1. MAPK/ERK Pathway
    Stem Cell/Wnt
  2. ERK

SCH772984 

Cat. No.: HY-50846 Purity: 98.06%
Data Sheet SDS Handling Instructions

SCH772984 potently inhibits ERK1 and ERK2 activity with IC50 values of 4 and 1 nM, respectively.

For research use only. We do not sell to patients.
SCH772984 Chemical Structure

SCH772984 Chemical Structure

CAS No. : 942183-80-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $155 In-stock
5 mg $120 In-stock
10 mg $180 In-stock
50 mg $540 In-stock
100 mg $840 In-stock
200 mg $1400 In-stock
500 mg   Get quote  
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Customer Review

    SCH772984 purchased from MCE. Usage Cited in: Okayama University. 2015.

    The role of Semaphorin4D in bone invasion by oral cancer.

    SCH772984 purchased from MCE. Usage Cited in: Neurotox Res. 2017 Jun 8.

    Lithium promotes autophagy flux by activating MEK/ERK pathway in cells. Original Western blot showing LC3-II and p62 abundance following treatment with lithium in the presence of PD184352 and SCH772984 in neurons. Arithmetic means±SEM (n=5) showing LC3-II abundance following treatment with lithium in the presence of PD184352 and SCH772984 in neurons.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    SCH772984 potently inhibits ERK1 and ERK2 activity with IC50 values of 4 and 1 nM, respectively.

    IC50 & Target

    IC50: 4/1 nM (ERK1/2)[1]

    In Vitro

    SCH772984 shows EC50 values less than 500 nM in approximately 88% and 49% of BRAF-mutant (n=25) or RAS-mutant (n=35) tumor lines, respectively. Flow cytometric analysis of SCH772984-sensitive melanoma cells revealed a G1 arrest as well as an increase in the sub-G1 fraction indicative of apoptosis. Less than 20% of cells wild-type for both RAS and BRAF (n=61) are sensitive to SCH772984[1].

    In Vivo

    Treatment of BRAF-mutant LOX melanoma xenografts with SCH772984 (50 mg/kg twice daily) leads to 98% tumor regression. Dose-dependent antitumor activity is also observed in the KRAS-mutant pancreatic MiaPaCa model, with 36% regression at 50 mg/kg twice daily. Importantly, tumor regression is accompanied by robust inhibition of ERK phosphorylation in tumor tissue. SCH772984 is well tolerated on this schedule as measured by morbidity, lethality, or body weight loss[1].

    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 1.7016 mL 8.5082 mL 17.0164 mL
    5 mM 0.3403 mL 1.7016 mL 3.4033 mL
    10 mM 0.1702 mL 0.8508 mL 1.7016 mL
    Kinase Assay
    [1]

    SCH772984 is tested in 8-point dilution curves in duplicate against purified ERK1 or ERK2. The enzyme is added to the reaction plate and incubated with the compound before adding a solution of substrate peptide and ATP. Fourteen microliters of diluted enzyme (0.3 ng 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 60 μL of IMAP Binding Solution (1:2,200 dilutions of IMAP beads in 1× 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[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    SCH772984 is dissolved in DMSO and stored, and then diluted with appropriate media before use[1].

    Cell proliferation experiments are carried out in a 96-well format (six replicates), and the BRAFV600E-mutant human melanoma cell line LOXIMV1 (LOX) are plated at a density of 4,000 cells per well. At 24 hours after cell seeding, cells are treated with DMSO or a 9-point IC50 dilution (0.001-10 μM) at a final concentration of 1% DMSO for all concentrations. Viability is assayed 5 days after dosing using the ViaLight luminescence kit. For the cell line panel viability assay, cells are treated with SCH772984 for 4 days and assayed by the CellTiterGlo luminescent cell viability assay[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1]

    SCH772984 is dissolved in DMSO and then diluted with PBS or saline[1].

    Mice[1]
    Nude mice are injected subcutaneously with specific cell lines, grown to approximately 100 mm3, randomized to treatment groups (10 mice/group), and treated intraperitoneally with either SCH772984 (12.5, 25, or 50 mg/kg) or vehicle. Tumor length (L), width (W), and height (H) are measured during and after the treatment periods by a caliper twice weekly on each mouse and then used to calculate tumor volume using the formula (L×W×H)/2. Animal body weights are measured on the same days twice weekly. Upon completion of the experiment, vehicle- and SCH772984-treated tumor biopsies are processed for Western blot analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    587.67

    Formula

    C₃₃H₃₃N₉O₂

    CAS No.

    942183-80-4

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: ≥ 51 mg/mL

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Inquiry Information

    Product Name:
    SCH772984
    Cat. No.:
    HY-50846
    Quantity: