Epertinib

CAS No. 908305-13-5

Epertinib ( S-222611;S222611 )

Catalog No. M16528 CAS No. 908305-13-5

Epertinib (S-222611) is a novel potent, orally active, reversible EGFR and HER2 inhibitor with IC50 of 1.48, 7.15 and 2.49 nM for EGFR, HER2 and HER4, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Epertinib
  • Note
    Research use only, not for human use.
  • Brief Description
    Epertinib (S-222611) is a novel potent, orally active, reversible EGFR and HER2 inhibitor with IC50 of 1.48, 7.15 and 2.49 nM for EGFR, HER2 and HER4, respectively.
  • Description
    Epertinib (S-222611) is a novel potent, orally active, reversible EGFR and HER2 inhibitor with IC50 of 1.48, 7.15 and 2.49 nM for EGFR, HER2 and HER4, respectively; does not inhibit KDR, IGF1R, SRC, KIT, PDGFRβ; phosphorylation of EGFR and HER2 kinases in NCI-N87 cells with IC50 of 4.5 and 1.6 nM, shows growth inhibition of NCI-N87 cell with IC50 of 8.3 nM; shows potent antitumor activity over lapatinib in a variety of xenograft models, exhibits excellent activity and could be effective against bone and brain metastasis.Breast Cancer Phase 2 Clinical
  • Synonyms
    S-222611;S222611
  • Pathway
    Angiogenesis
  • Target
    EGFR
  • Recptor
    EGFR
  • Research Area
    Cancer
  • Indication
    Breast Cancer

Chemical Information

  • CAS Number
    908305-13-5
  • Formula Weight
    560.03
  • Molecular Formula
    C30H27ClFN5O3
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    CC#C/C(C1=CC2=C(NC3=CC=C(OCC4=CC=CC(F)=C4)C(Cl)=C3)N=CN=C2C=C1)=N\OC[C@@H]5NCCOC5
  • Chemical Name
    (R,Z)-1-(4-((3-chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6-yl)but-2-yn-1-one O-morpholin-3-ylmethyl oxime

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Tanaka H, et al. Cancer Sci. 2014 Aug;105(8):1040-8.
2. Spicer J, et al. Eur J Cancer. 2015 Jan;51(2):137-45.
3. Tanaka Y, et al. Sci Rep. 2018 Jan 10;8(1):343.
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