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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4 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.

    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 NEn0XGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWHCb|ZiUUN3ME2wMlI1KG6P NHj4[GMzPTN3MEmzNS=>
WM-266-4 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfWUVM1UUN3ME2yNEBvVQ>? MW[yN|YyPDh7OB?=
UACC-62 NUjzZ21jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPXdVFuUUN3ME2zNEBvVQ>? NVXuXo94OjN4MUS4PVg>
Colo-205 NGDsRm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLWRo9PUUN3ME2zOkBvVQ>? NELwU2ozOzZzNEi5PC=>
SK-Mel-1 MnjSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3z5WGlEPTB;M{egcm0> Mm\uNlM3OTR6OUi=
WiDr MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HBRmlEPTB;M{mgcm0> NXjUUXk{OjN4MUS4PVg>
M14 MlT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYi4boNSUUN3ME20O{BvVQ>? NVjOZZZiOjN4MUS4PVg>
HT-29 MmnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHIfZlLUUN3ME21NEBvVQ>? MkHtNlM3OTR6OUi=
8505C NWXSOGd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPE[IZKSzVyPUWwJI5O NF\tOWkzOzZzNEi5PC=>
HT-144 Ml;SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jKSmlEPTB;NkCgcm0> MkX6NlM3OTR6OUi=
SK-Mel-5 MnvoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLXZnpKSzVyPU[2JI5O M3PrclI{PjF2OEm4
A375-SM NX\aTms6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvHZWtbUUN3ME23OUBvVQ>? MVGyN|YyPDh7OB?=
SK-Mel-28 M2\pTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlvOTWM2OD16NTDuUS=> M3zUZVI{PjF2OEm4
LOX NVPycY4xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\lTWlEPTB;MUCwJI5O MWmyN|YyPDh7OB?=
SK-Mel-3 NVP4SZBCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rZbmlEPTB;MUG4JI5O NYrCeGFJOjN4MUS4PVg>
K1 M3jPZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;TTWM2OD1zM{Cgcm0> M2jOVVI{PjF2OEm4
Hs-695T M2r5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLTTWM2OD1zNkWgcm0> M{CzcFI{PjF2OEm4
BHT-101 NGi2WolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTNyMDDuUS=> NH7SPW8zOzZzNEi5PC=>
RPMI-7951 M3rMU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXGO3lKSzVyPUO0OEBvVQ>? MlK4NlM3OTR6OUi=
A2058 NUP2NGd[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NETSe5dKSzVyPUO2NEBvVQ>? M2f0PVI{PjF2OEm4
SK-Hep-1 MmnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGTXdG9KSzVyPUG0NlIhdk1? M3ixSFI{PjF2OEm4
A673 NF[2O4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4j2[WlEPTB;M{CwNUBvVQ>? MYSyN|YyPDh7OB?=
DBTRG-05MG MnjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGjiR4JKSzVyPUOwNFEhdk1? MmfuNlM3OTR6OUi=
SW-626 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTN|IH7N NVX4SXRoOjN4MUS4PVg>
LoVo M3LoOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTR5IH7N NFr0RW0zOzZzNEi5PC=>
MiaPaCa MmGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTV|IH7N NIi1[HIzOzZzNEi5PC=>
SW-620 NEfzOnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoH4TWM2OD1zMESgcm0> MkfNNlM3OTR6OUi=
CAPAN-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfQTWM2OD1zMESgcm0> NEPwVo4zOzZzNEi5PC=>
SW-527 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fjdGlEPTB;MUKxJI5O M1rCNFI{PjF2OEm4
HCT-116 M13iV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULFWXp3UUN3ME2xNlghdk1? NFrpV5QzOzZzNEi5PC=>
SW-480 NY\ZRZM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnq2TWM2OD1zNkWgcm0> NIDOd2kzOzZzNEi5PC=>
HPAC M3TscWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVX3bohvUUN3ME2xO|Ahdk1? M1nJS|I{PjF2OEm4
OVCAR-5 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HufmlEPTB;MkC4JI5O NGnTe5AzOzZzNEi5PC=>
AsPc-1 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NE\Ge|VKSzVyPUK3NEBvVQ>? MmTzNlM3OTR6OUi=
A549 M4rY[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fzWGlEPTB;M{K2JI5O MojpNlM3OTR6OUi=
SNU-1 Ml[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTvVI1SUUN3ME2zOVQhdk1? MmfrNlM3OTR6OUi=
HOP62 M2j1eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTZ5NjDuUS=> NUXVbo53OjN4MUS4PVg>
H23 M3r2W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TSNmlEPTB;MUCwNEBvVQ>? NX34fmdpOjN4MUS4PVg>
