For research use only. Not for therapeutic Use.
Enzastaurin (LY317615)（Cat No.:I002225）is an oral serine/threonine kinase inhibitor that primarily targets protein kinase C (PKC) and the phosphatidylinositol 3-kinase (PI3K) signaling pathway. By inhibiting these pathways, enzastaurin disrupts cell growth, survival, and angiogenesis in various cancer types. It has shown potential in clinical studies, particularly in treating hematologic malignancies and solid tumors, often in combination with other therapies. Enzastaurin’s ability to modulate critical signaling networks makes it a valuable compound for research into targeted cancer therapies, with ongoing investigations into its efficacy and safety profiles.
| Catalog Number | I002225 |
| CAS Number | 170364-57-5 |
| Synonyms | 3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione |
| Molecular Formula | C₃₂H₂₉N₅O₂ |
| Purity | ≥95% |
| Target | TGF-beta/Smad |
| Solubility | DMSO ≥47mg/mL Water <1.2mg/mL Ethanol <1.2mg/mL |
| Storage | 3 years -20C powder |
| IC50 | 6 nM [1] |
| IUPAC Name | 3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione |
| InChI | InChI=1S/C32H29N5O2/c1-35-19-25(23-9-2-4-11-27(23)35)29-30(32(39)34-31(29)38)26-20-37(28-12-5-3-10-24(26)28)22-13-16-36(17-14-22)18-21-8-6-7-15-33-21/h2-12,15,19-20,22H,13-14,16-18H2,1H3,(H,34,38,39) |
| InChIKey | AXRCEOKUDYDWLF-UHFFFAOYSA-N |
| SMILES | CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CN(C5=CC=CC=C54)C6CCN(CC6)CC7=CC=CC=N7 |
| Reference | </br>1:Molecular mechanism underlying the pharmacological interactions of the protein kinase C-β inhibitor enzastaurin and erlotinib in non-small cell lung cancer cells. Steen NV, Potze L, Giovannetti E, Cavazzoni A, Ruijtenbeek R, Rolfo C, Pauwels P, Peters GJ.Am J Cancer Res. 2017 Apr 1;7(4):816-830. eCollection 2017. PMID: 28469955 Free PMC Article</br>2:Enzastaurin: A lesson in drug development. Bourhill T, Narendran A, Johnston RN.Crit Rev Oncol Hematol. 2017 Apr;112:72-79. doi: 10.1016/j.critrevonc.2017.02.003. Epub 2017 Feb 11. Review. PMID: 28325267 </br>3:Randomized, Double-Blind, Phase III Trial of Enzastaurin Versus Placebo in Patients Achieving Remission After First-Line Therapy for High-Risk Diffuse Large B-Cell Lymphoma. Crump M, Leppä S, Fayad L, Lee JJ, Di Rocco A, Ogura M, Hagberg H, Schnell F, Rifkin R, Mackensen A, Offner F, Pinter-Brown L, Smith S, Tobinai K, Yeh SP, Hsi ED, Nguyen T, Shi P, Hahka-Kemppinen M, Thornton D, Lin B, Kahl B, Schmitz N, Savage KJ, Habermann T.J Clin Oncol. 2016 Jul 20;34(21):2484-92. doi: 10.1200/JCO.2015.65.7171. Epub 2016 May 23. PMID: 27217449 </br>4:A pharmacokinetic and safety study of a fixed oral dose of enzastaurin HCl in native Chinese patients with refractory solid tumors and lymphoma. Li X, Fang X, Li S, Zhang W, Yang N, Cui Y, Huang H, Cai R, Lin X, Fu X, Hong H, Lin T.Oncotarget. 2016 Apr 5;7(14):18585-93. doi: 10.18632/oncotarget.7875. PMID: 26942463 Free PMC Article</br>5:A phase II trial of enzastaurin (LY317615) in combination with bevacizumab in adults with recurrent malignant gliomas. Odia Y, Iwamoto FM, Moustakas A, Fraum TJ, Salgado CA, Li A, Kreisl TN, Sul J, Butman JA, Fine HA.J Neurooncol. 2016 Mar;127(1):127-35. doi: 10.1007/s11060-015-2020-x. Epub 2015 Dec 7. PMID: 26643807 </br>6:Effects of enzastaurin and its metabolites on the QT interval in cancer patients. Welch PA, Ng WT, Darstein CL, Musib L, Lesimple T.J Clin Pharmacol. 2016 Jan;56(1):101-8. doi: 10.1002/jcph.573. Epub 2015 Aug 17. PMID: 26096682 </br>7:The potential of enzastaurin to enhance platelet aggregation and growth factor secretion: implications for cancer cell survival. Lesyk G, Fong T, Ruvolo PP, Jurasz P.J Thromb Haemost. 2015 Aug;13(8):1514-20. doi: 10.1111/jth.13010. Epub 2015 Jun 17. PMID: 25990653 </br>8:A randomized, phase 2 study of R-CHOP plus enzastaurin vs R-CHOP in patients with intermediate- or high-risk diffuse large B-cell lymphoma. Hainsworth JD, Arrowsmith ER, McCleod M, Hsi ED, Hamid O, Shi P, Lin BK, Fayad LE.Leuk Lymphoma. 2016;57(1):216-8. doi: 10.3109/10428194.2015.1045898. Epub 2015 Oct 5. No abstract available. PMID: 25956042 </br>9:Enzastaurin inhibits ABCB1-mediated drug efflux independently of effects on protein kinase C signalling and the cellular p53 status. Michaelis M, Rothweiler F, Löschmann N, Sharifi M, Ghafourian T, Cinatl J Jr.Oncotarget. 2015 Jul 10;6(19):17605-20. PMID: 25749379 Free PMC Article</br>10:Protein kinase C β inhibition by enzastaurin leads to mitotic missegregation and preferential cytotoxicity toward colorectal cancer cells with chromosomal instability (CIN). Ouaret D, Larsen AK.Cell Cycle. 2014;13(17):2697-706. doi: 10.4161/15384101.2015.945383. PMID: 25486357 Free PMC Article |
