2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Biological activity
Description
Target:
In Vivo
Mice treated with Ricolinostat (ACY-1215), Bortezomib, or Ricolinostat plus Bortezomib show a significant delay in tumor growth (P=0.01, P=0.006, and P<0.0001, respectively). Combined treatment with Ricolinostat and Bortezomib shows significant suppression of tumor growth and significantly prolonged overall survival (OS) compare with the control group (17 days in the control vs 40 days in the combination-treated group, P<0.0001) and the Ricolinostat (ACY-1215)-treated group (22 days in the Bortezomib group vs 40 days in the combination-treated group, P<0.0001). Weight loss in the combination-treated group is between 4% and 12% compare with the same-day control group values during treatment, with complete recovery after the last injection. As is observed in the plasmacytoma model, a significant therapeutic advantage is found by combining Ricolinostat with Bortezomib compare with either agent alone[1].
In Vitro
Ricolinostat (ACY-1215) has slight activity against HDAC8 (IC50=0.1 μM), and has minimal activity (IC50>1 μM) against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1, and Sirtuin2. The effect of Ricolinostat (ACY-1215) on multiple myeloma (MM) cell viability is determined with MTT assays using MM cell lines. Exposure of MM cell lines for 48 hours results in dose-dependent decreased viability, with IC50 values ranging from 2-8μM. Ricolinostat (ACY-1215) demonstrates significant activity in the MM Bortezomib-resistant cell line (ANBL-6.BR), demonstrating the ability of Ricolinostat (ACY-1215) to overcome Bortezomib resistance[1].
Kinase Assay
Cell Assay
Animal Administration
References
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