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ACY-1215 (Rocilinostat) | HDAC6/8 inhibitor

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Price:
$149.00
Catalog #:
C2121-2s
Quantity:


Product Description

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.

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