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Description |
SCH772984 is a novel, specific inhibitor of ERK1/2 with IC50 values of 4 nM and 1 nM in cell-free assay, respectively, And show robust efficacy in RAS- or BRAF-mutant cancer cells. |
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Features |
Does not directly inhibit MEK1, MEK2, BRAF, or CRAF enzyme activity. |
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Targets |
ERK2 [1]
(Cell-free assay) |
ERK1 [1]
(Cell-free assay) |
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1 nM |
4 nM |
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In vitro |
SCH772984 is a novel, selective and ATP competitive inhibitor of ERK1/2. SCH772984 inhibits phosphorylation of the ERK substrate p90 ribosomal S6 kinase (T359/S363 phospho-RSK) in a dose-dependent manner. SCH772984 also inhibits phosphorylation of residues in the activation loop of ERK itself. SCH772984 demonstrates EC50 values <500 nM in approximately 88% and 49% of BRAF-mutant or RAS-mutant tumor lines, respectively. Importantly, SCH772984 effectively inhibited MAPK signaling and cell proliferation in tumor cells resistant to concurrent treatment with BRAF and MEK inhibitors. [1]
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Cell Data |
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Assay |
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Methods |
Test Index |
PMID |
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Western blot |
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26725216 |
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Growth inhibition assay |
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30118499 |
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Immunofluorescence |
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30833752 30213106 |
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In vivo |
SCH772984 induces tumor regressions in xenograft models at tolerated doses. SCH772984 effectively inhibites MAPK signaling and cell proliferation in BRAF or MEK inhibitor resistant models. [1] |
China (Mainland)
