Art. -Nr.: HY-12872

Nazartinib

Name: Nazartinib
Brand: MedChemExpress
SKU: HY-12872
Price: 90.00 USD
Availability: InStock
Rating: 5 (9 reviews)

(Synonyms: EGF816)

9 Cited Publications

Kundenbewertung

Based on 9 publication(s) in Google Scholar

Nazartinib (EGF816) is a covalent mutant-selective EGFR inhibitor, with K_i and K_inact of 31 nM and 0.222 min⁻¹ on EGFR(L858R/790M) mutant, respectively.

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Reinheit : 99.53%
CAS. Nr.: 1508250-71-2
Formel: C₂₆H₃₁ClN₆O₂
Molecular Weight:495.02

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 2 years , -20°C, 1 year

Nazartinib Chemical Structure

CAS. Nr.: 1508250-71-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (9)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Nazartinib (EGF816) is a covalent mutant-selective EGFR inhibitor, with K_i and K_inact of 31 nM and 0.222 min⁻¹ on EGFR(L858R/790M) mutant, respectively.

IC₅₀ & Target

^[1]

EGFR^L858R/T790M

31 nM (Ki)

Alle EGFR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HaCaT	IC₅₀	160.6 nM Compound: 47; EGF816	Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method	[PMID: 27433829]
NCI-H1975	IC₅₀	25 nM Compound: EGF816	Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as suppression of cell proliferation Inhibition of EGFR L858R/T790M double mutant in human NCI-H1975 cells assessed as suppression of cell proliferation	[PMID: 26968253]

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

In H1975 mouse xenograft model, Nazartinib (EGF816; 50 and 20 mg/kg or 25 mg/kg, p.o.) demonstrates dose-dependent efficacy with near complete tumor cells regression at the highest dose tested (50 mg/kg)^[1]. In H1975 mouse model, Nazartinib (EGF816; 10 mg/kg, p.o.) induces tumor growth inhibition with a T/C (tumor/control volume) of 29%, and when doses are 30 and 100 mg/kg, tumor regressions are achieved (T/C, -61% and -80%, respectively). In the H3255 xenograft model, Nazartinib (30 mg/kg, p.o.) shows significant antitumor activity. Antiproliferative activity of Nazartinib on 89 lung cancer cell lines indicates that Nazartinib selectively inhibits cell lines containing EGFR with catalytic domain mutations^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1508250-71-2
Appearance Solid
Molecular Weight 495.02
Formel C₂₆H₃₁ClN₆O₂
Color Off-white to yellow
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
Synonyms

EGF816
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (9)

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Journal Impact Factor

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
Patent

US20250312348A1.
Patent

US20220177473A1.
Patent

US20220175778A1.
Patent

US20210361655A1.
Patent

US20190160066A1

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (202.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0201 mL

10.1006 mL

20.2012 mL

5 mM

0.4040 mL

2.0201 mL

4.0402 mL

10 mM

0.2020 mL

1.0101 mL

2.0201 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0201 mL	10.1006 mL	20.2012 mL	50.5030 mL
	5 mM	0.4040 mL	2.0201 mL	4.0402 mL	10.1006 mL
	10 mM	0.2020 mL	1.0101 mL	2.0201 mL	5.0503 mL
	15 mM	0.1347 mL	0.6734 mL	1.3467 mL	3.3669 mL
	20 mM	0.1010 mL	0.5050 mL	1.0101 mL	2.5252 mL
	25 mM	0.0808 mL	0.4040 mL	0.8080 mL	2.0201 mL
	30 mM	0.0673 mL	0.3367 mL	0.6734 mL	1.6834 mL
	40 mM	0.0505 mL	0.2525 mL	0.5050 mL	1.2626 mL
	50 mM	0.0404 mL	0.2020 mL	0.4040 mL	1.0101 mL
	60 mM	0.0337 mL	0.1683 mL	0.3367 mL	0.8417 mL
	80 mM	0.0253 mL	0.1263 mL	0.2525 mL	0.6313 mL
	100 mM	0.0202 mL	0.1010 mL	0.2020 mL	0.5050 mL

Bioz

Keywords

Nazartinib

9 Cited Publications

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Nazartinib

Publications Citing Use of MedChemExpress (MCE) Nazartinib

Alle EGFR Isoform-spezifische Produkte anzeigen