Enzastaurin, Free Base (LY-317615, D04014, CAS 170364-57-5), >99%

LC Laboratories' Product Number E-4506 - Enzastaurin, Free Base (LY-317615, D04014, CAS 170364-57-5), >99% - for research use only. 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. Enzastaurin induces apoptosis in multiple myeloma (MM) cell lines by inhibiting signaling through the AKT pathway, which is caspase-independent. Enzastaurin has an antitumor effect on Waldenstr√Ä√úm macroglobulinemia both in vitro and in vivo. Enzastaurin enhances the antiangiogenic effects of radiation by radiosensitizing human endothelial cells in pancreatic cancer xenografts. 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. 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. 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. Our enzastaurin product is the free base, whose CAS number is 170364-57-5. The CAS number of the dihydrochloride salt is 365253-37-8.

• Supplier: LC Laboratories
• Product #: E-4506
• Sku #: E-4506_500mg