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J-4567 JNJ-10198409, Free Base, >99%      NEW!

Synonyms:  [PDGF Receptor Tyrosine Kinase Inhibitor IV] [RWJ-540973] [RWJ 540973] [RWJ540973]

M.W. 325.34

C18H16FN3O2

[627518-40-5]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO.  Disposal:  A

Find and View a Certificate of Analysis for this product

View the MSDS for this product

• JNJ-10198409, also known as RWJ 540973, is a potent inhibitor of platelet-derived growth factor receptor tyrosine kinase (PDGF-RTK).

• JNJ-10198409 has anti-PDGFR-β kinase activity with an IC50 of 4.2 nM and potent antiproliferative activity in six of eight human tumor cell lines, with IC50 values of less than 33 nM.  Ho, C.Y., et al.  "(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines:  platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells."  J. Med. Chem. 48:  8163-8173 (2005).

• The in vivo inhibitory effect of JNJ-10198409 on PDGF-RTK was confirmed in tumor tissues after administering the compound orally in a nude mouse xenograft model of human LoVo colon cancer.  D'Andrea, M.R., et al.  "Validation of in vivo pharmacodynamic activity of a novel PDGF receptor tyrosine kinase inhibitor using immunohistochemistry and quantitative image analysis."  Mol. Cancer Ther. 4:  1198-1204 (2005).

• Multiple UDP-glucuronosyltransferase 1A enzymes are responsible for the glucuronidation of JNJ-10198409 in human liver microsomes.  Yan, Z., et al.  "N-glucuronidation of the platelet-derived growth factor receptor tyrosine kinase inhibitor 6,7-(dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)-(3-fluoro-phenyl)-amine by human UDP-glucuronosyltransferases."  Drug Metab Dispos 34:  748-755 (2006).

• JNJ-10198409 demonstrated potent anti-proliferative activities against human leukemia cells K562 and SUP-B15.  It induced cell apoptosis concentration-dependently while the remaining viable cells demonstrated G2/M cell cycle arrest.  Using K562 growing as a solid tumor in nude mice, JNJ-10198409 caused dose-dependent inhibition of tumor growth without overt toxicity in vivo.  Mei, J., et al.  "A novel PDGFR kinase, c-ABL and c-Kit inhibitor with unique anti-proliferative activity inducing specific cell cycle dysregulation in human leukemia cells "  Proc. Amer. Assoc. Cancer Res. 45:  Abstract #5982 (2005).

• JNJ-10198409 has both anti-angiogenesis and tumor cell anti-proliferative activities.  Mei, J., et al.  "A novel PDGF receptor tyrosine kinase inhibitor with dual anti-angiogenesis and tumor cell anti-proliferative activity."  Proc. Amer. Assoc. Cancer Res. 45:  Abstract #3990 (2004).  Tuman R., et al.  "Discovery of a novel, dual mechanism anti-angiogenic and anti-proliferative agent with oral anti-tumor activity."  Proc. Amer. Assoc. Cancer Res. 45:  Abstract #4558 (2004).

• JNJ-10198409 selectively inhibited neuroblastoma cell growth in alamarBlue® assays and rapidly induced neuroblastoma cell apoptosis without affecting the growth of primary pediatric neural crest-like stem cells.  It may function by inhibiting the activity of Src family kinases.  Fujitani, M., et al.  "Potent and selective cytotoxic and cytostatic activity of JNJ-10198409 against neuroblastoma cells."  Chiba Medical J. 88E:  27-34 (2012).

• As of October 2012, it appears that Chemical Abstracts Service is erroneously using the name "JNJ-10198409" for CAS number 627512-69-0.  The structure that Chemical Abstracts Service shows for CAS number 627512-69-0 is actually a double-bond tautomer of JNJ-10198409, according to J. Med. Chem. 48:  8163-8173 (2005).  This is the publication that describes the discovery of JNJ-10198409 and in which the CAS number 627518-40-5 is specifically assigned to the correct structure for JNJ-10198409.  Thus, it appears that the correct CAS number for the correct structure is 627518-40-5, as appears near the top of this product entry.

