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Enzastaurin

Cat. No. M1704
Enzastaurin Structure
Synonym:

LY317615

Size Price Availability Quantity
10mg USD 85 In stock
50mg USD 230 In stock
100mg USD 355 In stock
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Quality Control
Biological Activity

Enzastaurin inhibits PKCβ, PKCα, PKCγ and PKCε with IC50's of 0.006, 0.039, 0.083 and 0.110 µM, respectively. Enzastaurin apparently inhibits tumor growth via multiple mechanisms: suppression of tumor cell proliferation, induction of tumor cell apoptosis and inhibition of tumor-induced angiogenesis.

Protocol
Cell Experiment
Cell lines PC-3 prostate cancer, HCT116 colon cancer, and U87MG glioblastoma cell lines
Preparation method Proliferation assays. Proliferation was assessed for all cell lines over a 6-day time course in media supplemented with 1% FBS (7 days total). Briefly, 1,000 cells were plated per well in a 96-well plate and changed to fresh media (1% FBS) with or without enzastaurin on days 1 and 4. On day 7, the media were removed and 100 μL propidium iodide (PI) solution (10 μg/mL in D-PBS) were added to each well. An initial reading for PI staining (excitation at 500 nmol/L, absorbance at 615 nmol/L) was done using the WallacVictor plate reader following a 30-minute incubation to determine the nonviable cell fraction. The plate was then frozen at −80 °C for 2 hours, thawed, and reread. The proliferative index was scored by subtracting the prefreeze data (nonviable cells) from the postfreeze data (all cells).
Concentrations 0~10µM
Incubation time 6 days
Animal Experiment
Animal models Athymic nude mice bearing HCT116 colon cancer xenografts
Formulation 10% acacia (Fisher Scientific, Fair Lawn, NJ) in water
Dosages twice daily at 75 mg/kg
Administration gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 515.61
Formula C32H29N5O2
CAS Number 170364-57-5
Purity 99.05%
Solubility DMSO
Storage at -20°C
References

A placebo-controlled, randomized phase II study of maintenance enzastaurin following whole brain radiation therapy in the treatment of brain metastases from lung cancer.
Grønberg et al. Lung Cancer. 2012 Aug 20. PMID: 22917813.

A Multicenter Phase II Study of Single-Agent Enzastaurin in Previously Treated Waldenstrom Macroglobulinemia.
Ghobrial et al. Clin Cancer Res. 2012 Aug 28. PMID: 22879385.

A phase II study of enzastaurin in combination with erlotinib in patients with previously treated advanced non-small cell lung cancer.
Clément-Duchêne et al. Lung Cancer. 2012 Jul 16. PMID: 22809813.

Phase I study of enzastaurin and bevacizumab in patients with advanced cancer: safety, efficacy and pharmacokinetics.
Nwankwo et al. Invest New Drugs. 2012 Jul 6. PMID: 22766773.

Combination of low doses of Enzastaurin and Lenalidomide has synergistic activity in B-non-Hodgkin lymphoma cell lines.
Cosenza et al. Ann Hematol. 2012 Oct;91(10):1613-22. PMID: 22623160.

Enzastaurin has anti-tumour effects in lung cancers with overexpressed JAK pathway molecules.
Shimokawa et al. Br J Cancer. 2012 Feb 28;106(5):867-75. PMID: 22333600.

A phase I study of LY317615 (enzastaurin) and temozolomide in patients with gliomas (EORTC trial 26054).
Rampling et al. Neuro Oncol. 2012 Mar;14(3):344-50. PMID: 22291006.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Enzastaurin, LY317615 supplier, PKC, inhibitors

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