Name: SCH772984 HCl
Price: 554.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    SCH772984 HCl is a specific inhibitor of extracellular signal-regulated kinase 1/2 (ERK1/2), with IC50 values of 4 nM and 1 nM, respectively [1].
    ERK1/2 is a mitogen-activated protein kinase (MAPK) which is involved in the development of various cancers, especially the ones with BRAF or RAS mutations. Phospho-ERK reactivation in cancer cells is associated with resistance to BRAF and MEK inhibitors [1].
    In BRAFV600E-mutant human melanoma cell line LOXIMV1 (LOX), SCH772984 at 0 ~ 300 nM inhibited phosphorylation of the ERK substrate p90 ribosomal S6 kinase in a dose-dependent manner. SCH772984 also reduced phosphorylation of residues in the activation loop of ERK itself. In addition, for approximately 88% and 49% of BRAF-mutant or RAS-mutant tumor lines, SCH772984 exhibited antiproliferative activity with EC50 values < 500 nM. SCH772984 effectively inhibited MAPK signaling and cell proliferation even in tumor cells resistant to concurrent treatment with BRAF and MAP-ERK kinase (MEK) inhibitors [1].
    In female nude mice bearing human LOX BRAFV600E tumors, SCH772984 (12.5, 25, 50 mg/kg, i.p., b.i.d., for 14 days) induced tumor regressions in a dose-dependent manner, and 98% tumor regression was achieved at the largest dose [1].
- Properties
  - CAS Number
    
    942183-80-4 (free base)
    
    Molecular Formula
    
    C33H34ClN9O2
    
    Molecular Weight
    
    624.17
    
    Appearance
    
    A solid
    
    Purity
    
    98.17%
    
    Solubility
    
    ≥23.5 mg/mL in H2O with gentle warming; insoluble in EtOH; ≥16.27 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

We Also Recommend

ELR510444

$289

MK3102

$378

SCH772984 TFA

$280

SCH772984 HCl

SCH772984 HCl

Background

We Also Recommend

ELR510444

ELR510444

MK3102

SCH772984 TFA