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SCH772984

Cat. No. M2084
SCH772984 Structure
Size Price Availability Quantity
5mg USD 150 In stock
10mg USD 200 In stock
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Quality Control
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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 587.67
Formula C33H33N9O2
CAS Number 942183-80-4
Purity 100.00%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
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).
Rating
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).
Rating
Product Citations
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: SCH772984 supplier, ERK, inhibitors

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