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    Rocilinostat (ACY1215; Ricolinostat)
    Rocilinostat (ACY1215; Ricolinostat)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0271
    CAS #: 1316214-52-4Purity ≥98%

    Description: Rocilinostat (formerly Ricolinostat; ACY-1215), an investigational drug, is a potent, orally bioavailable and selective HDAC6 inhibitor with potential anticancer activity. It inhibits HDAC6 with an IC50 of 5 nM in a cell-free assay, shows more than 10-fold selectivity for HDAC6 over HDAC1/2/3, and has no/little activity against HDAC8.

    References: Blood. 2012 Mar 15;119(11):2579-89.

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    Molecular Weight (MW)433.5
    FormulaC24H27N5O3
    CAS No.1316214-52-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 86 mg/mL (198.4 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo) 2% DMSO+30% PEG 300+ddH2O: 5 mg/mL
    Synonyms

    Ricolinostat; Rocilinostat; ACY 1215; ACY1215; ACY-1215

    Chemical Name: 2-(diphenylamino)-N-(7-(hydroxyamino)-7-oxoheptyl)pyrimidine-5-carboxamide

    InChi Key: QGZYDVAGYRLSKP-UHFFFAOYSA-N

    InChi Code: InChI=1S/C24H27N5O3/c30-22(28-32)15-9-1-2-10-16-25-23(31)19-17-26-24(27-18-19)29(20-11-5-3-6-12-20)21-13-7-4-8-14-21/h3-8,11-14,17-18,32H,1-2,9-10,15-16H2,(H,25,31)(H,28,30)

    SMILES Code: O=C(C1=CN=C(N(C2=CC=CC=C2)C3=CC=CC=C3)N=C1)NCCCCCCC(NO)=O


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    In Vitro

    In vitro activity: 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.


    Kinase Assay: ACY-1215 was dissolved and subsequently diluted in assay buffer [50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, and 20 μM tris(2-carboxyethyl)phosphine] to 6-fold the final concentration. HDAC enzymes were diluted to 1.5-fold of the final concentration in assay buffer and pre-incubated with ACY-1215 for 10 minutes before the addition of the substrate. The amount of FTS (HDAC1, HDAC2, HDAC3, and HDAC6) or MAZ-1675 (HDAC4, HDAC5, HDAC7, HDAC8, and HDAC9) used for each enzyme was equal to the Michaelis constant (Km), as determined by a titration curve. FTS or MAZ-1675 was diluted in assay buffer to 6-fold the final concentration with 0.3 μM sequencing grade trypsin. The substrate/trypsin mix was added to the enzyme/compound mix and the plate was shaken for 60 seconds and then placed into a SpectraMax M5 microtiter plate reader. The enzymatic reaction was monitored for release of 7-amino-4-methoxy-coumarin over 30 minutes, after deacetylation of the lysine side chain in the peptide substrate, and the linear rate of the reaction was calculated. HDAC11, sirtuin1, and sirtuin2 assays were performed by Cerep.


    Cell Assay: ACY-1215 induces less cytotoxicity in PHA-stimulated or unstimulated PBMCs. In purified CD4+ T cells, ACY-1215 induces toxicity with IC50 value of 2.5 μM. In MM cell lines, ACY-1215 dose-dependently decreases viability with IC50 value of 2-8 μM and induces significant cytotoxicity. In MM.1S cells, ACY-1215 dose-dependently reduces DNA synthesis of MM cells adherent to BMSCs and also inhibits growth induced by IL-6 and IGF-1.

    In VivoACY-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.
    Animal modelMale SCID mice inoculated subcutaneously with MM.1S cells.
    Formulation & DosageFormulated in 10% DMSO in 5% dextrose in water; 50 mg/kg; 5 days a week for 3 weeks; Oral administration.
    References

    Blood. 2012 Mar 15;119(11):2579-89.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

     

    Rocilinostat (ACY-1215)

     

    Rocilinostat (ACY-1215)

     

    Rocilinostat (ACY-1215)

     Rocilinostat (ACY-1215)
    ACY-1215 PK/PD profile. Blood. 2012 Mar 15;119(11):2579-89. 
     
    Rocilinostat (ACY-1215)
    ACY-1215 selectively inhibits HDAC6. Blood. 2012 Mar 15;119(11):2579-89. 
     
    Rocilinostat (ACY-1215)
    ACY-1215 in combination with bortezomib induces significant anti-MM activity in vivo. Blood. 2012 Mar 15;119(11):2579-89. 


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