkCwNEBvVQ>? MVSyN|YyPDh7OB?=
SJCRH30 MmOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTNXXRKSzVyPUKwNFIhdk1? MoPKNlM3OTR6OUi=
ES-2 MmjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXRTWM2OD1{NkW5JI5O M1vpNFI{PjF2OEm4
HT-1376 Mm\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULPT3BpUUN3ME2yPFAxKG6P NEXvRZMzOzZzNEi5PC=>
A172 NI[3[4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYT0ZWNjUUN3ME2zNFAxKG6P NWDNW|BOOjN4MUS4PVg>
769P NELHOpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlvMTWM2OD1|MECwJI5O NEnuVYozOzZzNEi5PC=>
NCI-H520 M2jHdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmnRTWM2OD1|MECwJI5O NEP2epAzOzZzNEi5PC=>
DU145 M2fCNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NET4TFlKSzVyPUOwNFAhdk1? M3fOd|I{PjF2OEm4
K562 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nubWlEPTB;M{CwNEBvVQ>? M4f2Z|I{PjF2OEm4
U-937 MmnaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTNyMECgcm0> NFq0TXEzOzZzNEi5PC=>
A204 M1nzPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1L6SmlEPTB;M{CwNUBvVQ>? NYW3PI11OjN4MUS4PVg>
DAOY NX;5fZNvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jPV2lEPTB;M{CwNUBvVQ>? NWr6eG9HOjN4MUS4PVg>
SF-268 NH70dHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoL0TWM2OD1|MECxJI5O NYfKOJMyOjN4MUS4PVg>
SF-295 M{HpeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTNyMEGgcm0> M{XqS|I{PjF2OEm4
SNB-19 NGq4[|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPLOVlFUUN3ME2zNFAyKG6P NIfYZZkzOzZzNEi5PC=>
SNB-75 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTNyMEGgcm0> M2j0ZlI{PjF2OEm4
U373-MG M{TxN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XCPWlEPTB;M{CwNUBvVQ>? NImzUW8zOzZzNEi5PC=>
786-O NU\ie3lyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUW1eWk{UUN3ME2zNFAyKG6P NHjj[ZozOzZzNEi5PC=>
A498 MlzyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPBTWM2OD1|MECxJI5O MkW0NlM3OTR6OUi=
ACHN MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHO[GNkUUN3ME2zNFAyKG6P Mn3uNlM3OTR6OUi=
EKVX NWjjW3U{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWX0cZVUUUN3ME2zNFAyKG6P M121WVI{PjF2OEm4
H226 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHXrbFFKSzVyPUOwNFEhdk1? M1O0VVI{PjF2OEm4
H522 MontS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTNyMEGgcm0> Mmn6NlM3OTR6OUi=
HeLa M2nKZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mof6TWM2OD1|MECxJI5O MmrZNlM3OTR6OUi=
SK-OV-3 MnLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHhVXlKSzVyPUOwNFEhdk1? NEmze2kzOzZzNEi5PC=>
Ln Cap NXzxUoFHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTNyMEGgcm0> MlPMNlM3OTR6OUi=
PC3 NEP2VGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfvTWM2OD1|MECxJI5O M{Dac|I{PjF2OEm4
SNU-16 MoTqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVq1Z4hjUUN3ME2zNFAyKG6P M4fOWlI{PjF2OEm4
FTC-133 NXv3UoZOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\JWGRwUUN3ME2zNFAyKG6P M1;VelI{PjF2OEm4
Ro82-W-1 NH3y[nJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nzVGlEPTB;M{CwNUBvVQ>? M37vS|I{PjF2OEm4
Daudi NInYW3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TLWWlEPTB;M{CwNUBvVQ>? NUfLN2JTOjN4MUS4PVg>
Jijoye MmXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;YTWM2OD1|MECxJI5O Mn7UNlM3OTR6OUi=
Jurkat NIHiNVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHJW5F7UUN3ME2zNFAyKG6P NIG5[3kzOzZzNEi5PC=>
J-82 M1XVd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTNyMEGgcm0> MU[yN|YyPDh7OB?=
TCC-SUP NGXic|VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPDW3pGUUN3ME2zNFAyKG6P NI\kN|gzOzZzNEi5PC=>
BT-474 MoPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3q3RmlEPTB;M{CwNUBvVQ>? MWiyN|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:
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