JNJ-28871063 hydrochloride | CAS# 944342-90-9 | ErbB receptor family inhibitor

MedKoo Cat#: 574760 | Name: JNJ-28871063 hydrochloride

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

JNJ-28871063 hydrochloride is an ErbB receptor family inhibitor that inhibits growth of human cancer cell lines overexpressing ErbB2 and growth of human tumor xenografts.

Chemical Structure

JNJ-28871063 hydrochloride

CAS# 944342-90-9

Theoretical Analysis

MedKoo Cat#: 574760

Name: JNJ-28871063 hydrochloride

CAS#: 944342-90-9

Chemical Formula: C24H28Cl2N6O3

Exact Mass: 518.1600

Molecular Weight: 519.43

Elemental Analysis: C, 55.50; H, 5.43; Cl, 13.65; N, 16.18; O, 9.24

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 515.00	2 Weeks
50mg	USD 1,550.00	2 Weeks

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Synonym

JNJ-28871063 hydrochloride; JNJ-28871063 HCl

IUPAC/Chemical Name

(E)-4-amino-6-((4-(benzyloxy)-3-chlorophenyl)amino)pyrimidine-5-carbaldehyde O-(2-morpholinoethyl) oxime hydrochloride

InChi Key

ZXKZRKQMKNRZNN-GZPZNDDGSA-N

InChi Code

InChI=1S/C24H27ClN6O3.ClH/c25-21-14-19(6-7-22(21)33-16-18-4-2-1-3-5-18)30-24-20(23(26)27-17-28-24)15-29-34-13-10-31-8-11-32-12-9-31;/h1-7,14-15,17H,8-13,16H2,(H3,26,27,28,30);1H/b29-15+;

SMILES Code

ClC1=CC(NC2=C(/C=N/OCCN3CCOCC3)C(N)=NC=N2)=CC=C1OCC4=CC=CC=C4.[H]Cl

Appearance

Solid powder

Purity

>97% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

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.

In vitro activity:

Treatment of human cancer cells with JNJ-28871063 inhibited phosphorylation of functionally important tyrosine residues in both EGFR and ErbB2 and blocked downstream signal transduction pathways responsible for proliferation and survival. Reference: Mol Pharmacol. 2008 Feb;73(2):338-48. https://pubmed.ncbi.nlm.nih.gov/17975007/

In vivo activity:

A single dose of JNJ-28871063 reduced phosphorylation of ErbB2 receptors in tumor-bearing mice, demonstrating target suppression in vivo. In an intracranial ErbB2-overexpressing tumor model, JNJ-28871063 extended survival relative to untreated animals. Reference: Mol Pharmacol. 2008 Feb;73(2):338-48. https://pubmed.ncbi.nlm.nih.gov/17975007/

	Solvent	mg/mL	mM
Solubility
	DMSO	26.0	50.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 519.43 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Emanuel SL, Hughes TV, Adams M, Rugg CA, Fuentes-Pesquera A, Connolly PJ, Pandey N, Moreno-Mazza S, Butler J, Borowski V, Middleton SA, Gruninger RH, Story JR, Napier C, Hollister B, Greenberger LM. 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. doi: 10.1124/mol.107.041236. Epub 2007 Nov 1. PMID: 17975007.

In vitro protocol:

In vivo protocol:

1. Contessa and Hamstra (2008) Revoking the privilege: targeting HER2 in the central nervous system. Mol.Pharmacol. 73 271 PMID: 17981994 2. Emanuel et al (2008) 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. 73 338 PMID: 17975007 3. Guessous et al (2008) Signaling pathways in medulloblastoma. J.Cell.Phys. 217 577