SCH772984

Catalog No.S7101

For research use only.

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.

SCH772984 Chemical Structure

CAS No. 942183-80-4

Selleck's SCH772984 has been cited by 437 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 NUnu[nJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mkf3TWM2OD1yLkK0JI5O Mn3TQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV|NUC5N|EoRjJ3M{WwPVMyRC:jPh?=
WM-266-4 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGf3fZVKSzVyPUKwJI5O NHTNPVU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
UACC-62 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\UTWM2OD1|MDDuUS=> NX2yeGFSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
Colo-205 NIL6ZmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTN4IH7N NWLY[WxJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
SK-Mel-1 NUK4W5lyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlz3TWM2OD1|NzDuUS=> NF:4N2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
WiDr NFrKXoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVy1[plVUUN3ME2zPUBvVQ>? MnvKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
M14 MoW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfRWFViUUN3ME20O{BvVQ>? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
HT-29 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fDfGlEPTB;NUCgcm0> NFXhWoo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
8505C NFeybZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\rfmlEPTB;NUCgcm0> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
HT-144 MkDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPPTWM2OD14MDDuUS=> NFHtZZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
SK-Mel-5 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDGNnA{UUN3ME22OkBvVQ>? MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
A375-SM MlPPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1fxbmlEPTB;N{Wgcm0> NFXJR489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
SK-Mel-28 M3vMN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnoSWhKSzVyPUi1JI5O NXPISZNGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
LOX NUHlPZdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnpTWM2OD1zMECgcm0> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
SK-Mel-3 M{S1Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfqRVJKSzVyPUGxPEBvVQ>? MmPsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
K1 NGezclNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4To[WlEPTB;MUOwJI5O MkfuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
Hs-695T Mmm2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTF4NTDuUS=> MlfhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
BHT-101 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\JVGlEPTB;M{CwJI5O M1PzTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
RPMI-7951 NGX2[JdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zhVmlEPTB;M{S0JI5O M3vrRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
A2058 Ml;wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{GzTmlEPTB;M{[wJI5O MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
SK-Hep-1 MnW4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTMZW5KSzVyPUG0NlIhdk1? NEXYR249[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
A673 NEjiXnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF7pTXVKSzVyPUOwNFEhdk1? NFjx[XY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
DBTRG-05MG NIHPdI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPwTWM2OD1|MECxJI5O M33W[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
SW-626 MlHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTR[lluUUN3ME2zN{BvVQ>? NUCwZnNQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
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MiaPaCa MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTV|IH7N MmDLQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
SW-620 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\6TWM2OD1zMESgcm0> NYPte2kzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2NVQ5QThpPkKzOlE1QDl6PD;hQi=>
CAPAN-1 M3u1N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXkTWM2OD1zMESgcm0> M4jCXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
SW-527 M4HFOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjyRmQyUUN3ME2xNlEhdk1? MlSxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
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SW-480 M1PSbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXO1fpE{UUN3ME2xOlUhdk1? MonUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4MUS4PVgoRjJ|NkG0PFk5RC:jPh?=
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SNU-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2SxVmlEPTB;M{W0JI5O MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
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H23 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXL3OVRrUUN3ME2xNFAxKG6P M1\YfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
MB-231 NGTm[YFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTFyMECgcm0> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
SU.86.86 MlnYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnrYTWM2OD1zMECxJI5O MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
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MDAH-2774 NFrsRnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnKyTWM2OD1{NkW3JI5O NFyyRZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
NCI-H157 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fHfWlEPTB;M{CwNEBvVQ>? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZzNEi5PEc,OjN4MUS4PVg9N2F-
HTB-177 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mon1TWM2OD1|MECwJI5O M{W3PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
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HCT-8 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLZ[5JiUUN3ME2zNFAyKG6P M4XtTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
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HT-1197 NV7IbHBGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4fsdWlEPTB;M{G2JI5O NH3YXYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[xOFg6QCd-MkO2NVQ5QTh:L3G+
Molt-3 MkTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\GUIRPUUN3ME22NFAhdk1? M1\DOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|NkG0PFk5Lz5{M{[xOFg6QDxxYU6=
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Assay
Methods Test Index PMID
Western blot cyclin B1 / cyclin D1 / p21 ; pRSK / pERK / pAKT / pMEK ; DUSP1 / DUSP4 / DUSP6 ; pCRAF(S338, S289, S296, S301) ; Aurora B / ETS1 / ETS2 26725216
Growth inhibition assay Cell viability 30118499
Immunofluorescence TOMM20 ; pERK1/2 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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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.

Animal Research:

[1]

  • Animal Models: Nude mice
  • Dosages: 12.5 mg/kg, 25 mg/kg, 50 mg/kg
  • Administration: i.p.

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

Chemical Information

Molecular Weight 587.67
Formula

C33H33N9O2

CAS No. 942183-80-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CC1C(=O)NC2=CC3=C(C=C2)NN=C3C4=CC=NC=C4)CC(=O)N5CCN(CC5)C6=CC=C(C=C6)C7=NC=CC=N7

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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
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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

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