Home >> Research Area >>Tyrosine Kinase/Adaptors>>EGFR>> JNJ 28871063 hydrochloride

JNJ 28871063 hydrochloride

Potent ErbB receptor family inhibitor CAS# 944342-90-9

JNJ 28871063 hydrochloride

Catalog No. BCC7662----Order now to get a substantial discount!

Product Name & Size Price Stock
JNJ 28871063 hydrochloride: 5mg $127 In Stock
JNJ 28871063 hydrochloride: 10mg Please Inquire In Stock
JNJ 28871063 hydrochloride: 20mg Please Inquire Please Inquire
JNJ 28871063 hydrochloride: 50mg Please Inquire Please Inquire
JNJ 28871063 hydrochloride: 100mg Please Inquire Please Inquire
JNJ 28871063 hydrochloride: 200mg Please Inquire Please Inquire
JNJ 28871063 hydrochloride: 500mg Please Inquire Please Inquire
JNJ 28871063 hydrochloride: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of JNJ 28871063 hydrochloride

Number of papers citing our products

Chemical structure

JNJ 28871063 hydrochloride

3D structure

Chemical Properties of JNJ 28871063 hydrochloride

Cas No. 944342-90-9 SDF Download SDF
PubChem ID 17747413 Appearance Powder
Formula C24H28Cl2N6O3 M.Wt 519.42
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 50 mM in DMSO
Chemical Name 4-N-(3-chloro-4-phenylmethoxyphenyl)-5-[(E)-2-morpholin-4-ylethoxyiminomethyl]pyrimidine-4,6-diamine;hydrochloride
SMILES C1COCCN1CCON=CC2=C(N=CN=C2NC3=CC(=C(C=C3)OCC4=CC=CC=C4)Cl)N.Cl
Standard InChIKey ZXKZRKQMKNRZNN-GZPZNDDGSA-N
Standard InChI 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+;
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of JNJ 28871063 hydrochloride

DescriptionPotent and selective ErbB receptor family inhibitor (IC50 values are 21, 22 and 38 nM for ErbB4, EGFR and ErbB2 respectively). Displays potent growth inhibition of human cancer cell lines overexpressing ErbB2 in vitro (IC50 = 60 - 168 nM) and inhibits growth of human tumor xenografts in vivo. Brain penetrant and orally active.

JNJ 28871063 hydrochloride Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

JNJ 28871063 hydrochloride Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of JNJ 28871063 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.9252 mL 9.6261 mL 19.2522 mL 38.5045 mL 48.1306 mL
5 mM 0.385 mL 1.9252 mL 3.8504 mL 7.7009 mL 9.6261 mL
10 mM 0.1925 mL 0.9626 mL 1.9252 mL 3.8504 mL 4.8131 mL
50 mM 0.0385 mL 0.1925 mL 0.385 mL 0.7701 mL 0.9626 mL
100 mM 0.0193 mL 0.0963 mL 0.1925 mL 0.385 mL 0.4813 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University
Featured Products
New Products
 

References on JNJ 28871063 hydrochloride

Revoking the privilege: targeting HER2 in the central nervous system.[Pubmed:17981994]

Mol Pharmacol. 2008 Feb;73(2):271-3.

Pharmacologic agents developed for cancer therapy have traditionally relied on a therapeutic ratio of effects between tumors and normal tissue. Over the past decade, this concept has been refined through the development of agents that are intended to specifically target tumor cells. The epidermal growth factor receptor (EGFR) (ErbB) family of receptor tyrosine kinases is an intensely studied target in many cancer cell types, and several successful therapeutic agents have been developed to block the growth promoting functions of these receptors. However, with their success has come the evolution of novel clinical scenarios by which tumor cells can evade these targeted therapies. Trastuzumab, a monoclonal antibody to Her2/ErbB2 that is used in breast cancer, has been shown to provide a survival benefit for patients whose tumors express this receptor but it does not have activity in the central nervous system because of the blood-brain barrier. In this issue of Molecular Pharmacology, Emanuel et al. (p. 328) report on a tyrosine kinase inhibitor that targets Her2/neu and also crosses the blood-brain barrier. Efforts to improve current strategies of targeting this receptor may lead not only to benefits in the treatment of breast cancer but also to advances in the treatment of other central nervous system malignancies, such as gliomas and medulloblastoma.

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.[Pubmed:17975007]

Mol Pharmacol. 2008 Feb;73(2):338-48.

JNJ-28871063 is a potent and highly selective pan-ErbB kinase inhibitor from a novel aminopyrimidine oxime structural class that blocks the proliferation of epidermal growth factor receptor (EGFR; ErbB1)- and ErbB2-overexpressing cells but does not affect the growth of non-ErbB-overexpressing cells. 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. A single dose of compound reduced phosphorylation of ErbB2 receptors in tumor-bearing mice, demonstrating target suppression in vivo. Tissue distribution studies show that JNJ-28871063 crosses the blood-brain barrier and penetrates into tumors, where it is able to accumulate to higher levels than those found in the plasma. JNJ-28871063 showed oral antitumor activity in human tumor xenograft models that overexpress EGFR and ErbB2. In an intracranial ErbB2-overexpressing tumor model, JNJ-28871063 extended survival relative to untreated animals. The brain is a primary site of metastasis for EGFR-overexpressing lung cancers and ErbB2-overexpressing breast cancers. Therefore, the ability to penetrate into the brain could be an advantage over existing therapies such as trastuzumab (Herceptin) and cetuximab (Erbitux), which are antibodies and do not cross the blood-brain barrier. These results show that JNJ-28871063 is orally bioavailable, has activity against EGFR and ErbB2-dependent tumor xenografts, and can penetrate into the brain and inhibit ErbB2-overexpressing tumor growth.

Keywords:

JNJ 28871063 hydrochloride,944342-90-9,Natural Products,EGFR, buy JNJ 28871063 hydrochloride , JNJ 28871063 hydrochloride supplier , purchase JNJ 28871063 hydrochloride , JNJ 28871063 hydrochloride cost , JNJ 28871063 hydrochloride manufacturer , order JNJ 28871063 hydrochloride , high purity JNJ 28871063 hydrochloride

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: