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CO-1686 hydrobromide

CAS No. 1446700-26-0

CO-1686 hydrobromide( Rociletinib hydrobromide | AVL-301 hydrobromide | CNX-419 hydrobromide )

Catalog No. M11900 CAS No. 1446700-26-0

A potent, highly selective, irreversible inhibitor of mutant EGFR with Ki of 21.5 nM for EGFR L858R/T790M.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    CO-1686 hydrobromide
  • Note
    Research use only, not for human use.
  • Brief Description
    A potent, highly selective, irreversible inhibitor of mutant EGFR with Ki of 21.5 nM for EGFR L858R/T790M.
  • Description
    A potent, highly selective, irreversible inhibitor of mutant EGFR with Ki of 21.5 nM for EGFR L858R/T790M; shows 22-fold selective over WT EGFR; EGFR del19, T790M, L858R/T790M and L858R mutant kinases demonstrates the highest degree of inhibition at 0.1 uM; orally bioavailable.Breast Cancer Phase 2 Clinical.
  • In Vitro
    Rociletinib (0.1 μM) inhibits EGFR potently and irreversibly, and inhibits more than 50% of 23 targets. Rociletinib potently and selectively inhibits growth of NSCLC cells expressing mutant EGFR and induces apoptosis. Rociletinib resistant NSCLC cell lines are sensitive to AKT inhibition.
  • In Vivo
    Rociletinib (100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models. Rociletinib (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice.
  • Synonyms
    Rociletinib hydrobromide | AVL-301 hydrobromide | CNX-419 hydrobromide
  • Pathway
    Angiogenesis
  • Target
    EGFR
  • Recptor
    EGFR
  • Research Area
    Cancer
  • Indication
    Breast Cancer

Chemical Information

  • CAS Number
    1446700-26-0
  • Formula Weight
    636.4634
  • Molecular Formula
    C27H29BrF3N7O3
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 59 mg/mL
  • SMILES
    CC(=O)N1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC(=CC=C4)NC(=O)C=C)C(F)(F)F)OC.Br
  • Chemical Name
    2-Propenamide, N-[3-[[2-[[4-(4-acetyl-1-piperazinyl)-2-methoxyphenyl]amino]-5-(trifluoromethyl)-4-pyrimidinyl]amino]phenyl]-, hydrobromide (1:1)

Shipping & Storage Information

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

Reference

1. Walter AO, et al. Cancer Discov. 2013 Dec;3(12):1404-15. 2. Tjin Tham Sjin R, et al. Mol Cancer Ther. 2014 Jun;13(6):1468-79. 3. Sequist LV, et al. N Engl J Med. 2015 Apr 30;372(18):1700-9.
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