Ricolinostat (ACY-1215)

Catalog No.S8001 Synonyms: Rocilinostat

Ricolinostat (ACY-1215)  Chemical Structure

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.

Size Price Stock Quantity  
In DMSO USD 190 In stock
USD 110 In stock
USD 170 In stock
USD 570 In stock
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3 Customer Reviews

  • (a) Representative images from hTERT RPE-1 cells transiently transfected with siControl (siC), treated with vehicle (DMSO), alisertib (MLN8237) or rocilinostat (ACY1215) at the time of serum withdrawal for 48 h. Ciliation monitored by immunofluorescent staining using acetylated α-tubulin (cilia marker) and pericentrin (basal body marker). Nuclei counterstained using DAPI. Highlighted boxes show magnified cilia. Scale bar, 3 μM.

    Oncogene, 2017. Ricolinostat (ACY-1215) purchased from Selleck.

    Immunoblot of MB99-1 cells treated with the indicated compound concentrations for 48 hours. Note that the HDAC6-selective inhibitors affect tubulin acetylation, but not histone H3 acetylation, whereas the pan-HDAC inhibitor TSA increases the acetylation of both.

    Mol Cancer Ther, 2015, 14(3):727-39.. Ricolinostat (ACY-1215) purchased from Selleck.

  • E. The expression levels of TP and TS mRNA were evaluated by qRealTime-PCR in untreated MCF-7 cells and in MCF-7 cells that were untreated or treated with selective HDACi at the indicated concentrations for 24 hours. F. The expression of TP, TS, acetylated H3 and acetylated α-tubulin proteins was determined by western blot in untreated cells and in MCF-7 cells that were treated for 48 hours with different HDACi at the indicated concentrations. α-tubulin was used as the protein loading control

    Oncotarget, 2016, 7(7):7715-31. Ricolinostat (ACY-1215) purchased from Selleck.

Purity & Quality Control

Choose Selective HDAC Inhibitors

Biological Activity

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.
Targets
HDAC6 [1]
(Cell-free assay)
HDAC2 [1]
(Cell-free assay)
HDAC3 [1]
(Cell-free assay)
HDAC1 [1]
(Cell-free assay)
HDAC8 [1]
(Cell-free assay)
4.7 nM 48 nM 51 nM 58 nM 100 nM
In vitro

