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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Enzastaurin (formerly known as LY317615; DB-102; DB102 and LY-317615) is a novel, potent, and selective inhibitor of PKCβ (Protein kinase C) with potential antitumor activity. It inhibits PKCβ with an IC50 of 6 nM in cell-free assays, and exhibits 6- to 20-fold selectivity against PKCα, PKCγ and PKCε. Enzastaurin is a synthetic macrocyclic bisindolemaleimide with potential antineoplastic activity. Enzastaurin binds to the ATP-binding site and selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis. It can decrease tumor blood supply and so tumor burden.
| ln Vitro |
When enzaturin (LY317615) is applied, all MM cell lines studied—MM.1S, MM.1R, RPMI 8226 (RPMI), RPMI-Dox40 (Dox40), NCI-H929, KMS-11, OPM-2, and U266—show a significant dose-dependent reduction of growth, with an IC50 ranging from 0.6 to 1.6 μM. Enzastaurin directly affects human tumor cells by causing apoptosis and inhibiting their growth in tumor cells that have been cultivated. Enzastaurin does not directly affect the phosphorylation of VEGFR, but it does inhibit the phosphorylation of GSK3βser9, ribosomal protein S6S240/244, and AKTThr308[1]. When it comes to CTCL malignant lymphocytes, ezastaurin accelerates apoptosis. In combination with GSK3 inhibitors, enzastaurin exhibits increased levels of cytotoxicity. Elevated levels of β-catenin total protein and β-catenin-mediated transcription are observed after treatment with enzastaurin and the GSK3 inhibitor AR-A014418. Similar to enzastaurin with AR-A014418, blocking β-catenin-mediated transcription or β-catenin small hairpin RNA (shRNA) knockdown results in harmful effects. Furthermore, enzastaurin and AR-A014418 therapy reduces CD44's surface expression and mRNA levels[2].
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| ln Vivo |
When radiation and ezastaurin are applied to xenografts, the density of microvessels is reduced more than when each treatment is applied alone. Tumor growth is postponed when microvessel density decreases[3].
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| References |
[1]. Graff JR, et al. The protein kinase Cbeta-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts. Cancer Res, 2005, 65(16),
[2]. Rovedo MA, et al. Inhibition of glycogen synthase kinase-3 increases the cytotoxicity of enzastaurin. J Invest Dermatol, 2011, 131(7), 1442-1449. [3]. Podar K, et al. Targeting PKC in multiple myeloma: in vitro and in vivo effects of the novel, orally available small-molecule inhibitor enzastaurin (LY317615.HCl). Blood, 2007, 109(4), 1669-1677 |
| Molecular Formula |
C32H29N5O2
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| Molecular Weight |
515.61
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| CAS # |
170364-57-5
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| Related CAS # |
170364-57-5; 359017-79-1 (HCl);365253-37-8 (2HCl);
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| SMILES |
O=C(C(C1=CN(C)C2=C1C=CC=C2)=C3C4=CN(C5CCN(CC6=NC=CC=C6)CC5)C7=C4C=CC=C7)NC3=O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9395 mL | 9.6973 mL | 19.3945 mL | |
| 5 mM | 0.3879 mL | 1.9395 mL | 3.8789 mL | |
| 10 mM | 0.1939 mL | 0.9697 mL | 1.9395 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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