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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.
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Application | MWT determination |
| 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). |
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Application | MWT determination |
| 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). |
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Application | QRT-PCR |
| 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. |
| 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 |
| Molecular Weight | 587.67 |
| Formula | C33H33N9O2 |
| CAS Number | 942183-80-4 |
| Solubility (25°C) | DMSO 10 mg/mL (ultrasonic and warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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