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Naquotinib

Name: Naquotinib
Brand: TargetMol
SKU: TQ0092
Price: 135 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. TQ0092Cas No. 1448232-80-1

Alias ASP8273

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

Naquotinib

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Purity: 97.49%

Catalog No. TQ0092Alias ASP8273Cas No. 1448232-80-1

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

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$43	In Stock	In Stock
2 mg	$61	In Stock	In Stock
5 mg	$98	In Stock	In Stock
50 mg	Preferential	In Stock	-
1 mL x 10 mM (in DMSO)	$135	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:97.49%

Appearance:Solid

Color:Yellow

Resource Download

COA HPLC HNMR

Product Introduction

Bioactivity

Description	Naquotinib (ASP8273) (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; (IC50s: 8-33 nM and 230 nM toward EGFR mutants and EGFR.
Targets&IC50	EGFR:230 nM, EGFR (mutants):8-33 nM
In vitro	In studies utilizing cells inherently dependent on EGFR, Naquotinib effectively hinders the proliferation of various cancer cell lines, including PC-9(del ex19), HCC827(del ex19), NCI-H1975(del ex19/T790M), and PC-9ER(del ex19/T790M), demonstrating IC50 values ranging from 8 to 33 nM [1]. It specifically targets and suppresses the phosphorylation of EGFR along with the subsequent activation of the ERK and Akt signaling pathways, starting at concentrations as low as 10nM in HCC827 and NCI-H1975 cells. However, this effect requires a much higher concentration of 1000nM in A431 cells. Notably, in NCI-H1650 (del ex19) cells, Naquotinib significantly curtails cell growth with an IC50 value of 70nM, showing its efficacy where other EGFR-TKIs have limited effectiveness [2].
In vivo	In NCI-H1975 (L858R/T790M), HCC827 (del ex19), and PC-9 (del ex19) xenograft models, oral administration of Naquotinib results in dose-dependent tumor regression, with the dosing schedules having no impact on its efficacy. Specifically, in an NCI-H1975 xenograft model, Naquotinib leads to complete tumor regression after a 14-day treatment period. Remarkably, 50% of the mice maintain complete regression for over 85 days following the cessation of Naquotinib treatment [2].
Synonyms	ASP8273

Chemical Properties

Molecular Weight	562.71
Formula	C₃₀H₄₂N₈O₃
Cas No.	1448232-80-1
Smiles	CCc1nc(C(N)=O)c(Nc2ccc(cc2)N2CCC(CC2)N2CCN(C)CC2)nc1O[C@@H]1CCN(C1)C(=O)C=C
Relative Density.	1.248 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: Insoluble

Ethanol: 80 mg/mL (142.17 mM), Sonication is recommended.

DMSO: 40 mg/mL (71.08 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.55 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	1.7771 mL	8.8856 mL	17.7711 mL	88.8557 mL
5 mM	0.3554 mL	1.7771 mL	3.5542 mL	17.7711 mL
10 mM	0.1777 mL	0.8886 mL	1.7771 mL	8.8856 mL
20 mM	0.0889 mL	0.4443 mL	0.8886 mL	4.4428 mL
50 mM	0.0355 mL	0.1777 mL	0.3554 mL	1.7771 mL

Ethanol

	1mg	5mg	10mg	50mg
100 mM	0.0178 mL	0.0889 mL	0.1777 mL	0.8886 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc