JNJ28871063 hydrochloride

Name: JNJ28871063 hydrochloride
Brand: MedChemExpress
SKU: HY-103441
Rating: 4.5 (1 reviews)

Cat. No.: HY-103441 Purity: 98.36%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

JNJ28871063 hydrochloride is an orally active, highly selective and ATP competitive pan-ErbB kinase inhibitor with IC₅₀ values of 22 nM, 38 nM, and 21 nM for ErbB1, ErbB2, and ErbB4, respectively. JNJ28871063 hydrochloride inhibits phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2. JNJ28871063 hydrochloride crosses the blood-brain barrier and has antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2.

For research use only. We do not sell to patients.

JNJ28871063 hydrochloride Chemical Structure

CAS No. : 944342-90-9

Size	Price	Stock	Quantity
5 mg	USD 304	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 517	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1086	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1806	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3000	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

ErbB1

22 nM (IC₅₀)

ErbB2

38 nM (IC₅₀)

ErbB4

21 nM (IC₅₀)

In Vitro

JNJ-28871063 demonstrates potent growth inhibition in vitro of human cancer cell lines (N87; BT474; SKBR3; A431; HN5) overexpressing the ErbB2 receptor with IC₅₀ values with 60-168 nM. 28871063 exhibited the least effect at inhibiting growth of non–ErbB-over-expressing cell lines (HeLa, A375, HCT116, HT29, MRC5 primary fibroblasts cells; IC₅₀>10 μM)^[1].
JNJ-28871063 hydrochloride (3 μM; 16 hours) reduces the basal level of ErbB2 phosphorylation in SKBR3 cells^[1].
JNJ28871063 hydrochloride is from an aminopyrimidine oxime structural class^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	BT474 cells
Concentration:	3 μM
Incubation Time:	16 hours
Result:	Reduced the basal level of ErbB2 phosphorylation.

In Vivo

JNJ28871063 hydrochloride (100 mg/kg/day; Oral; for 30 days) shows significant inhibition of tumor growth (TGI=71%)^[1].
JNJ28871063 hydrochloride produces a significant inhibition of tumor growth at 100 mg/kg (TGI=66.8%) in an A431 human tumor xenograft model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nude mice bearing N87 tumor xenografts^[1]
Dosage:	100 mg/kg
Administration:	Oral; daily for 30 days
Result:	Showed significant inhibition of tumor growth (TGI=71%).

Molecular Weight

519.42

Formula

C₂₄H₂₈Cl₂N₆O₃

CAS No.

944342-90-9

Appearance

Solid

Color

Light yellow to yellow

SMILES

NC1=C(/C=N/OCCN2CCOCC2)C(NC3=CC(Cl)=C(OCC4=CC=CC=C4)C=C3)=NC=N1.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (192.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9252 mL	9.6261 mL	19.2522 mL
5 mM	0.3850 mL	1.9252 mL	3.8504 mL
10 mM	0.1925 mL	0.9626 mL	1.9252 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (9.63 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (9.63 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (9.63 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.36%

Select Batch:

Data Sheet (275 KB) SDS (252 KB)

COA (249 KB) HNMR (142 KB) RP-HPLC (170 KB) LCMS (104 KB)

Handling Instructions (2659 KB)

References

[1]. Stuart L Emanuel, et al. Cellular and in vivo activity of JNJ-28871063, a nonquinazoline pan-ErbB kinase inhibitor that crosses the blood-brain barrier and displays efficacy against intracranial tumors. Mol Pharmacol. 2008 Feb;73(2):338-48. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.9252 mL	9.6261 mL	19.2522 mL	48.1306 mL
	5 mM	0.3850 mL	1.9252 mL	3.8504 mL	9.6261 mL
	10 mM	0.1925 mL	0.9626 mL	1.9252 mL	4.8131 mL
	15 mM	0.1283 mL	0.6417 mL	1.2835 mL	3.2087 mL
	20 mM	0.0963 mL	0.4813 mL	0.9626 mL	2.4065 mL
	25 mM	0.0770 mL	0.3850 mL	0.7701 mL	1.9252 mL
	30 mM	0.0642 mL	0.3209 mL	0.6417 mL	1.6044 mL
	40 mM	0.0481 mL	0.2407 mL	0.4813 mL	1.2033 mL
	50 mM	0.0385 mL	0.1925 mL	0.3850 mL	0.9626 mL
	60 mM	0.0321 mL	0.1604 mL	0.3209 mL	0.8022 mL
	80 mM	0.0241 mL	0.1203 mL	0.2407 mL	0.6016 mL
	100 mM	0.0193 mL	0.0963 mL	0.1925 mL	0.4813 mL