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Naquotinib mesylate

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Naquotinib mesylate

Catalog No. T12175Cas No. 1448237-05-5

Naquotinib mesylate (ASP8273 (mesylate)) is an orally available, mutant-selective and irreversible inhibitor of EGFR(iC50s of 8-33 nM and 230 nM for toward EGFR mutants and EGFR).

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Pack Size	Price	Availability	Quantity
2 mg	$58	5 days

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Product Introduction

Bioactivity

Description	Naquotinib mesylate (ASP8273 (mesylate)) is an orally available, mutant-selective and irreversible inhibitor of EGFR(iC50s of 8-33 nM and 230 nM for toward EGFR mutants and EGFR).
Targets&IC50	EGFR:230 nM
In vitro	In NCI-H1650 (del ex19), Naquotinib inhibits cell growth with an IC50 value of 70nM while other EGFR-TKIs are only partially effective.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[2].
In vivo	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].
Alias	ASP8273 (mesylate)

Chemical Properties

Molecular Weight	658.81
Formula	C31H46N8O6S
Cas No.	1448237-05-5

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 12.5 mg/mL (18.97 mM), Sonication and heating are recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.5179 mL	7.5894 mL	15.1789 mL	75.8944 mL
5 mM	0.3036 mL	1.5179 mL	3.0358 mL	15.1789 mL
10 mM	0.1518 mL	0.7589 mL	1.5179 mL	7.5894 mL

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In Vivo Formulation Calculator (Clear solution)

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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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