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.

    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

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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 NVPVcFh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHCTWM2OD1zNE[4JOKyKDNzMDDuUS=> M13tTlI3PDR|MEe4
A-172 MoHLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYexNOKhdk1? MX[yOE81QCCq MWHpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MlXtNlYyPTB|NEC=
U87MG M3L3Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4L1TlExyqCwTR?= MnPMNlQwPDhiaB?= NXLCUo82cW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? MWeyOlE2ODN2MB?=
Hbl-1 NH3Cc4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXyOFghcA>? M3PTbWlEPTB;MT62JO69VQ>? NEDqeFMzPjFzNkK3NC=>
OCI-Ly10 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInaUpY1QCCq NWXGWXBIUUN3ME2wMlkh|ryP Mk\pNlYyOTZ{N{C=
Riva M3XiO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTYPWl{PDhiaB?= MY\JR|UxRTJwMjFOwG0> NFvITpEzPjFzNkK3NC=>
Su-DHL2 M4HGV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFrIU4Y1QCCq MVXJR|UxRTNwMzFOwG0> MlHaNlYyOTZ{N{C=
OCI-Ly1 NIDFemdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX:5U|g2PDhiaB?= NXrzRplkUUN3ME2yMlQh|ryP NG\ZNW4zPjFzNkK3NC=>
OCI-Ly7 NF3oVXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{m5b|Q5KGh? NITUSGpKSzVyPUGuNkDPxE1? NWL5OmJwOjZzMU[yO|A>
Su-DHL4 MnjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2WxWVQ5KGh? NGXKOZNKSzVyPUSuO{DPxE1? NHf1XmgzPjFzNkK3NC=>
Su-DHL6 NVzEOGQ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXBSZRMPDhiaB?= MorRTWM2OD1|LkKg{txO M2m1R|I3OTF4Mkew
Hbl-2 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\ZOFghcA>? MUTJR|UxRTFwOTFOwG0> NGHxbZIzPjFzNkK3NC=>
Jeko-1 M{e1PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFuzc3k1QCCq NXXiT5dIUUN3ME2xMlUh|ryP NWnNbYQ4OjZzMU[yO|A>
Jvm-2 M1O0Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXe0PEBp MX\JR|UxRTRwMDFOwG0> NX7zc3pIOjZzMU[yO|A>
Rec-1  NWDHZ3R2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjJOFghcA>? MkO3TWM2OD1{LkOg{txO NHnPXYUzPjFzNkK3NC=>
CCL-119 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1ntOFQ5KGh? M3zmVmlEPTB;MT63JO69VQ>? NEfQc3EzPjFzNkK3NC=>
H9 MmfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLDZ3I1QCCq M2LEemlEPTB;MT6yJO69VQ>? NW[3PIdtOjZzMU[yO|A>
HH Mn;3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XQTlQ5KGh? MmLFTWM2OD1{LkWg{txO M3TYVVI3OTF4Mkew
Sup-T1 MkS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLOSII1QCCq M3nOdWlEPTB;MT62JO69VQ>? Ml\sNlYyOTZ{N{C=
MM.1S Mn3HSpVv[3Srb36gRZN{[Xl? MWiwMVXPxE1? MVq2JIg> M3zhZYlv[3KnYYPld{Bi[2W2eXzheIVlKM7zLYT1ZpVtcW5? MlfPNlIzPjJ5NkC=
MM.1S NVP6Znc6TnWwY4Tpc44hSXO|YYm= M3n6d|AvOjVxMd88US=> NHXk[YIyQCCq M{C2UYlv[3KnYYPld{Bi[2W2eXzheIVlKM7zLYT1ZpVtcW5? M2\FWFIzOjZ{N{[w
MM.1R NGXUR2FHfW6ldHnvckBCe3OjeR?= M{\jZ|AvOjVxMd88US=> MYSxPEBp Mk\rbY5kemWjc3XzJIFk\XS7bHH0[YQh|rFvdIXieYxqdg>? M1HkRlIzOjZ{N{[w
RPMI8226  NFnURWRHfW6ldHnvckBCe3OjeR?= Mn3pNE4zPS9zzszN MkDTNVghcA>? MlnFbY5kemWjc3XzJIFk\XS7bHH0[YQh|rFvdIXieYxqdg>? NGXwUpMzOjJ4Mke2NC=>
MM.1S NFvKTlVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4WzTlAuQM7:TR?= NEDkOYI1QCCq MmD5[IVkemWjc3XzJG1ONWOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy Mm\vNlIzPjJ5NkC=
OPM1 MVzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXXKbIIyOC16zszN NGizNow1QCCq NVrMRppo\GWlcnXhd4V{KE2PLXPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M4LrUVIzOjZ{N{[w
RPMI NHLBXnFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGPaUlAxNTkQvF2= MVm0PEBp M3v5eoRm[3KnYYPld{BOVS2lZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NUXlVWRVOjJ{NkK3OlA>
MM.1R NI\JXGxE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MofkNE05|ryP NF;iW|A1QCCq MV;k[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MW[yNlI3Ojd4MB?=
LR5 MV3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHfyNGUxNTkQvF2= MWe0PEBp NGXrOJZl\WO{ZXHz[ZMhVU1vY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVyyNlI3Ojd4MB?=
OPM2 MX3D[YxtKF[rYXLpcIl1gSCDc4PhfS=> M{fudFAuQM7:TR?= M{HnS|Q5KGh? NIK0NHBl\WO{ZXHz[ZMhVU1vY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MUOyNlI3Ojd4MB?=

... 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

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 slightly soluble or insoluble
Ethanol slightly soluble or 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
in solvent
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID