JNJ-10198409, Free Base (PDGF Receptor Tyrosine Kinase Inhibitor IV, RWJ 540973, CAS 627518-40-5), >99%

LC Laboratories' Product Number J-4567 - JNJ-10198409, Free Base (PDGF Receptor Tyrosine Kinase Inhibitor IV, RWJ 540973, CAS 627518-40-5), >99% - for research use only. 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. 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. Multiple UDP-glucuronosyltransferase 1A enzymes are responsible for the glucuronidation of JNJ-10198409 in human liver microsomes. 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. JNJ-10198409 has both anti-angiogenesis and tumor cell anti-proliferative activities. 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. 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. Another CAS number previously assigned to this product, namely 872872-33-8 has been deleted by CAS and is no longer in use.

• Supplier: LC Laboratories
• Product #: J-4567
• Sku #: J-4567_5mg