Nazartinib mesylate
Based on 9 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 1508250-72-3
- Formula: C27H35ClN6O5S
- Molecular Weight:591.12
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Nazartinib mesylate
More- Cancer Res. 2021 Sep 15;81(18):4822-4834. [Abstract]
- Cancer Lett. 2021 Oct 28:519:141-149. [Abstract]
- R Soc Open Sci. 2020 Jan 15;7(1):191595. [Abstract]
- R Soc Open Sci. 2019 Aug 14;6(8):190852. [Abstract]
- Patent. US20250312348A1.
- Patent. US20220177473A1.
- Patent. US20220175778A1.
- Patent. US20210361655A1.
- Patent. US20190160066A1
All EGFR Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
EGFRL858R/T790M 31 nM (Ki) |
In Vitro
Nazartinib (EGF816) has inhibitory effect on the mutant cell lines with IC50s of 4, 6, 2 nM in H1975, H3255, and HCC827, respectively, and demonstrates improved ADME and PK properties[1]. Nazartinib (EGF816) shows potent inhibition of pEGFR levels in H3255, HCC827, and H1975 cell lines with EC50 values of 5, 1, and 3 nM, respectively. Nazartinib inhibits cell proliferation, with EC50 values of 9, 11, and 25 nM in H3255, HCC827, and H1975, respectively. Nazartinib has an OC50 (compound concentration at 50% occupancy) value of 2 and 5 nM on HCC827 and H1975, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1508250-72-3
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Molecular Weight 591.12
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Formula C27H35ClN6O5S
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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
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Synonyms
EGF816 mesylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (9)
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Journal Impact Factor
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Most Recent
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Cancer Res
Targeting c-Myc to Overcome Acquired Resistance of EGFR Mutant NSCLC Cells to the Third-Generation EGFR Tyrosine Kinase Inhibitor, Osimertinib. [Abstract]2021 Sep 15;81(18):4822-4834. PMID: 34289988 -
Cancer Lett
Inhibition of MEK5/ERK5 signaling overcomes acquired resistance to the third generation EGFR inhibitor, osimertinib, via enhancing Bim-dependent apoptosis. [Abstract]2021 Oct 28:519:141-149. PMID: 34245854 -
R Soc Open Sci
Spectroscopic and molecular docking studies reveal binding characteristics of nazartinib (EGF816) to human serum albumin. [Abstract]2020 Jan 15;7(1):191595. PMID: 32218978 -
R Soc Open Sci
Liquid chromatography-tandem mass spectrometry metabolic profiling of nazartinib reveals the formation of unexpected reactive metabolites. [Abstract]2019 Aug 14;6(8):190852. PMID: 31598253 -
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Purity & Documentation
References
[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 [Content Brief]
[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 [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Nazartinib mesylate Related Classifications
HY-12872A Related Classifications
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