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Products Details
Product Description
– Nazartinib mesylate (EGF816 mesylate) is a novel, covalent mutant-selective EGFR inhibitor, with Ki and Kinact of 31 nM and 0.222 min−1 on EGFR(L858R/790M) mutant, respectively.
Web ID
– HY-12872A
Shipping
– Room temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C27H35ClN6O5S
References
– [1]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|[2]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
CAS Number
– 1508250-72-3
Molecular Weight
– 591.12
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.CS(=O)(O)=O
Clinical Information
– Phase 2
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– EGFR
Isoform
– EGFR/ErbB1/HER1
Pathway
– JAK/STAT Signaling;Protein Tyrosine Kinase/RTK
Product type
– Reference compound
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