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SCH772984

Cat. No. M2084
SCH772984 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 150  USD150 In stock
2mg USD 80  USD80 In stock
5mg USD 120  USD120 In stock
10mg USD 180  USD180 In stock
50mg USD 480  USD480 In stock
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Quality Control & Documentation
Biological Activity

SCH772984 is a novel and selective inhibitor of ERK1/2 that displays behaviors of both type I and type II kinase inhibitors. SCH772984 has nanomolar cellular potency in tumor cells with mutations in BRAF, NRAS, or KRAS. SCH772984 effectively inhibited MAPK signaling and cell proliferation in BRAF or MEK inhibitor-resistant models as well as in tumor cells resistant to concurrent treatment with BRAF and MEK inhibitors. SCH772984 induces tumor regressions in xenograft models at tolerated doses.

Product Citations
Customer Product Validations & Biological Datas
Source J Neurosci (2018). Figure 7. SCH772984 (Abmole Bioscience)
Method QRT-PCR
Cell Lines Primary cortical neurons
Concentrations 5 nM, 50 nM
Incubation Time 4 h
Results These results suggested that in addition to the increase in GluN2A protein levels in the synaptosomes and mitochondria, additional unknown mechanism(s), which could up-regulate the ERK-CREB signaling, might also contribute to the resistance of Hipk2-/- DA neurons to CCCP.
Source Saudi Pharmaceutical Journal (2016) . Figure 2.SCH772984, produced by AbMole
Method MWT determination
Cell Lines
Concentrations 0, 0.1, 1, 10μg
Incubation Time 3, 6, 9, 12, 15, 18 and 24 hr
Results Comparing model group with Sham group and intrathecal tube group, MWT shows no significant differences at different time (p>0.05); comparing model group with BCP group and intrathecal tube +BCP group, MWT shows significant differences at different time (p<0.05); comparing model group with BCP group, MWT shows significant differences (p<0.05); comparing BCP group and intrathecal tube +BCP group, MWT shows no significant differences (p>0.05).
Source Saudi Pharmaceutical Journal (2016) . Figure 1.SCH772984, produced by AbMole
Method MWT determination
Cell Lines
Concentrations 0, 0.1, 1, 10μg
Incubation Time 3, 6, 9, 12, 15, 18 and 24 hr
Results Comparing model group with Sham group and intrathecal tube group, MWT shows no significant differences at different time (p>0.05); comparing model group with BCP group and intrathecal tube +BCP group, MWT shows significant differences at different time (p<0.05); comparing model group with BCP group, MWT shows significant differences (p<0.05); comparing BCP group and intrathecal tube +BCP group, MWT shows no significant differences (p>0.05).
Protocol (for reference only)
Cell Experiment
Cell lines BRAF- or RAS-mutant tumor cells
Preparation method Cell proliferation experiments were carried out in a 96-well format (six replicates), and cells were plated at a density of 4,000 cells per well. At 24 hours after cell seeding, cells were treated with DMSO or a 9-point IC50 dilution (0.001–10 μmol/L) at a final concentration of 1% DMSO for all concentrations. Viability was assayed 5 days after dosing using the ViaLight luminescence kit (Lonza) following the manufacturer's recommendations (n = 6, mean ± SE). For the cell line panel viability assay, cells were treated with SCH772984 for 4 days and assayed by the CellTiterGlo luminescent cell viability assay (Promega).
Concentrations 0.001–10 μmol/L
Incubation time 4 days
Animal Experiment
Animal models Female nude mice bearing human LOX BRAF-mutant/MiaPaCa KRAS-mutant pancreatic/ melanoma xenograft model
Formulation normal saline
Dosages 12.5, 25, or 50 mg/kg for 14 days
Administration intraperitoneally
Chemical Information
Molecular Weight 587.67
Formula C33H33N9O2
CAS Number 942183-80-4
Solubility (25°C) DMSO 12 mg/mL warming
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Morris EJ, et al. Cancer Discov. Discovery of a Novel ERK Inhibitor with Activity in Models of Acquired Resistance to BRAF and MEK Inhibitors.

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  Catalog
Abmole Inhibitor Catalog




Keywords: SCH772984 supplier, ERK, inhibitors, activators


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