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JNJ28871063 hydrochloride

Name: JNJ28871063 hydrochloride
Brand: TargetMol
SKU: T22881
Price: 93 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T22881Cas No. 944342-90-9

Alias JNJ-28871063 hydrochloride, JNJ 28871063 hydrochloride

JNJ28871063 hydrochloride is an orally active, ATP-competitive, and highly selective pan-ErbB kinase inhibitor with IC50 values of 22 nM for ErbB1, 38 nM for ErbB2, and 21 nM for ErbB4, JNJ28871063 hydrochloride effectively inhibits phosphorylation of key tyrosine residues in EGFR and ErbB2, crossing the blood–brain barrier, and demonstrating antitumor efficacy in xenograft models overexpressing EGFR and ErbB2.

JNJ28871063 hydrochloride

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Purity: 99.95%

Catalog No. T22881Alias JNJ-28871063 hydrochloride, JNJ 28871063 hydrochlorideCas No. 944342-90-9

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$93	-	In Stock
5 mg	$228	-	In Stock
10 mg	$372	-	In Stock
25 mg	$762	-	In Stock
50 mg	$1,320	-	In Stock
100 mg	$2,120	-	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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Purity:99.95%

Appearance:Solid

Color:Yellow

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	JNJ28871063 hydrochloride is an orally active, ATP-competitive, and highly selective pan-ErbB kinase inhibitor with IC50 values of 22 nM for ErbB1, 38 nM for ErbB2, and 21 nM for ErbB4, JNJ28871063 hydrochloride effectively inhibits phosphorylation of key tyrosine residues in EGFR and ErbB2, crossing the blood–brain barrier, and demonstrating antitumor efficacy in xenograft models overexpressing EGFR and ErbB2.
Targets&IC50	HER2:38 nM, Her1:22 nM
In vitro	In kinase assays, JNJ28871063 hydrochloride inhibited ErbB1, ErbB2, and ErbB4 with IC50 values of 22-38 nM. In cellular assays, it demonstrated growth inhibition in ErbB-overexpressing cancer cells (IC50 60-168 nM) while showing low potency in low-expression lines (>10 μM). Treatment (3 μM, 16 h) reduced basal ErbB2 phosphorylation in BT474 and SKBR3 cells [1].
In vivo	In nude mice bearing N87 (gastric cancer) xenografts, oral administration of JNJ28871063 hydrochloride (100 mg/kg/day for 30 days) resulted in a tumor growth inhibition (TGI) of 71%. In an A431 (epidermoid carcinoma) xenograft model, the same dosage produced a TGI of 66.8%. A characteristic of the compound is its ability to cross the blood-brain barrier (BBB), demonstrating activity against intracranial tumors in preclinical models of ErbB-driven cancers [1].
Synonyms	JNJ-28871063 hydrochloride, JNJ 28871063 hydrochloride

Chemical Properties

Molecular Weight	519.42
Formula	C₂₄H₂₈Cl₂N₆O₃
Cas No.	944342-90-9
Smiles	N(C=1C(/C=N/OCCN2CCOCC2)=C(N)N=CN1)C3=CC(Cl)=C(OCC4=CC=CC=C4)C=C3.Cl
Relative Density.	no data available

Storage & Solubility Information

Storage

store at low temperature | 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 (154.02 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1 mg/mL (1.93 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	1.9252 mL	9.6261 mL	19.2522 mL	96.2612 mL
5 mM	0.3850 mL	1.9252 mL	3.8504 mL	19.2522 mL
10 mM	0.1925 mL	0.9626 mL	1.9252 mL	9.6261 mL
20 mM	0.0963 mL	0.4813 mL	0.9626 mL	4.8131 mL
50 mM	0.0385 mL	0.1925 mL	0.3850 mL	1.9252 mL
100 mM	0.0193 mL	0.0963 mL	0.1925 mL	0.9626 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