EGF816 mesylate

CAS No. 1508250-72-3

EGF816 mesylate ( EGF-816 mesylate;Nazartinib mesylate )

Catalog No. M12106 CAS No. 1508250-72-3

EGF816 (Nazartinib) is a potent, irreversible, mutant-selective EGFR inhibitor with Ki and Kinact of 31 nM and 0.222 min-1, respectively.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    EGF816 mesylate
  • Note
    Research use only, not for human use.
  • Brief Description
    EGF816 (Nazartinib) is a potent, irreversible, mutant-selective EGFR inhibitor with Ki and Kinact of 31 nM and 0.222 min-1, respectively.
  • Description
    EGF816 (Nazartinib) is a potent, irreversible, mutant-selective EGFR inhibitor with Ki and Kinact of 31 nM and 0.222 min-1, respectively; shows potent inhibition of pEGFR levels in H3255, HCC827, and H1975 with EC50 of 5, 1, and 3 nM, which harbor the L858R, Ex19del, and L858R/T790M mutations, respectively, inhibitscell proliferation with EC50 of 9, 11, and 25 nM, but not the WT EGFR-containing patient-derived cell lines; potently inhibits the most common EGFR mutations L858R, Ex19del, and T790M in vitro; causes tumor regressions in vivo in several patient-derived xenograft models, also demonstrates antitumor activity in exon 20 insertion mutant model.Lung Cancer Phase 3 Clinical
  • Synonyms
    EGF-816 mesylate;Nazartinib mesylate
  • Pathway
    Angiogenesis
  • Target
    EGFR
  • Recptor
    EGFR
  • Research Area
    Cancer
  • Indication
    Lung Cancer

Chemical Information

  • CAS Number
    1508250-72-3
  • Formula Weight
    591.12
  • Molecular Formula
    C27H35ClN6O5S
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • SMILES
    CC1=NC=CC(=C1)C(=O)NC2=NC3=C(N2C4CCCCN(C4)C(=O)C=CCN(C)C)C(=CC=C3)Cl.CS(=O)(=O)O
  • Chemical Name
    4-Pyridinecarboxamide, N-[7-chloro-1-[(3R)-1-[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]hexahydro-1H-azepin-3-yl]-1H-benzimidazol-2-yl]-2-methyl-, methanesulfonate (1:1)

Shipping & Storage Information

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

Reference

1. Lelais G, et al. J Med Chem. 2016 Jul 28;59(14):6671-89.
2. Jia Y, et al. Cancer Res. 2016 Mar 15;76(6):1591-602.
3. Liao BC, et al. Lung Cancer. 2017 Aug;110:7-13.
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