ACY-1215 (Rocilinostat) is an orally-available, hydroxamic acid-based, selective inhibitor of HDAC6 and HDAC8 with IC50 values of 5 nM and 100 nM, respectively. ACY-1215 is12-, 10-, and 11-fold less active against HDAC1, HDAC2, and HDAC3, respecitvely, and has minimal activity (IC50 > 1 uM) against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1 and Sirtuin2. [1]
To demonstrate ACY-1215 selectivity for HDAC6, MM.1S cells were cultured with increasing doses of ACY-1215 for 6 hours. Dose-dependent increased acetylated a-tubulin was observed at low doses (0.62 uM) with no effect on histone acetylation.
ACY-1215 has been shown to work synergistically with bortezomib in multiple myeloma models.
Technical information:
| Chemical Formula: | C24H27N5O3 | |
| CAS #: | 1316214-52-4 | |
| Molecular Weight: | 433.5 | |
| Purity: | > 98% | |
| Appearance: | White solid | |
| Chemical Name: | 2-(diphenylamino)-N-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | ACY-1215, ACR1215, Rocilinostat |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Santo et al., Preclinical activity, pharmacodynamic, and pharmacokinetic properties of a selective HDAC6 inhibitor, ACY-1215, in combination with bortezomib in multiple myeloma. Blood 2012, 119, 2579-2589. Pubmed ID: 22262760 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
