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Enzastaurin (LY317615)

PKCβ isozyme selective inhibitor

Enzastaurin (LY317615)

Catalog No. A1670
Size Price Stock Qty
Evaluation Sample $28.00  All Inclusive In stock
5mg $50.00 In stock
25mg $120.00 In stock
100mg $360.00 In stock

All inclusive: Shipping and all other fees included

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Enzastaurin (LY317615)

Related Biological Data

Enzastaurin (LY317615)

Related Biological Data

Enzastaurin (LY317615)

Biological Activity

Description Enzastaurin (LY317615) is a potent and selective inhibitor of PKCβ with IC50 of 6 nM.
Targets PKCβ PKCα PKCγ PKCε    
IC50 6 nM 39 nM 83 nM 110 nM    

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Chemical Properties

Cas No. 170364-57-5 SDF Download SDF
Chemical Name 3-(1-methylindol-3-yl)-4-[1-[1-(pyridin-2-ylmethyl)piperidin-4-yl]indol-3-yl]pyrrole-2,5-dione
Canonical 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
Formula C32H29N5O2 M.Wt 515.61
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Research Update

1. A randomized, double-blind, placebo-controlled, Phase II study with and without enzastaurin in combination with docetaxel-based chemotherapy in patients with castration-resistant metastatic prostate cancer. Invest New Drugs. 2013 Aug;31(4):1044-50. doi: 10.1007/s10637-013-9940-0. Epub 2013 Feb 24.
Abstract
The efficacy of docetaxel/prednisone with or without enzastaurin, an inhibitor of the beta isoform of protein kinase C with therapeutic activity against prostate cancer, in patients with castration-resistant metastatic prostate cancer has been explored.
2. The serine-threonine kinase p90RSK is a new target of enzastaurin in follicular lymphoma cells. Br J Pharmacol. 2013 Dec;170(7):1374-83. doi: 10.1111/bph.12351.
Abstract
Follicular lymphoma cells are characterized not only by genetic alterations involving Bcl-2, Bcl-6 OR C-mYc but also by alterations in B-cell receptor signaling pathways.
4. Phase I study of enzastaurin and bevacizumab in patients with advanced cancer: safety, efficacy and pharmacokinetics. Invest New Drugs. 2013 Jun;31(3):653-60. doi: 10.1007/s10637-012-9850-6. Epub 2012 Jul 6.
Abstract
The combination of enzastaurin and bevacizumab, which showed synergistic antitumor activity in preclinical studies, was evaluated for safety and efficacy.
5. A double-blind, randomized, placebo-controlled, phase 2 study of maintenance enzastaurin with 5-fluorouracil/leucovorin plus bevacizumab after first-line therapy for metastatic colorectal cancer. Cancer. 2012 Sep 1;118(17):4132-8. doi: 10.1002/cncr.26692. Epub 2011 Dec 27.
Abstract
Enzastaurin with 5-fluorouracil/leucovorin plus bevacizumab was evaluated as maintance therapy for MCRC, since the combination of enzastaurin and bevacizumab was well-tolerated and demonstrated synergistic antitumor effects in phse 1 studies.

Background

Enzastaurin (LY317615) is a potent PKC beta inhibitor for PKCβ, PKCα, PKCγ and PKCε with IC50 of 6 nM, 39 nM, 83 nM and 110 nM, respectively. Enzastaurin inhibits growth in all MM cell lines investigated, including MM.1S, MM.1R, RPMI 8226 (RPMI), RPMI-Dox