• Product NameEGF816
• Brief DescriptionInhibitors
• Purification98.00%
• Biological ActivityNazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex19del) and T790M mt, with up to 60-fold selectivity over wild type (wt) EGFR in vitro.
• Target NameEGFR inhibitor
• CAS No. 1508250-71-2
• Calculated MW 495.02
• Formulation C26H31ClN6O2
• Storage 3 years -20˚C powder;2 years -80˚C in solvent;

• Research Area:Others
  SMILES:CC1=NC=CC(=C1)C(=O)NC2=NC3=C(N2[C@@H]4CCCCN(C4)C(=O)/C=C/CN(C)C)C(=CC=C3)Cl
  Pathways:Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
  Receptor:EGFR (mutant)
  Boling pt:
  Melting pt:
  Solubility:DMSO: 99 mg/mL (199.99 mM); Ethanol: 99 mg/mL (199.99 mM)
  Appearance:
  Remark:For obtaining a higher solubility , please warm the tube at 37 ˚C and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20 ˚C for several month.

1. Grald Lelais, et al Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers. J. Med. Chem., 2016, 59 (14), pp 6671C6689

• Flow Cytometry (FCM) General Protocol
• Immunofluorescence(IC)
• Immunohistochemistry(Polymer)
• Western Blotting