MB-231 M1frfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTFyMECgcm0> NIHr[mkzOzZzNEi5PC=>
SU.86.86 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTHTWM2OD1zMECxJI5O MW[yN|YyPDh7OB?=
CFPAC-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{SxO2lEPTB;MUCwNUBvVQ>? NFHzUowzOzZzNEi5PC=>
A427 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTXe5VKSzVyPUG0N|Mhdk1? NXHuXIl1OjN4MUS4PVg>
MDAH-2774 M{f2TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn:xTWM2OD1{NkW3JI5O NGDScVczOzZzNEi5PC=>
NCI-H157 NUfsVJpxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTNyMECgcm0> MXSyN|YyPDh7OB?=
HTB-177 NYnObIpyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTNyMECgcm0> Mn3qNlM3OTR6OUi=
UM-UC-3 M4XTR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LkRmlEPTB;M{CwNUBvVQ>? NGm4NJozOzZzNEi5PC=>
HCT-8 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTNyMEGgcm0> Ml7rNlM3OTR6OUi=
Panc-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjlTWM2OD1|MECxJI5O M2S0O|I{PjF2OEm4
DLD-1 MnzjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTNyMEGgcm0> NF;iPGwzOzZzNEi5PC=>
HCT-15 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWPFOlB1UUN3ME2zNFAyKG6P NF3sTGMzOzZzNEi5PC=>
HL-60 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHHTWM2OD1|MDDuUS=> NX3pZZEzOjN4MUS4PVg>
SK-Mel-2 MnPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTUTWM2OD1|NDDuUS=> NYnpS21TOjN4MUS4PVg>
RD NWm3U3dtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LKNmlEPTB;MUKzJI5O MkjzNlM3OTR6OUi=
HT-1197 M3XXXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLMTWM2OD1|MU[gcm0> NVrWNoVkOjN4MUS4PVg>
Molt-3 Mlr1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTZyMDDuUS=> NX7WW3BVOjN4MUS4PVg>
PA-1 NXnK[5ZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLQPI9KSzVyPUGwNFEhdk1? MWWyN|YyPDh7OB?=
Molt-4 MmT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDGSIQ5UUN3ME2zNFAyKG6P NFnBS|gzOzZzNEi5PC=>
NCI-H292 NFvyeHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEH2U|hKSzVyPUmwJI5O NEX5VWszOzZzNEi5PC=>
A2780 M2fz[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTF2MzDuUS=> NWW4dYJTOjN4MUS4PVg>
IGROV-1 NFKwcY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2L3U2lEPTB;MUS2JI5O MV:yN|YyPDh7OB?=
SK-N-SH NXT4RWplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYH6d4tIUUN3ME2xOVAhdk1? M3nxNFI{PjF2OEm4
N-87 MlfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGOzVllKSzVyPUOwO{BvVQ>? MYSyN|YyPDh7OB?=
H322 MnvOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTGTWM2OD1|MkWgcm0> M{e3flI{PjF2OEm4
H716 NGPxNJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoiyTWM2OD1|M{Sgcm0> NF3QUpkzOzZzNEi5PC=>
TT MljrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrJZWd7UUN3ME20NFYhdk1? NVvsUVZEOjN4MUS4PVg>
Caki-1 MkfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTR3MDDuUS=> NVLEU29MOjN4MUS4PVg>
5637 M2\jV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2TKRmlEPTB;NkGwJI5O M1nCeFI{PjF2OEm4
MB-453 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPVclRuUUN3ME22O|Ihdk1? MkWxNlM3OTR6OUi=
RT-4 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLYclBkUUN3ME24NVAhdk1? M2XRUVI{PjF2OEm4
HOP92 M13mWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXO1NVNRUUN3ME24NlAhdk1? NIHMb2EzOzZzNEi5PC=>
KG-1 NWPteohCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{KzNGlEPTB;OUCwJI5O MmfoNlM3OTR6OUi=
Hs-294T MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIfhb|FKSzVyPUm0OUBvVQ>? NHnpXHIzOzZzNEi5PC=>
SF-539 Mn76S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTFyMECgcm0> NXLnRWtJOjN4MUS4PVg>
U-251 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH71W|hKSzVyPUGwNFAhdk1? MlXENlM3OTR6OUi=
MB-468 NF;WepdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTFyMECgcm0> MXGyN|YyPDh7OB?=
HS746T MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HMSmlEPTB;MUCwNEBvVQ>? MnXkNlM3OTR6OUi=
SCABER NHf1PJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnkZ5hoUUN3ME2xNFAxKG6P MXqyN|YyPDh7OB?=
MCF-7 NI\ONVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkL6TWM2OD1zMECxJI5O MnXRNlM3OTR6OUi=
