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Zongertinib

Name: Zongertinib
Brand: TargetMol
SKU: T69534
Price: 64 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: BI 764532, BI 1810631) Copy Product Info

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Synonyms: BI 764532, BI 1810631

Catalog No. T69534 Copy Product Info

Purity: 99.83%

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Zongertinib (BI 1810631) is a HER2 inhibitor, a selective HER2 tyrosine kinase inhibitor (with IC50 values of 13 nM and 579 nM for HER2 and EGFR, respectively), featuring covalent binding properties, used for solid tumor research.

Cas No. 2728667-27-2

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Pack Size	Price	USA Stock	Global Stock
1 mg	$64	In Stock	In Stock
5 mg	$156	In Stock	In Stock
10 mg	$247	In Stock	In Stock
25 mg	$413	In Stock	In Stock
50 mg	$579	-	In Stock
100 mg	$787	-	In Stock
1 mL x 10 mM (in DMSO)	$183	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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Custom-made molecule. TargetMol’s expert synthesis team delivers cost-effective solutions. Contact us for inquiries. Committed to serving you.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.83%

Appearance:Solid

Color:Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	Zongertinib (BI 1810631) is a HER2 inhibitor, a selective HER2 tyrosine kinase inhibitor (with IC50 values of 13 nM and 579 nM for HER2 and EGFR, respectively), featuring covalent binding properties, used for solid tumor research.
Targets & IC50	BaF3 HER2 WT cells:1 nM, A431 cells (EGFR wt amp):> 5000 nM, BaF3 HER2 YVMA cells:16 nM, NCI-H2170 HER2 YVMA cells:33 nM, NCI-H-2170 cells (HER2 WT Amp):6 nM, BaF3 EGF dep cells:1540 nM
In vitro	Methods: Phosphorylation assays were performed in HEK cells, and proliferation assays were conducted in Ba/F3 cells. Results: Zongertinib demonstrated high potency against HER2 YVMA with selectivity over wild-type EGFR; in Ba/F3 cells, its inhibitory effect on HER2 YVMA was 100-fold higher than that on wild-type EGFR. [1]
In vivo	Methods: In NCI-N87 (HER2-amplified) and PC-9 HER2YVMA CDX and PDX models, Zongertinib (5-50 mg/kg) was administered orally once daily, alone or in combination with T-DXd, T-DM1, or adagrasib, for 21-60 consecutive days. Results: Zongertinib alone significantly inhibited tumor growth, and combination with ADCs or KRASG12C inhibitors synergistically enhanced anti-tumor activity with good tolerability. [2]
Synonyms	BI 764532, BI 1810631

Chemical Properties

Molecular Weight	535.6
Formula	C₂₉H₂₉N₉O₂
Cas No.	2728667-27-2
Smiles	N(C=1C2=C(C=NC(=N2)N3CCC(NC(C=C)=O)CC3)N=CN1)C4=CC(C)=C(OC=5C=C6C(=CC5)N(C)C=N6)C=C4

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: 45.91 mg/mL (85.72 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2 mg/mL (3.73 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	1.8671 mL	9.3353 mL	18.6706 mL	93.3532 mL
5 mM	0.3734 mL	1.8671 mL	3.7341 mL	18.6706 mL
10 mM	0.1867 mL	0.9335 mL	1.8671 mL	9.3353 mL
20 mM	0.0934 mL	0.4668 mL	0.9335 mL	4.6677 mL
50 mM	0.0373 mL	0.1867 mL	0.3734 mL	1.8671 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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