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E-4506 Enzastaurin, Free Base, >99%

[LY-317615] [D04014] [LY 317615] [LY317615]

M.W. 515.60

C32H29N5O2

[170364-57-5]

M.I. 14:  10293

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO at 7.1 mg/mL with warming; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 1-10 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility.  Disposal:  A

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• 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. Graff, J.R., et al.  "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. 65:  7462-7469 (2005).

• Enzastaurin induces apoptosis in multiple myeloma (MM) cell lines by inhibiting signaling through the AKT pathway, which is caspase-independent.  Rizvi, M.A., et al.  "Enzastaurin (LY317615), a protein kinase Cβ inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines."  Mol. Cancer Ther. 5:  1783-1789 (2006).

• Enzastaurin has an antitumor effect on Waldenström macroglobulinemia both in vitro and in vivo.  Moreau, A.S., et al.  "Protein kinase C inhibitor enzastaurin induces in vitro and in vivo antitumor activity in Waldenström macroglobulinemia."  Blood 109:  4964-4972 (2007).

• Enzastaurin enhances the antiangiogenic effects of radiation by radiosensitizing human endothelial cells in pancreatic cancer xenografts.  Spalding, A.C., et al.  "Enzastaurin, an inhibitor of PKCβ, enhances antiangiogenic effects and cytotoxicity of radiation against endothelial cells."  Transl. Oncol. 1:  195-201 (2008).

• Enzastaurin had a synergistic inhibitory effect with the EGFR inhibitor gefitinib on the proliferation of parental and gefitinib-resistant (GR) cancer cells.  Enzastaurin also demonstrated antitumour activity cooperatively with gefitinib in mice grafted with GEO and GEO-GR colon tumours.  Gelardi, T., et al.  "Enzastaurin inhibits tumours sensitive and resistant to anti-EGFR drugs."  Br. J. Cancer 99:  473-480 (2008).

• Fifty-five patients with relapsed or refractory diffuse large B-cell lymphoma (DLBCL) were treated with enzastaurin.  Of these, 12 patients showed prolonged freedom from progression (FFP) (FFP ≥ 2 cycles, one cycle = 28 days).  Enzastaurin was well-tolerated.  Robertson, M.J., et al.  "Phase II study of enzastaurin, a protein kinase C Beta inhibitor, in patients with relapsed or refractory diffuse large B-cell lymphoma."  J. Clin. Oncol. 25:  1741-1746 (2007).

• Sixty patients with relapsed or refractory mantle cell lymphoma (MCL) were treated with enzastaurin.  Enzastaurin had a favorable toxicity profile with minimal hematological toxicity.  Twenty-two patients were FFP for ≥ 3 cycles, 6 of 22 were FFP for >6 months.  Two patients remained on treatment and FFP at >23 months.  Morschhauser, F., et al.  "A phase II study of enzastaurin, a protein kinase C beta inhibitor, in patients with relapsed or refractory mantle cell lymphoma."  Ann. Oncol. 19:  247-253 (2008).

• Our enzastaurin product is the free base, whose CAS number is given above.  The CAS number of the dihydrochloride salt is 365253-37-8.

• Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.