Cat. No. Name Size Price Add Cart
KI0583ACY-121510 mg$170
ACY-121550 mg$490
ACY-1215200 mg$1700

Chemical Characteristic

Product NameACY-1215
SynonymsRocilinostat
CAS No.1316214-52-4
Molecular Weight 433.5
FormulaC24H27N5O3
Chemical Name2-(Diphenylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]-5-pyrimidinecarboxamide
Smilesc1(ncc(cn1)C(=O)NCCCCCCC(=O)NO)N(c1ccccc1)c1ccccc1
Chemical Structure
DocumentsCOA HPLC MS

Biological activities

ACY-1215 is a histone deacetylase (HDAC) 6-selective inhibitor. ACY-1215 exhibits potent and selective inhibitory activity against HDAC6, with an enzymatic IC50 of 5 nM. ACY-1215 has minimal activity against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1, and Sirtuin2, with IC50 > 1 μM. ACY-1215 has an inhibitory activity against HDAC1, HDAC2, HDAC3 and HDAC8 with IC50 of 58, 51, 48 and 100 nM, respectively. The IC50 of ACY-1215 for T-cell toxicity is 2.5 μM. ACY-1215 induces dose-dependent cytotoxicity in multiple myeloma (MM) cells alone or in coculture with cytokines or BM stromal cells (BMSCs). ACY-1215 in combination with bortezomib induces synergistic anti-MM activity. ACY-1215 in combination with bortezomib induces anti-MM activity in vivo in a plasmacytoma and disseminated MM model.[1]

Protocols

ACY-1215 is dissolved first in DMSO at a concentration of 10 mM. [1]

References

[1] Santo L, 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(11): 2579-2589.

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