Catalog No.S8001 Synonyms: Rocilinostat
Molecular Weight(MW): 433.5
Ricolinostat (ACY-1215) is a selective HDAC6 inhibitor with IC50 of 5 nM in a cell-free assay. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2. Phase 2.
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|Description||Ricolinostat (ACY-1215) is a selective HDAC6 inhibitor with IC50 of 5 nM in a cell-free assay. It is >10-fold more selective for HDAC6 than HDAC1/2/3 (class I HDACs) with slight activity against HDAC8, minimal activity against HDAC4/5/7/9/11, Sirtuin1, and Sirtuin2. Phase 2.|
|Features||Induced less cytotoxicity in PHA-stimulated PBMCs from 4 healthy donors compared with the pan-HDAC inhibitor SAHA.|
ACY-1215 is a hydroxamic acid derivative. ACY-1215 is 12-, 10-, and 11-fold less active against HDAC1, HDAC2, and HDAC3 (class I HDACs), respectively. ACY-1215 has minimal activity (IC50 > 1μM) against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1, and Sirtuin2, and has slight activity against HDAC8 (IC50 = 0.1μM). The IC50 values for ACY-1215 for T-cell toxicity is 2.5μM. ACY-1215 overcomes tumor cell growth and survival conferred by BMSCs and cytokines in the BM milieu. ACY-1215 in combination with bortezomib induces synergistic anti-MM activity. 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, confirming its specific inhibitory effect on HDAC6 activity. 
|In vivo||ACY-1215 in combination with bortezomib triggered more significant anti-MM activity than either agent alone in suppressing tumor growth and prolonging survival in both plasmacytoma model and disseminated MM model without significant adverse effects. ACY-1215 is readily absorbed by tumor tissue. Moreover, the drug does not accumulate in tumor tissue, as evidenced by the parallel decline of acetylated α-tubulin in blood cells and tumor tissue by 24 hours after dose. |
|In vitro||DMSO||86 mg/mL (198.38 mM)|
|In vivo||2% DMSO+30% PEG 300+ddH2O||5mg/mL|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02787369||Recruiting||Recurrent Chronic Lymphoid Leukemia||Dana-Farber Cancer Institute|Acetylon Pharmaceuticals Incorporated||May 2016||Phase 1|
|NCT02632071||Recruiting||Metastatic Breast Cancer|Breast Carcinoma||Kevin Kalinsky|Acetylon Pharmaceuticals Incorporated|Columbia University||February 2016||Phase 1|
|NCT02189343||Active, not recruiting||Multiple Myeloma||Acetylon Pharmaceuticals Incorporated||August 2014||Phase 1|
|NCT02091063||Recruiting||Lymphoma|Lymphoid Malignancies||Jennifer Amengual|Acetylon Pharmaceuticals Incorporated|Columbia University||March 2014||Phase 1|Phase 2|
|NCT02088398||Completed||Healthy||Acetylon Pharmaceuticals Incorporated||March 2014||Phase 1|
|NCT01997840||Active, not recruiting||Multiple Myeloma||Acetylon Pharmaceuticals Incorporated||November 2013||Phase 1|Phase 2|
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