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.
J Neurosci 2018 Mar 26.
HIPK2-mediated transcriptional control of NMDA receptor subunit expression regulates neuronal survival and cell death
SCH772984 purchased from AbMole
Saudi Pharmaceutical Journal. 2016 May;24(3):354-62.
Analgesic effect and possible mechanism of SCH772984 intrathecal injection on rats with bone cancer pain.
SCH772984 purchased from AbMole
Cell Experiment | |
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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 | |
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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 |
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
Molecular Weight | 587.67 |
Formula | C33H33N9O2 |
CAS Number | 942183-80-4 |
Purity | 100.00% |
Solubility | DMSO |
Storage | at -20°C |
Discovery of a Novel ERK Inhibitor with Activity in Models of Acquired Resistance to BRAF and MEK Inhibitors.
Morris EJ, et al. Cancer Discov. 2013 Jul;3(7):742-50. PMID: 23614898.
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