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BI-4142

Name: BI-4142
Brand: TargetMol
SKU: T63643
Price: 179 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	Availability
1 mg	$179	In Stock
5 mg	$463	In Stock
10 mg	$728	In Stock
25 mg	$1,180	In Stock
50 mg	$1,630	In Stock
100 mg	$2,470	In Stock
1 mL x 10 mM (in DMSO)	$558	In Stock

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Batch Information

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Purity:98.09%

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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	Ba/F3 EGFRWT:2400 nM, Ba/F3 HER2YVMA:18 nM, HER2:5 nM, HEK HER2YVMA:10 nM, HEK EGFRWT:270 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
Color	Yellow
Appearance	Solid

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 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

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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