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TAS6417

Name: TAS6417
Brand: TargetMol
SKU: T16996
Price: 89 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T16996Cas No. 1661854-97-2

Zipalertinib (TAS6417, CLN-081) is a novel, highly potent, orally active covalent EGFR tyrosine kinase inhibitor that uniquely binds to the ATP binding site of the EGFR hinge region with an IC50 value of 1.1-8.0 nM.

TAS6417

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Purity: 99.71%

Catalog No. T16996Cas No. 1661854-97-2

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$89	In Stock	In Stock
2 mg	$126	In Stock	In Stock
5 mg	$198	In Stock	In Stock
10 mg	$328	In Stock	In Stock
25 mg	$662	In Stock	In Stock
50 mg	$883	In Stock	In Stock
100 mg	$1,190	In Stock	In Stock
200 mg	$1,630	-	In Stock
1 mL x 10 mM (in DMSO)	$226	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:99.71%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Zipalertinib (TAS6417, CLN-081) is a novel, highly potent, orally active covalent EGFR tyrosine kinase inhibitor that uniquely binds to the ATP binding site of the EGFR hinge region with an IC50 value of 1.1-8.0 nM.
Targets&IC50	EGFR:1.1-8.0 nM
In vitro	METHODS: Two cell lines with EGFR exon 20 insertion isolated and established from lung cancer patients, BID007 and BID019, were treated with Zipalertinib (TAS6417, CLN-081) (0.001, 0.01, 0.1, 1, 10 μM). RESULTS Zipalertinib (TAS6417, CLN-081) inhibited EGFR phosphorylation in both cell lines at 10 nM and 100 nM. [1]
In vivo	METHODS: Nude mice bearing NIH/3T3 EGFR G719A allografts, nude mice bearing BID007, and nude mice bearing H1975 cells were treated with TAS6417 (50, 100, 200 mg/kg, oral, 15 days) to study the in vivo efficacy of Zipalertinib (TAS6417, CLN-081) against EGFR mutations. RESULTS Zipalertinib (TAS6417, CLN-081) inhibited tumor formation in nude mice bearing H1975, NIH/3T3 expressing G719A, NIH/3T3 expressing G719A+T790M, BID007, and H1975-insSVD. [1]

Chemical Properties

Molecular Weight	396.44
Formula	C₂₃H₂₀N₆O
Cas No.	1661854-97-2
Smiles	CC1=C[C@@H](Cn2c1c(-c1cnc3ccccc3c1)c1c(N)ncnc21)NC(=O)C=C
Relative Density.	1.40 g/cm3 (Predicted)

Storage & Solubility Information

Storage

keep away from direct sunlight | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 55 mg/mL (138.73 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (6.31 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

	1mg	5mg	10mg	50mg
1 mM	2.5224 mL	12.6122 mL	25.2245 mL	126.1225 mL
5 mM	0.5045 mL	2.5224 mL	5.0449 mL	25.2245 mL
10 mM	0.2522 mL	1.2612 mL	2.5224 mL	12.6122 mL
20 mM	0.1261 mL	0.6306 mL	1.2612 mL	6.3061 mL
50 mM	0.0504 mL	0.2522 mL	0.5045 mL	2.5224 mL
100 mM	0.0252 mL	0.1261 mL	0.2522 mL	1.2612 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