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Rocilinostat

Chemical Structure : Rocilinostat

CAS No.: 1316214-52-4

Rocilinostat (ACY-1215, ACY1215)

Catalog No.: PC-73193Not For Human Use, Lab Use Only.

Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor with IC50 of 5 nM.

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Biological Activity

Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor with IC50 of 5 nM.
Ricolinostat (ACY-1215) displays 10-12 fold less active against HDAC1, HDAC2, and HDAC3 (class I HDACs), minimal activity (IC50 > 1 uM) against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2, and has slight activity against HDAC8 (IC50=0.1 uM).
ACY-1215 induces dose-dependent cytotoxicity in MM cells (IC50=2-8 uM), induces synergistic anti-MM activity in combination with bortezomib.
ACY-1215 in combination with bortezomib induces significant anti-MM activity in vivo.

Physicochemical Properties

M.Wt 433.5
Formula C24H27N5O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(Diphenylamino)-N-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide

References

1. Santo L, et al. Blood. 2012 Mar 15;119(11):2579-89.

2. Amengual JE, et al. Clin Cancer Res. 2015 Oct 15;21(20):4663-75.

3. Mishima Y, et al. Br J Haematol. 2015 May;169(3):423-34.

4. Dasmahapatra G, et al. Mol Cancer Ther. 2014 Dec;13(12):2886-97.

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