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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