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. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RPMI8226 M2rYNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPIbYlKSzVyPUG0OlghyrFiM{GwJI5O M4\kdlI3PDR|MEe4
A-172 NXHLcGZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX6xNOKhdk1? NUfiS3dyOjRxNEigbC=> NGnxUlNqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NUP4XZVjOjZzNUCzOFA>
U87MG MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmrLNVDDqG6P M{\Mc|I1NzR6IHi= NWW1OGtZcW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? NVu0UlIzOjZzNUCzOFA>
Hbl-1 NHzDV2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn[5OFghcA>? MknkTWM2OD1zLk[g{txO Mn7rNlYyOTZ{N{C=
OCI-Ly10 NI\JOGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTqOFghcA>? MWDJR|UxRTBwOTFOwG0> MViyOlEyPjJ5MB?=
Riva MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG[3[ng1QCCq NWnpRWlZUUN3ME2yMlIh|ryP MkL2NlYyOTZ{N{C=
Su-DHL2 NIDLbYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWm0PEBp NIThdZdKSzVyPUOuN{DPxE1? Mnq1NlYyOTZ{N{C=
OCI-Ly1 NU\2OYhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\JSoU1QCCq MmToTWM2OD1{LkSg{txO MoDONlYyOTZ{N{C=
OCI-Ly7 MnHqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXW0PEBp MX;JR|UxRTFwMjFOwG0> M4P4elI3OTF4Mkew
Su-DHL4 NXO1doFET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoSxOFghcA>? NVK2T2FiUUN3ME20Mlch|ryP NFv6SogzPjFzNkK3NC=>
Su-DHL6 NGGw[FFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVv1XFM3PDhiaB?= MWrJR|UxRTNwMjFOwG0> MWqyOlEyPjJ5MB?=
Hbl-2 M1LKcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTJWJE1QCCq MmTOTWM2OD1zLkmg{txO MXWyOlEyPjJ5MB?=
Jeko-1 M1HzWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHrNZc1QCCq MVzJR|UxRTFwNTFOwG0> MoHCNlYyOTZ{N{C=
Jvm-2 M13kZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[2VmFUPDhiaB?= NUDuTXJyUUN3ME20MlAh|ryP NIHHc2gzPjFzNkK3NC=>
Rec-1  NFjGRpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7BZ441QCCq NV3ZeHhNUUN3ME2yMlMh|ryP NVXnNG81OjZzMU[yO|A>
CCL-119 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;McFQ5KGh? MXnJR|UxRTFwNzFOwG0> MXSyOlEyPjJ5MB?=
H9 M4GyU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVq0PEBp MmrVTWM2OD1zLkKg{txO NG\nPIgzPjFzNkK3NC=>
HH NILDTm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjKOWM1QCCq MXrJR|UxRTJwNTFOwG0> NX\MUHg5OjZzMU[yO|A>
Sup-T1 M{nGeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFP6NIU1QCCq MnnQTWM2OD1zLk[g{txO M12zSlI3OTF4Mkew
MM.1S NGrzboxHfW6ldHnvckBCe3OjeR?= M3;WXVAuPc7:TR?= NFL0WYQ3KGh? MX\pcoNz\WG|ZYOgZYNmfHmuYYTl[EDPuS22dXL1cIlv NHrtXGEzOjJ4Mke2NC=>
MM.1S M1fMSWZ2dmO2aX;uJGF{e2G7 MmrENE4zPS9zzszN MXmxPEBp M172eolv[3KnYYPld{Bi[2W2eXzheIVlKM7zLYT1ZpVtcW5? NUXmSnZ[OjJ{NkK3OlA>
MM.1R NGfkO|dHfW6ldHnvckBCe3OjeR?= MYGwMlI2NzIQvF2= MoXtNVghcA>? MV3pcoNz\WG|ZYOgZYNmfHmuYYTl[EDPuS22dXL1cIlv M33G[|IzOjZ{N{[w
RPMI8226  MVLGeY5kfGmxbjDBd5NigQ>? MUmwMlI2NzIQvF2= NHTmSokyQCCq MU\pcoNz\WG|ZYOgZYNmfHmuYYTl[EDPuS22dXL1cIlv MljJNlIzPjJ5NkC=
MM.1S M4HOemNmdGxiVnnhZoltcXS7IFHzd4F6 NV;1bHdxOC16zszN Mkj1OFghcA>? NWezN5dV\GWlcnXhd4V{KE2PLXPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MV2yNlI3Ojd4MB?=
OPM1 NXLONJh6S2WubDDWbYFjcWyrdImgRZN{[Xl? M1vzSlAuQM7:TR?= NXTYUXRWPDhiaB?= MXPk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MoLXNlIzPjJ5NkC=
RPMI M1TQU2NmdGxiVnnhZoltcXS7IFHzd4F6 MXuwMVjPxE1? NXLES5JmPDhiaB?= MXPk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MWCyNlI3Ojd4MB?=
MM.1R MmH0R4VtdCCYaXHibYxqfHliQYPzZZk> MXWwMVjPxE1? NVXYfZVyPDhiaB?= NWT4Tolu\GWlcnXhd4V{KE2PLXPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHLVeIIzOjJ4Mke2NC=>
LR5 Mo\tR4VtdCCYaXHibYxqfHliQYPzZZk> MYWwMVjPxE1? MmXpOFghcA>? MmrE[IVkemWjc3XzJG1ONWOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MkXzNlIzPjJ5NkC=
OPM2 NHTkeVBE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NUjXcnpDOC16zszN NYfqOmtnPDhiaB?= Mo\G[IVkemWjc3XzJG1ONWOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NGnaZ3MzOjJ4Mke2NC=>

... Click to View More Cell Line Experimental Data

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. [1]

Protocol

Kinase Assay:

[1]

+ Expand

HDAC enzymatic assays:

ACY-1215 is 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 are 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 is equal to the Michaelis constant (Km), as determined by a titration curve. FTS or MAZ-1675 is diluted in assay buffer to 6-fold the final concentration with 0.3μM sequencing grade trypsin. The substrate/trypsin mix is added to the enzyme/compound mix and the plate is shaken for 60 seconds and then placed into a SpectraMax M5 microtiter plate reader. The enzymatic reaction is 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 is calculated.
Cell Research:

[1]

+ Expand
  • Cell lines: MM cell lines, patient MM cells, and PBMCs
  • Concentrations: ~8 μM
  • Incubation Time: 48 hours
  • Method:

    PBMCs from healthy donors are isolated and stimulated with 2.5 μg/mL of phytohemagglutinin (PHA) for 48 hours in the presence of increasing concentrations of ACY-1215. DNA synthesis is measured by tritiated thymidine uptake. CD4+T cells are purified from human blood with the Rosette Sep negative-selection kit. Cells are stimulated by CD3/CD28 Dynabeads for 7 days in the presence of compounds. Cell viability is assessed using alamarBlue. MM cells (2-3 × 104cells/well) are incubated in 96-well culture plates with medium and different concentrations of ACY-1215, bortezomib, and/or recombinant IL-6 (10 ng/mL) or insulin-like growth factor-1 (IGF-1; 50 ng/mL) for 24 hours at 37°C, and tritiated thymidine incorporation is measured.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: MM xenograft SCID mouse model
  • Formulation: 10% DMSO in 5% dextrose in water
  • Dosages: 50 mg/kg
  • Administration: ip
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (198.38 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+ddH2O
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 433.5
Formula

C24H27N5O3

CAS No. 1316214-52-4
Storage powder
Synonyms Rocilinostat

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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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    What would you suggest to obtain a clear solution?

  • Answer:

    S8001 ACY-1215 can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 5 mg/ml clearly while it in 1% DMSO/30% polyethylene glycol/1% Tween 80 at 30 mg/ml is a suspension for oral administration. Please note that the precipitation will go out from the clear solution after stayed for about half an hour, So it is recommended to prepare the solution just before use.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID