Nazartinib mesylate

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.

Product Specifications

CAS Number

[1508250-72-3]

Product Name Alternative

EGF816 (mesylate)

UNSPSC

12352005

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-mesylate.html

Solubility

10 mM in DMSO

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

Molecular Formula

C27H35ClN6O5S

Molecular Weight

591.12

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