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Nazartinib

Product Specifications

Product Name Alternative

EGF816

UNSPSC Description

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.

Target Antigen

EGFR

Type

Reference compound

Related Pathways

JAK/STAT Signaling;Protein Tyrosine Kinase/RTK

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/EGF816.html

Purity

99.03

Solubility

DMSO : ≥ 242 mg/mL

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 Weight

495.02

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)

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-12872/Nazartinib-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-12872/Nazartinib-SDS-MedChemExpress.pdf

Clinical Information

Phase 3

CAS Number

1508250-71-2

Available Sizes

Curated Selection

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