Enzastaurin

Key Product Details

Product Description

Enzastaurin is a potent PKCβ inhibitor (IC₅₀ values are 6, 39, 83 and 110 nM for PKCβ, PKCα, PKCγ and PKCε, respectively). Suppresses proliferation and induces apoptosis in HCT116 colon carcinoma and U87MG glioblastoma cells in vitro. Reduces tumor growth and exhibits antiangiogenic activity in HT-29 colon carcinoma xenografts in mice. Also suppresses growth of HCT116 and U87MG xenografts in mice. Orally active.

Product Specifications for Enzastaurin

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for Enzastaurin

The following data is based on the product molecular weight 515.60.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.2 mM	9.70 mL	48.49 mL	96.97 mL
1 mM	1.94 mL	9.70 mL	19.39 mL
2 mM	0.97 mL	4.85 mL	9.70 mL
10 mM	0.19 mL	0.97 mL	1.94 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Graff The protein kinase Cβ-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 PMID: 16103100
• Teicher Antiangiogenic and antitumor effects of a protein kinase Cβ inhibitor in human HT-29 colon carcinoma and human CaKi1 renal cell carcinoma xenografts. Anticancer Res. 2001 PMID: 11848470

Product Documents for Enzastaurin