Nazartinib
Nazartinib (EGF816) is a covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min 1 on EGFR (L858R/790M) mutant, respectively.
Product Specifications
CAS Number
[1508250-71-2]
Product Name Alternative
EGF816
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
EGFR
Type
Reference compound
Related Pathways
JAK/STAT Signaling; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/EGF816.html
Purity
99.53
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C(C1=CC(C)=NC=C1)NC2=NC3=CC=CC(Cl)=C3N2[C@H]4CN(C(/C=C/CN(C)C)=O)CCCC4
Molecular Formula
C26H31ClN6O2
Molecular Weight
495.02
Precautions
H302, H315, H319, H335
References & Citations
[1]Lelais G, 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 (T79|[2]Jia Y, et al. EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor. Cancer Res. 2016 Mar 15;76 (6) :1591-602
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Isoform
EGFR/ErbB1/HER1
Available Sizes
Curated Selection
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