CHL-1 MnixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTF2NkCgcm0> M1fJbVI{PjF2OEm4
U87MG M{C2dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\qTWM2OD1{MECwJI5O NV\2WIxlOjN4MUS4PVg>
SJCRH30 NUPYNYJXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTJyMEKgcm0> MlT5NlM3OTR6OUi=
ES-2 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrCU4tKSzVyPUK2OVkhdk1? MXKyN|YyPDh7OB?=
HT-1376 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1rVWGlEPTB;MkiwNEBvVQ>? NVXvVIZtOjN4MUS4PVg>
A172 NWXyeoNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2flTWlEPTB;M{CwNEBvVQ>? NV\VdmRuOjN4MUS4PVg>
769P MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTNyMECgcm0> M2fWNVI{PjF2OEm4
NCI-H520 NYDoR5U2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVH6e5VSUUN3ME2zNFAxKG6P Mlm3NlM3OTR6OUi=
DU145 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\jcXRKSzVyPUOwNFAhdk1? Mn32NlM3OTR6OUi=
K562 M1HWc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fOeGlEPTB;M{CwNEBvVQ>? MVWyN|YyPDh7OB?=
U-937 NGH2ZpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTNyMECgcm0> NIrHU4ozOzZzNEi5PC=>
A204 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnDTWM2OD1|MECxJI5O NFLT[pIzOzZzNEi5PC=>
DAOY M4HOTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HYVGlEPTB;M{CwNUBvVQ>? M1e2UFI{PjF2OEm4
SF-268 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrSc|RKSzVyPUOwNFEhdk1? MmHFNlM3OTR6OUi=
SF-295 M2O0NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLTbmVKSzVyPUOwNFEhdk1? NYr3W|dEOjN4MUS4PVg>
SNB-19 M3XS[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTNyMEGgcm0> MUeyN|YyPDh7OB?=
SNB-75 NFjITGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWPrNldHUUN3ME2zNFAyKG6P NHHFTJkzOzZzNEi5PC=>
U373-MG MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknaTWM2OD1|MECxJI5O M2CyRVI{PjF2OEm4
786-O NF;wRXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\aRVcyUUN3ME2zNFAyKG6P NWD6WXpDOjN4MUS4PVg>
A498 MnzkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTsTWM2OD1|MECxJI5O NF76R|UzOzZzNEi5PC=>
ACHN NYLyWVJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHHTWM2OD1|MECxJI5O NYS1N4FZOjN4MUS4PVg>
EKVX M4XvZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXrTWM2OD1|MECxJI5O NWjnUpBVOjN4MUS4PVg>
H226 MmPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTNyMEGgcm0> M4LXfVI{PjF2OEm4
H522 NEC5c3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfB[lVVUUN3ME2zNFAyKG6P Mn7aNlM3OTR6OUi=
HeLa M2DiOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHLTUndKSzVyPUOwNFEhdk1? MonGNlM3OTR6OUi=
SK-OV-3 NEn5TlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;mfmNKSzVyPUOwNFEhdk1? NVPhd3ZOOjN4MUS4PVg>
Ln Cap MlLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTNyMEGgcm0> MnXkNlM3OTR6OUi=
PC3 M4DvXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnPfW12UUN3ME2zNFAyKG6P NHTlOI0zOzZzNEi5PC=>
SNU-16 NHH1R5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzF[WtwUUN3ME2zNFAyKG6P MVGyN|YyPDh7OB?=
FTC-133 MmTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTNyMEGgcm0> M{PuUlI{PjF2OEm4
Ro82-W-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4H3fGlEPTB;M{CwNUBvVQ>? M374clI{PjF2OEm4
Daudi NYXwXoJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvXOlN7UUN3ME2zNFAyKG6P NWG2fmsxOjN4MUS4PVg>
Jijoye MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGjMcWtKSzVyPUOwNFEhdk1? MnXuNlM3OTR6OUi=
Jurkat M3zreWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXTWcnZpUUN3ME2zNFAyKG6P M4TlOVI{PjF2OEm4
J-82 NVfxcpNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVrQNJdiUUN3ME2zNFAyKG6P MlPwNlM3OTR6OUi=
TCC-SUP M2fkcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWq3W2xoUUN3ME2zNFAyKG6P MW[yN|YyPDh7OB?=
BT-474 MonyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjhRoxiUUN3ME2zNFAyKG6P NYT2XW11OjN4MUS4PVg>
ZR-75-1 NU\GOXgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPqPZJuUUN3ME2zNFAyKG6P MnnTNlM3OTR6OUi=

... 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
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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