2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. Nazartinib

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.

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Nazartinib

Nazartinib Estructura química

No. CAS : 1508250-71-2

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Revisión del cliente

Based on 9 publication(s) in Google Scholar

Other Forms of Nazartinib:

Nazartinib Related Antibodies

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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Descripciòn

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.

IC50 & Target[1]

EGFRL858R/T790M

31 nM (Ki)

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.

Nazartinib Related Antibodies
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.
Ensayo clínico
Peso molecular

495.02

Fòrmula

C26H31ClN6O2
No. CAS
Appearance

Solid

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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0201 mL 10.1006 mL 20.2012 mL
5 mM 0.4040 mL 2.0201 mL 4.0402 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Calculadora de molaridad

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

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

V1

=
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C2

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V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación

Purity: 99.53%

SDS (393 KB)

COA (256 KB) HNMR (258 KB) NP-HPLC (243 KB) LCMS (96 KB)

Instrucciones de manejo (2659 KB)
Referencias
Ensayo de quinasas
[1]

Recombinant kinase domain of EGFR L858R and T790M-L858R mutants are incubated with Nazartinib to confirm covalent modification of EGFR and site of adduction. Recombinant enzyme is incubated at room temperature with a 20-fold molar excess of compound in 40 mM Tris, pH 8, 500 mM NaCl, 1% glycerol, 5 mM TCEP for 1 h. The reaction is quenched by addition of dithiothreitol (DTT, 80-fold excess to compound) and transfer to ice. A third of the reaction (10 μL) is processed for intact MS by adding an equal volume of 6 M Guan HCl, 100 mM Tris, pH 8, 20 mM DTT, 10 mM TCEP and incubating at room temperature for 15 min. Intact MS analysis is performed on an Agilent 6520 QToF mass spectrometer equipped with a dual spray ion source (IS of 4500 V, fragmentor of 250 V, fas temp of 350°C, and skimmer of 75 V). The samples are injected onto a PLRP-S column (2.1 mm×50 mm), heated to 60°C, and desalted for 2 min at 500 μL/min and 3% B prior to elution with a fast gradient of 3-50% B in 3 min (B, 0.1% formic acid). The data are analyzed in MassHunter for automatic peak selection, integration, and spectral deconvolution with a mass range of 15 000-75 000 Da.

MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Ensayo celular
[2]

Cells are seeded 500 cells/well in solid white 384-well plates in maintenance media. Serial diluted compounds are transferred to cells. After 3 days, cell viability is measured by CellTiter-Glo. BaF3 cell viability is measured 2 days after compound treatment using Bright-Glo Luciferase Assay System. Luminescent readout is normalized to 0.1% DMSO-treated cells and empty wells. Five EGFR TKI-resistant cell lines are generated at Massachusetts General Hospital. MGH134, MGH121, MGH141, and MGH157 are derived from patients who developed resistance to erlotinib with acquired T790M mutation. MGH119-R is generated in vitro by treating MGH119 with gefitinib for a prolonged period. The sensitivity of Nazartinib on these lines is tested.

MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Administraciòn de animales
[1]

Foxn1 nude mice bearing the H1975 tumors are randomized and used for efficacy studies. Compounds are formulated in 0.5% MC, 0.5% Tween 80 suspension formulation and administered by oral gavage at a dosing volume of 10 μL/g of the animal body weight. Animals in each group receive one oral dose of either vehicle (n=6) or the different test compounds (n=6 in each dose group). Plasma samples are collected for PK measurements at 30 min, 3 h, 7 h, and 24 h after last dose on day 5. Body weight is monitored daily, and the % change in body weight is calculated as [(BWcurrent-BWinitial)/(BWinitial)]×100. Data are presented as percent body weight change from the day of treatment initiation. Tumor sizes are assessed three times during the efficacy study for 5 days. Tumor sizes are determined by using caliper measurements. Tumor volumes are calculated with the formula (length×width×width)/2.

MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias

Complete Stock Solution Preparation Table

* 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.

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
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Nazartinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nazartinib1508250-71-2EGF816EGF 816EGF-816EGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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