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Rocilinostat

Cat. No. M2123
Rocilinostat Structure
Synonym:

ACY-1215

Size Price Availability Quantity
10mg USD 130 In stock
50mg USD 390 In stock
100mg USD 550 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 433.5
Formula C24H27N5O3
CAS Number 1316214-52-4
Purity >99%
Solubility DMSO 80 mg/mL
Storage at -20°C
References

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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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Rocilinostat, ACY-1215 supplier, HDAC, inhibitors

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