• Another CAS number previously assigned to this product, namely 872872-33-8 has been deleted by CAS and is no longer in use.

• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.

** Our prices are lower than other vendors', but there is no compromise in quality.  Read how we are able to accomplish this:  Product Quality Discussion.

NOTES:
1.  The purpose of our competitor price comparison tables is to enable our visitors to compare the prices and purities of products of nominally equivalent quality, for vendors whose price and purity claims are openly available from a website or catalog (without a need for the customer to contact the vendor and request a quotation in order to obtain a price and purity for a standard product size).  However, the quality comparisons in these tables are not absolute:  although our product purities are uniformly very high and are established by careful testing of every lot in our laboratories, we cannot and do not vouch for the purities claimed by other vendors in these competitor price comparison tables.  (We do carry out occasional testing of other vendors' products -- see below --  and we have found many instances where vendors' product purities are far below their claimed levels.)  Effective April 1, 2011, our price comparison tables only include products where a purity commitment is found together with sizes and prices on at least one page of the vendor's web site.

2.  Researching and compiling sizes and prices for the >160 competitive vendors and more than 175 products is an expensive and tedious task for our small company.  Thus, we typically only perform revisions of these tables annually or less frequently.  The date and source of each competitive vendor's prices is indicated at the bottom of this page.  Obviously, we make no guarantee that competitive vendor prices will remain unchanged in the interval between our annual revisions.  We may occasionally update individual competitive vendor information and add new competitive vendors as we locate them.

3.  In some circumstances we permanently remove vendors from our price comparison tables.  Circumstances that lead to permanent removal are: 

A.  If a vendor does not honor its advertised price (ignoring small price increases) for one or more products when an order is attempted.  Example:  a vendor listed a compound at $808 for 10 grams on its website price list, but quoted $4,500 per 10 grams upon our inquiry.  That vendor has been permanently removed from our price comparison tables.

B.  If, on a product-by-product basis, our analyses of a vendor's product show purities more than a few percent below the vendor's advertised purities.  Example:  a vendor advertises a purity for 97% for a compound, but repeated elemental analyses show a minimum of 9% inorganic material present, beyond any salt counterion.  Another example: an HPLC analysis at a relevant UV detector wavelength shows 92% purity for a vendor's product for which 98% purity is claimed.  We realize of course that UV absorbances for impurities can be higher than for the main compound, but our products meet our purity commitment of typically >99% irrespective of absorbance factors for impurities, and we apply that standard to products from other vendors.

C.  Again on a product-by-product basis, if a vendor makes no purity claim for a given product, then their product is not shown on that product table.

D.  If we find that, as a pattern, several of a competitive vendor's products fail to meet their advertised purity commitments by significant margins or if a vendor does not provide standard and consistent purity claims for several of its products, then that vendor is permanently removed from all of our competitor price tables.

E.  Finally, if we determine that a vendor has provided fraudulent information on its website, in its literature or on a certificate of analysis, that vendor is permanently removed from all of our price comparison tables.

4.  IMPORTANT:  The presence of a competitive vendor entry in our price comparison tables does not necessarily mean that we have analyzed any of that vendor's products for purity; indeed, in most cases we have not.

5.  Please note:  where necessary, competitor prices are rounded to the nearest whole dollar.

To the best of our knowledge, the prices listed above for our competitors' products were correct as of the dates listed below for the sources of our annual price information update process.

Pricing Sources and Dates:  LC Labs - Current, EMD Chemicals - website - Jan 2013, Sigma-Aldrich - website - Jan 2013, Santa Cruz Biotech - website - Jan 2013, Cayman Chemical - website - Dec 2012, Cambridge BioScience - website - Oct 2012, Chemdea - website - Dec 2012, Krackeler Scientific - website - Jan 2013, Sapphire North America - website - Apr 2013.