Rocilinostat (also known as ACY 1215) is a selective HDAC6 inhibitor with potential antineoplastic activity. Rocilinostat (ACY-1215) selectively targets and binds to HDAC6, thereby disrupting the Hsp90 protein chaperone system through hyperacetylation of Hsp90 and preventing the subsequent aggresomal protein degradation. ACY-1215 has minimal activity (IC50 >1 μM) against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1 and Sirtuin2, and has slight activity against HDAC8 (IC50 = 0.1 μM). In vivo, the anti-MM activity of rocilinostat in combination with bortezomib was confirmed using 2 different xenograft SCID mouse models: human MM injected subcutaneously and luciferase-expressing human MM injected intravenously. Rocilinostat (ACY-1215) induces potent acetylation of α-tubulin at very low doses and triggers acetylation of lysine on histone H3 and histone H4 only at higher doses. Compared to non-selective HDAC inhibitor, ACY-1215 is able to reduce the toxic effects on normal, healthy cells.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 80 mg/mL|
Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma.
Santo L, et al. Blood. 2012 Mar 15;119(11):2579-89. PMID: 22262760.
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BRD73954 ia a potent and selective HDAC inhibitor with IC50 of 36 nM and 120 nM for HDAC6 and HDAC8, respectively.
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