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Tucatinib hemiethanolate

Name: Tucatinib hemiethanolate
Brand: TargetMol
SKU: T36648
Price: 40 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T36648Cas No. 1429755-56-5

Alias ONT-380 hemiethanolate, Irbinitinib hemiethanolate, ARRY-380 hemiethanolate

Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active, and selective HER2 inhibitor with an IC50 of 8 nM.

Tucatinib hemiethanolate

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Purity: 99.76%

Catalog No. T36648Alias ONT-380 hemiethanolate, Irbinitinib hemiethanolate, ARRY-380 hemiethanolateCas No. 1429755-56-5

Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active, and selective HER2 inhibitor with an IC50 of 8 nM.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$40	In Stock	In Stock
10 mg	$61	In Stock	In Stock
25 mg	$98	In Stock	In Stock
50 mg	$139	In Stock	In Stock
100 mg	$198	-	In Stock
1 mL x 10 mM (in DMSO)	$44	In Stock	In Stock

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

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Purity:99.76%

Appearance:Solid

Color:White

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COA HPLC HNMR

Product Introduction

Bioactivity

Description	Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active, and selective HER2 inhibitor with an IC50 of 8 nM.
Targets&IC50	HER2:8 nM (IC50)
In vitro	Tucatinib hemiglycolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 over EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 but not EGFR[1].
In vivo	Tucatinib hemiethanolate (ONT-380 hemiethanolate, 200 mg/kg/d) improves survival at maximum-tolerated dose[1] and reduces brain pErbB2 levels by 80%[2]. This compound (ARRY-380 hemiethanolate) shows significant tumor growth inhibition (TGI)—50% at 50 mg/kg/d and up to 96% at 100 mg/kg/d, with over 50% reduction in baseline tumor size in 9 out of 12 animals at the higher dosage. When combined with trastuzumab at 50 mg/kg/d, it achieves 98% TGI, with complete regressions in 9 out of 12 animals and partial regressions in two[3].
Synonyms	ONT-380 hemiethanolate, Irbinitinib hemiethanolate, ARRY-380 hemiethanolate

Chemical Properties

Molecular Weight	1007.11
Formula	C₅₄H₅₄N₁₆O₅
Cas No.	1429755-56-5
Smiles	CCO.Cc1cc(Nc2ncnc3ccc(NC4=NC(C)(C)CO4)cc23)ccc1Oc1ccn2ncnc2c1.Cc1cc(Nc2ncnc3ccc(NC4=NC(C)(C)CO4)cc23)ccc1Oc1ccn2ncnc2c1
Relative Density.	no data available

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

DMSO: 125 mg/mL (124.12 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (3.28 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	0.9929 mL	4.9647 mL	9.9294 mL	49.6470 mL
5 mM	0.1986 mL	0.9929 mL	1.9859 mL	9.9294 mL
10 mM	0.0993 mL	0.4965 mL	0.9929 mL	4.9647 mL
20 mM	0.0496 mL	0.2482 mL	0.4965 mL	2.4824 mL
50 mM	0.0199 mL	0.0993 mL	0.1986 mL	0.9929 mL
100 mM	0.0099 mL	0.0496 mL	0.0993 mL	0.4965 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