SCH772984

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0 Metric Ton	Negotiable

0 Metric Ton

Negotiable

Min.Order :0 Metric Ton
Purity: >97%

Keywords

SCH772984 ERK inhibitor 942183-80-4

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Biological Activity

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.

Features

Does not directly inhibit MEK1, MEK2, BRAF, or CRAF enzyme activity.

Targets

ERK2 [1] (Cell-free assay)	ERK1 [1] (Cell-free assay)
1 nM	4 nM

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]

Cell Data

Cell Lines	Assay Type	Activity Description	PMID
2P-ERK2	Growth Inhibition Assay	IC50=0.24 nM	25350931
WM-266-4	Growth Inhibition Assay	IC50=20 nM	23614898
UACC-62	Growth Inhibition Assay	IC50=30 nM	23614898

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	cyclin B1 / cyclin D1 / p21; pRSK / pERK / pAKT / pMEK; DUSP1 / DUSP4 / DUSP6; pCRAF(S338, S289, S296, S301); Aurora B / ETS1 / ETS2;	26725216
Growth inhibition assay	Cell viability;	30118499
Immunofluorescence	TOMM20; pERK1/2;	30833752 30213106

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]

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