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.
| Molecular Weight | 433.5 |
| Formula | C24H27N5O3 |
| CAS Number | 1316214-52-4 |
| Solubility (25°C) | DMSO 77 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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