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BI-4142

Name: BI-4142
Brand: TargetMol
SKU: T63643
Price: 55 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T63643Cas No. 2682003-36-5

BI-4142 is an orally active, potent and selective HER2 inhibitor that inhibits cancer cell proliferation, suppresses her2-dependent cell lines and inhibits downstream signalling.

BI-4142

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Purity: 98.09%

Catalog No. T63643Cas No. 2682003-36-5

BI-4142 is an orally active, potent and selective HER2 inhibitor that inhibits cancer cell proliferation, suppresses her2-dependent cell lines and inhibits downstream signalling.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$55	-	In Stock
5 mg	$129	-	In Stock
10 mg	$197	-	In Stock
25 mg	$396	-	In Stock
50 mg	$596	-	In Stock
100 mg	$893	-	In Stock
200 mg	$1,490	-	In Stock
1 mL x 10 mM (in DMSO)	$148	-	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:98.09%

Appearance:Solid

Color:Yellow

Resource Download

COA HNMR HPLC

Product Introduction

Bioactivity

Description	BI-4142 is an orally active, potent and selective HER2 inhibitor that inhibits cancer cell proliferation, suppresses her2-dependent cell lines and inhibits downstream signalling.
Targets&IC50	HEK EGFRWT:270 nM, HER2:5 nM, HEK HER2YVMA:10 nM, Ba/F3 HER2YVMA cells:18 nM, Ba/F3 EGFRWT cells:2400 nM
In vitro	BI-4142 inhibits HER2-dependent cell lines and downstream signaling, with IC50 values of 10 nM, 18 nM, 270 nM, and 2400 nM against HEK HER2YVMA, Ba/F3 HER2YVMA, HEK EGFRWT, and Ba/F3 EGFRWT, respectively[1].BI-4142 (1 nM-5 μM, 72 h or 96 h) exhibits antiproliferative activity against tumor cells[1]. In the CaCo-2 assay, BI-4142 displays good permeability and no PgP-mediated efflux liability[1].
In vivo	BI-4142 administered at doses ranging from 0 to 100 mg/kg, orally twice daily for 40 days, significantly inhibits tumor growth and suppresses oncogenic signaling[1].

Chemical Properties

Molecular Weight	521.57
Formula	C₂₈H₂₇N₉O₂
Cas No.	2682003-36-5
Smiles	O=C(C=C)N1CCN(C2=NC=C3N=CN=C(NC4=CC=C(OC=5C=CC6=C(N=CN6C)C5)C(=C4)C)C3=N2)CC1

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: 80 mg/mL (153.38 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9173 mL	9.5864 mL	19.1729 mL	95.8644 mL
5 mM	0.3835 mL	1.9173 mL	3.8346 mL	19.1729 mL
10 mM	0.1917 mL	0.9586 mL	1.9173 mL	9.5864 mL
20 mM	0.0959 mL	0.4793 mL	0.9586 mL	4.7932 mL
50 mM	0.0383 mL	0.1917 mL	0.3835 mL	1.9173 mL
100 mM	0.0192 mL	0.0959 mL	0.1917 mL	0.9586 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