Enzastaurin - CAS 170364-57-5
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Not Intended for Therapeutic Use. For research use only.
Enzastaurin HCL is the hydrochloride salt of enzastaurin, a synthetic macrocyclic bisindolemaleimide with potential antineoplastic activity. Binding to the ATP-binding site, enzastaurin selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply and so tumor burden.
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Enzastaurin HCl; Enzastaurin Hydrochloride; LY317615; LY-317615; D04014; LY 317615.
Current Developer:
Eli Lilly Inc
1.A phase II trial of enzastaurin (LY317615) in combination with bevacizumab in adults with recurrent malignant gliomas.
Odia Y1, Iwamoto FM2, Moustakas A3, Fraum TJ4, Salgado CA5, Li A6, Kreisl TN2, Sul J7, Butman JA8, Fine HA9. J Neurooncol. 2016 Mar;127(1):127-35. doi: 10.1007/s11060-015-2020-x. Epub 2015 Dec 7.
We evaluated the efficacy of combination enzastaurin (LY317615) and bevacizumab for recurrent malignant gliomas and explored serologic correlates. We enrolled 81 patients with glioblastomas (GBM, n = 40) and anaplastic gliomas (AG, n = 41). Patients received enzastaurin as a loading dose of 1125 mg, followed by 500 or 875 mg daily for patients on non-enzyme-inducing or enzyme-inducing antiepileptics, respectively. Patients received bevacizumab 10 mg/kg intravenously biweekly. Clinical evaluations were repeated every 4 weeks. Magnetic resonance imaging was obtained at baseline and every 8 weeks from treatment onset. Phosphorylated glycogen synthase kinase (GSK)-3 levels from peripheral blood mononuclear cells (PBMCs) were checked with each MRI. Median overall survival was 7.5 and 12.4 months for glioblastomas and anaplastic glioma cohorts, with median progression-free survivals of 2.0 and 4.4 months, respectively. Of GBM patients, 3/40 (7.
2.A deleterious gene-by-environment interaction imposed by calcium channel blockers in Marfan syndrome.
Doyle JJ1,2, Doyle AJ1,3, Wilson NK1, Habashi JP1,4, Bedja D5,6, Whitworth RE7, Lindsay ME8, Schoenhoff F9,10, Myers L1, Huso N1, Bachir S1, Squires O1, Rusholme B1, Ehsan H2, Huso D11, Thomas CJ12, Caulfield MJ3, Van Eyk JE10, Judge DP13, Dietz HC1,4,13; Elife. 2015 Oct 27;4. pii: e08648. doi: 10.7554/eLife.08648.
Calcium channel blockers (CCBs) are prescribed to patients with Marfan syndrome for prophylaxis against aortic aneurysm progression, despite limited evidence for their efficacy and safety in the disorder. Unexpectedly, Marfan mice treated with CCBs show accelerated aneurysm expansion, rupture, and premature lethality. This effect is both extracellular signal-regulated kinase (ERK1/2) dependent and angiotensin-II type 1 receptor (AT1R) dependent. We have identified protein kinase C beta (PKCβ) as a critical mediator of this pathway and demonstrate that the PKCβ inhibitor enzastaurin, and the clinically available anti-hypertensive agent hydralazine, both normalize aortic growth in Marfan mice, in association with reduced PKCβ and ERK1/2 activation. Furthermore, patients with Marfan syndrome and other forms of inherited thoracic aortic aneurysm taking CCBs display increased risk of aortic dissection and need for aortic surgery, compared to patients on other antihypertensive agents.
3.PKCβ Inhibitors Attenuate Amphetamine-Stimulated Dopamine Efflux.
Zestos AG1,2, Mikelman SR1, Kennedy RT1,2, Gnegy ME1. ACS Chem Neurosci. 2016 Mar 28. [Epub ahead of print]
Amphetamine abuse afflicts over 13 million people, and there is currently no universally accepted treatment for amphetamine addiction. Amphetamine serves as a substrate for the dopamine transporter and reverses the transporter to cause an increase in extracellular dopamine. Activation of the beta subunit of protein kinase C (PKCβ) enhances extracellular dopamine in the presence of amphetamine by facilitating the reverse transport of dopamine and internalizing the D2 autoreceptor. We previously demonstrated that PKCβ inhibitors block amphetamine-stimulated dopamine efflux in synaptosomes from rat striatum in vitro. In this study, we utilized in vivo microdialysis in live, behaving rats to assess the effect of the PKCβ inhibitors, enzastaurin and ruboxistaurin, on amphetamine-stimulated locomotion and increases in monoamines and their metabolites. A 30 min perfusion of the nucleus accumbens core with 1 μM enzastaurin or 1 μM ruboxistaurin reduced efflux of dopamine and its metabolite 3-methoxytyramine induced by amphetamine by approximately 50%.
4.Long chain n-3 polyunsaturated fatty acids increase the efficacy of docetaxel in mammary cancer cells by downregulating Akt and PKCε/δ-induced ERK pathways.
Chauvin L1, Goupille C2, Blanc C1, Pinault M1, Domingo I1, Guimaraes C1, Bougnoux P2, Chevalier S3, Mahéo K4. Biochim Biophys Acta. 2016 Apr;1864(4):380-90. doi: 10.1016/j.bbalip.2016.01.012. Epub 2016 Jan 26.
Taxanes can induce drug resistance by increasing signaling pathways such as PI3K/Akt and ERK, which promote survival and cell growth in human cancer cells. We have previously shown that long chain n-3 polyunsaturated fatty acids, such as docosahexaenoic acid (DHA, 22:6n-3) decrease resistance of experimental mammary tumors to anticancer drugs. Our objective was to determine whether DHA could increase tumor sensitivity to docetaxel by down-regulating these survival pathways. In docetaxel-treated MDA-MB-231 cells, phosphorylated-ERK1/2 levels were increased by 60% in membrane and nuclear compartments, compared to untreated cells. Our data showed that ERK1/2 activation depended on PKC activation since: i) enzastaurin (a pan-PKC inhibitor) blocked docetaxel-induced ERK1/2 phosphorylation ii) docetaxel increased PKC activity by 30% and phosphatidic acid level by 1.6-fold iii) inhibition of PKCε and PKCδ by siRNA resulted in reduced phosphorylated ERK1/2 levels.
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CAS 170364-57-5 Enzastaurin

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