SCH772984

Catalog No.S7101 Batch:S710105

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Technical Data

Formula

C33H33N9O2
Molecular Weight 587.67 CAS No. 942183-80-4
Solubility (25°C)* In vitro DMSO 14 mg/mL (23.82 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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.
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. This compound inhibits phosphorylation of the ERK substrate p90 ribosomal S6 kinase (T359/S363 phospho-RSK) in a dose-dependent manner. It also inhibits phosphorylation of residues in the activation loop of ERK itself. This inhibitor demonstrates EC50 values <500 nM in approximately 88% and 49% of BRAF-mutant or RAS-mutant tumor lines, respectively. Importantly, it effectively inhibited MAPK signaling and cell proliferation in tumor cells resistant to concurrent treatment with BRAF and MEK inhibitors. [1]
In vivo SCH772984 induces tumor regressions in xenograft models at tolerated doses. This compound effectively inhibites MAPK signaling and cell proliferation in BRAF or MEK inhibitor resistant models. [1]
Features Does not directly inhibit MEK1, MEK2, BRAF, or CRAF enzyme activity.

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 this 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 Assay:

[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 this compound for 4 days and assayed by CellTiterGlo luminescent cell viability assay.
Animal Study:

[1]
  • Animal Models

    Nude mice

  • Dosages

    12.5 mg/kg, 25 mg/kg, 50 mg/kg

  • Administration

    i.p.

References

  • https://pubmed.ncbi.nlm.nih.gov/23614898/

Customer Product Validation

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.

Data from [ Leuk Lymphoma , 2014 , 1, 8 ]

<p>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.</p>

, , Biochem Biophys Res Commun, 2017, 485(4):775-781

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

Data from [ , , Nature, 2016, 534(7609):647-51 ]

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.

Data from [ , , Cell Research, 2015, 25: 561-573 ]

Selleck's SCH772984 Has Been Cited by 684 Publications

Macropinocytosis maintains CAF subtype identity under metabolic stress in pancreatic cancer [ Cancer Cell, 2025, S1535-6108(25)00271-5] PubMed: 40712568
Macrophage-derived amphiregulin induces myofibroblast transition in adipogenic lineage precursors near Staphylococcus aureus abscess in bone marrow [ Nat Commun, 2025, 16(1):8409] PubMed: 40998791
mTORC1 cooperates with tRNA wobble modification to sustain the protein synthesis machinery [ Nat Commun, 2025, 16(1):4201] PubMed: 40328729
Orosomucoid 1 Ameliorates Temporomandibular Joint Osteoarthritis by Maintaining Cartilage Homeostasis [ Adv Sci (Weinh), 2025, 12(36):e00028] PubMed: 40583170
EGFR TKIs suppress MUC1 glycosylation through the PI3K/AKT/SP1/C1GALT1 pathway to enhance TnMUC1 CAR-T efficacy in EGFR-mutant NSCLC [ Cell Rep Med, 2025, S2666-3791(25)00272-1] PubMed: 40562040
Tumorigenesis Driven by BRAFV600E Requires Secondary Mutations that Overcome it's Feedback Inhibition of RAC1 and Migration [ Cancer Res, 2025, 10.1158/0008-5472.CAN-24-2220] PubMed: 39992718
Targeting CLEC4E in immunosuppressive tumour-associated macrophages via BET inhibition [ Clin Transl Med, 2025, 15(10):e70505] PubMed: 41088887
Enhancing CAR-T Cell Metabolic Fitness and Memory Phenotype for Improved Efficacy against Hepatocellular Carcinoma [ Int J Biol Sci, 2025, 21(9):4231-4251] PubMed: 40612678
Opposing roles for GSK3β and ERK1-dependent phosphorylation of huntingtin during neuronal dysfunction and cell death in Huntington's disease [ Cell Death Dis, 2025, 16(1):328] PubMed: 40263294
ERK activation waves coordinate mechanical cell competition leading to collective elimination via extrusion of bacterially infected cells [ Cell Rep, 2025, 44(1):115193] PubMed: 39817903

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.