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Synkinase Newsletter Jan 2013_VEGFR

It was reported that AVEO Oncology and Astellas Pharma have begun enrolling patients with advanced triple negative breast cancer in the third study for Tivozanib (AV-951). This double-blind, multicenter trial led by AVEO is designed to assess the efficacy profile of tivozanib combination therapy with paclitaxel against placebo combination therapy with paclitaxel in advanced or metastatic breast cancer (mBC) patients. The study is also designed to assess the potential tumor biomarkers that possibly respond to tivozanib in triple negative breast cancer patients.************************************************************************** Tivozanib (AV-951) is a selective and potent and oral VEGFR inhibitor with quinoline-urea moiety. It inhibits VEGFR1, VEGFR2 and VEGFR3 with IC50 at 0.21 nM, 0.16 nM and 0.24 nM, respectively. Tivozanib blocks VEGF-dependent activation of mitogen-activated protein kinases and proliferation of endothelial cells. *************************** ********************************************************* Synkinase (www.synkinase.com) supplies the most comprehensive collection of recently disclosed VEGFR inhibitors such as Tivozanib, Brivanib, Brivanib Alanilate, Cabozantinib, Dovitinib, Indetanib, Lilifanib, Motesanib, Orantinib (SU-6668), Ponatinib, Pozapanib, Regorafenib, Sorafenib, Vandetanib, AG13958, E7080, JNJ-38158471, SAR131675, SU-5402, and XL880. All of the kinase inhibitors listed on our website are in stock and can be delivered within 1-3 days. Please visit www.synkinase.com or contact service@synkinase.com for any inquiries or orders@synkinase.com for any ordering process.

Date:2013-01-04

SynKinase Newsletter: December 12 2012

A kinase interaction map profiling the activity of 178 commercially available kinase inhibitors against a panel of 300 recombinant kinases from over 100,00 independent functional assays was recently reported in Nature Biotechnology 29, 1039-1045, 2011 (doi: 10.1038/nbt.2017) by Jeffrey R. Peterson, Ph.D., and colleagues at the Fox Chase Cancer Center. ********************************************************************************************** Protein kinases represent important therapeutic targets because of their key roles in cell signaling, but designing selective inhibitors has been a challenge. Owing to evolutionary conservation of the ATP-binding site, which represents a useful target epitope for most kinase inhibitors, individual inhibitors are likely to promiscuously inhibit multiple kinases. This report revealed complex and often unexpected interactions between protein kinases and kinase inhibitors, with a wide spectrum of promiscuity. Many off-target interactions occur with seemingly unrelated kinases, revealing how large-scale profiling can identify multitargeted inhibitors of specific, diverse kinases. This finding has a remarkable impact on drug discovery and development in kinase area, as current selectivity assessment of newly identified kinase inhibitors is often carried out by testing against a limited panel of closely related kinases, based on the assumption that any off-target inter¬actions that occur will most likely impact on kinases with similar amino acid sequence. The results from this report provide a resource for selecting compounds to elucidate kinase function and for interpreting the results of experiments involving kinase inhibitors. ******************************************************* ********************************** Full text is available at: http://www.nature.com/nbt/journal/v29/n11/abs/nbt.2017.html

Date:2012-12-11

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Synkinase has opened a warehouse in San Diego California. We will provide next day delivery. Call 1-887-854-6273 to place your order today.

Date:2012-12-11

SynKinase Newsletter in November 2012: Kinase Inhibitor Selectivity

Protein kinases represent the most important classes of therapeutic targets because of their pivotal roles in virtually all aspects of cellular physiology. However, most of small molecule kinase inhibitors interact with multiple member of the protein kinase family, achieving highly selective kinase inhibition is challenging. ********************** ******************************************************* ************************************ Recently, Davis and collegues at Ambit and DiscoverX tested the interaction of 72 kinase inhibitors with 442 kinases (Nature Biotechnology 29, 1046-1052, 2011 (doi: 10.1038/nbt.1990). Their data showed that, as a class, Type II inhibitors – which bind adjacently to the region occupied by ATP and prefer an inactive kinase conformation – are more selective than Type I inhibitors – which target the ATP binding site of the kinase in its active conformation. But they also found a few individual Type I inhibitors are among the most selective identified so far. Their data also demonstrated that selective inhibitors have been developed against the majority of kinase targeted by the compounds tested. Furthermore, they identified a class of “group-selective” inhibitors are broadly active against a single subfamily of kinases, but selective outside that subfamily. The data set suggests compounds to use as tools to study kinase for which no dedicated inhibitors exist. This paper provides information that can aid the identification of selective kinase inhibitors for use as tool compounds, and assist in kinase inhibitor drug discovery. ******* **************************************************** **************************** ***************************************************** *********** As one of the kinase inhibitors suppliers for this work, Synkinase (www.synkinase.com) has in stock more than 160 of recently disclosed small molecule kinase inhibitors, which include type I, type II and type III inhibitors. All of the kinase inhibitors listed on our website can be delivered within 1-3 days. We also supply a kinase array which consists of 96 kinase inhibitors at 0.5mg or 1mg in standard 96-well plate; or we can customize the kinase plate according to your research needs. Please visit www.synkinase.com or enquire service@synkinase.com for more information.

Date:2012-08-23

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