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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	Availability
1 mg	$89	In Stock
2 mg	$126	In Stock
5 mg	$198	In Stock
10 mg	$328	In Stock
25 mg	$663	In Stock
50 mg	$1,060	In Stock
100 mg	$1,630	In Stock
500 mg	$3,280	In Stock
1 mL x 10 mM (in DMSO)	$226	In Stock

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Purity:99.71%

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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)
Color	White
Appearance	Solid

Storage & Solubility Information

Storage

keep away from direct sunlight | Powder: -20°C for 3 years | 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.

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 mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/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

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

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 μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

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