Cat. No.: HY-19729

Naquotinib

(Synonyms: ASP8273)

5 Cited Publications

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Based on 5 publication(s) in Google Scholar

Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC₅₀s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

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Pureté: 98.10%
CAS No.: 1448232-80-1
Formule: C₃₀H₄₂N₈O₃
Masse moléculaire:562.71

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Naquotinib Chemical Structure

CAS No.: 1448232-80-1

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC₅₀s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.

IC₅₀ & Target^[1]

EGFR

230 nM (IC₅₀)

EGFR^T790M

EGFR^L858R/T790M

EGFR^L858R

EGFR^{Exon 19 deletion/T790M}

Voir tous les produits spécifiques à Isoform EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
NCI-H1975	IC₅₀	8 nM Compound: ASP8273	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]
PC-9	IC₅₀	8 nM Compound: ASP8273	Inhibition of EGFR Del ex19 mutant in human PC9 cells assessed as suppression of cell proliferation Inhibition of EGFR Del ex19 mutant in human PC9 cells assessed as suppression of cell proliferation	[PMID: 26968253]
PC-9	IC₅₀	8 nM Compound: ASP8273	Inhibition of EGFR Del ex19/T790M double mutant in human PC9 cells assessed as suppression of cell proliferation Inhibition of EGFR Del ex19/T790M double mutant in human PC9 cells assessed as suppression of cell proliferation	[PMID: 26968253]

In Vitro

In assays using endogenously EGFR-dependent cells, Naquotinib inhibits the growth of PC-9(del ex19), HCC827(del ex19), NCI-H1975(del ex19/T790M) and PC-9ER(del ex19/T790M) with IC₅₀s of 8-33 nM^[1]. Naquotinib selectively inhibits phosphorylation of EGFR and its down-stream signal pathway, ERK and Akt from 10nM in HCC827 and NCI-H1975 while inhibitory effects are only detected at 1000nM in A431.In NCI-H1650 (del ex19), Naquotinib inhibits cell growth with an IC₅₀ value of 70nM while other EGFR-TKIs are only partially effective^[2].

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

In Vivo

Oral Naquotinib treatment dose dependently induces tumor regression in NCI-H1975 (L858R/T790M), HCC827 (del ex19) and PC-9 (del ex19) xenograft models. Dosing schedules does not affect the efficacy of Naquotinib. In an NCI-H1975 xenograft model, complete regression of tumor is achieved after 14-days of Naquotinib treatment. Complete regression is maintained in 50% of mice more than 85 days after cessation of Naquotinib treatment^[2].

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

Chemical Information

CAS No. 1448232-80-1
Appearance Solid
Masse moléculaire 562.71
Formule C₃₀H₄₂N₈O₃
Color Light yellow to yellow
SMILES

O=C(C1=NC(CC)=C(O[C@H]2CN(C(C=C)=O)CC2)N=C1NC3=CC=C(N4CCC(N5CCN(C)CC5)CC4)C=C3)N
Synonyms

ASP8273
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (5)

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Cell Rep

Drug repurposing screens reveal cell-type-specific entry pathways and FDA-approved drugs active against SARS-Cov-2. [Abstract]

2021 Apr 6;35(1):108959. PMID: 33811811
RSC Adv

Reactive intermediates in naquotinib metabolism identified by liquid chromatography-tandem mass spectrometry: phase I metabolic profiling. [Abstract]

2019 Apr 1;9(18):10211-10225. PMID: 35520926
RSC Adv

A simple liquid chromatography-tandem mass spectrometry method to accurately determine the novel third-generation EGFR-TKI naquotinib with its applicability to metabolic stability assessment. [Abstract]

2019 Feb 7;9(9):4862-4869. PMID: 35514667
R Soc Open Sci

A highly sensitive LC-MS/MS method to determine novel Bruton's tyrosine kinase inhibitor spebrutinib: application to metabolic stability evaluation. [Abstract]

2019 Jun 5;6(6):190434. PMID: 31312501
bioRxiv

2020 Jun.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (177.71 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

1.7771 mL

8.8856 mL

17.7711 mL

5 mM

0.3554 mL

1.7771 mL

3.5542 mL

10 mM

0.1777 mL

0.8886 mL

1.7771 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: 2.5 mg/mL (4.44 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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)
Instruction de manipulation (2659 KB)

Références

[1]. Sakagami H, et al. ASP8273, a novel mutant-selective irreversible EGFR inhibitor, inhibits growth of non-small cell lung cancer (NSCLC) cells with EGFR activating and T790M resistance mutations. [abstract]. In: Proceedings of the 105th Annual Meeting of t

[2]. Konagai S, et al. ASP8273 selectively inhibits mutant EGFR signal pathway and induces tumor shrinkage in EGFR mutated tumor models. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Ph

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7771 mL	8.8856 mL	17.7711 mL	44.4279 mL
	5 mM	0.3554 mL	1.7771 mL	3.5542 mL	8.8856 mL
	10 mM	0.1777 mL	0.8886 mL	1.7771 mL	4.4428 mL
	15 mM	0.1185 mL	0.5924 mL	1.1847 mL	2.9619 mL
	20 mM	0.0889 mL	0.4443 mL	0.8886 mL	2.2214 mL
	25 mM	0.0711 mL	0.3554 mL	0.7108 mL	1.7771 mL
	30 mM	0.0592 mL	0.2962 mL	0.5924 mL	1.4809 mL
	40 mM	0.0444 mL	0.2221 mL	0.4443 mL	1.1107 mL
	50 mM	0.0355 mL	0.1777 mL	0.3554 mL	0.8886 mL
	60 mM	0.0296 mL	0.1481 mL	0.2962 mL	0.7405 mL
	80 mM	0.0222 mL	0.1111 mL	0.2221 mL	0.5553 mL
	100 mM	0.0178 mL	0.0889 mL	0.1777 mL	0.4443 mL

Keywords

Naquotinib

5 Cited Publications

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Naquotinib

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Publications Citing Use of MedChemExpress (MCE) Naquotinib

Voir tous les produits spécifiques à Isoform EGFR

Activité biologique

Chemical Information

Publications (5)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Naquotinib Related Classifications

HY-19729 Related Classifications