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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1 Customer Review

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

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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 NVP5PWZlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13McWlEPTB;MUS2PEDDuSB|MUCgcm0> MoDlNlY1PDNyN{i=
A-172 NHPUeXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXqxNOKhdk1? NU\NeJRGOjRxNEigbC=> M2DSTYlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NHHKb20zPjF3MEO0NC=>
U87MG NWrlV4Q5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYexNOKhdk1? MY[yOE81QCCq NGHKfJFqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 MkPiNlYyPTB|NEC=
Hbl-1 NISyXmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUi0PEBp MlzRTWM2OD1zLk[g{txO NYXNb3B1OjZzMU[yO|A>
OCI-Ly10 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfJd5Q1QCCq MXjJR|UxRTBwOTFOwG0> NUX0TokzOjZzMU[yO|A>
Riva NVL1bZR3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUW4U3g5PDhiaB?= NFzkS4hKSzVyPUKuNkDPxE1? NUfScWs4OjZzMU[yO|A>
Su-DHL2 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrxOFghcA>? M1TvfWlEPTB;Mz6zJO69VQ>? MWOyOlEyPjJ5MB?=
OCI-Ly1 NIDvOI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nuV|Q5KGh? M3TNdGlEPTB;Mj60JO69VQ>? MYKyOlEyPjJ5MB?=
OCI-Ly7 NGO5VYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TGPFQ5KGh? NEnmWlhKSzVyPUGuNkDPxE1? NXu1NFJFOjZzMU[yO|A>
Su-DHL4 MmTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nDbFQ5KGh? MUfJR|UxRTRwNzFOwG0> MVyyOlEyPjJ5MB?=
Su-DHL6 NHfJbphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXpOpk1QCCq M{iweWlEPTB;Mz6yJO69VQ>? MmPkNlYyOTZ{N{C=
Hbl-2 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnvWGU4PDhiaB?= Ml\KTWM2OD1zLkmg{txO NUfmU5FjOjZzMU[yO|A>
Jeko-1 M3jMdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDIbGg1QCCq M1;hZmlEPTB;MT61JO69VQ>? NG\tfnMzPjFzNkK3NC=>
Jvm-2 MnHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDl[YlrPDhiaB?= NYr3XJk5UUN3ME20MlAh|ryP NFXWdJYzPjFzNkK3NC=>
Rec-1  MonQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXy[I81QCCq M2XaNGlEPTB;Mj6zJO69VQ>? M1KxSlI3OTF4Mkew
CCL-119 M4jo[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYK0PEBp M2LRUmlEPTB;MT63JO69VQ>? MYOyOlEyPjJ5MB?=
H9 MmrRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWG0PEBp NF75cXNKSzVyPUGuNkDPxE1? M3fpT|I3OTF4Mkew
HH MkPvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\jOVQ5KGh? MnzPTWM2OD1{LkWg{txO MnjKNlYyOTZ{N{C=
Sup-T1 M2Kxc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\EOFghcA>? NFX3b|BKSzVyPUGuOkDPxE1? MXGyOlEyPjJ5MB?=
MM.1S M4rYdmZ2dmO2aX;uJGF{e2G7 M4nzNVAuPc7:TR?= M3XSZlYhcA>? M3THe4lv[3KnYYPld{Bi[2W2eXzheIVlKM7zLYT1ZpVtcW5? NWLWTGQ6OjJ{NkK3OlA>
MM.1S MnfxSpVv[3Srb36gRZN{[Xl? M3S0RVAvOjVxMd88US=> NWHm[2lpOThiaB?= MkPkbY5kemWjc3XzJIFk\XS7bHH0[YQh|rFvdIXieYxqdg>? M3vw[lIzOjZ{N{[w
MM.1R NGDDWFVHfW6ldHnvckBCe3OjeR?= MU[wMlI2NzIQvF2= MVSxPEBp M37QW4lv[3KnYYPld{Bi[2W2eXzheIVlKM7zLYT1ZpVtcW5? NHnKRVgzOjJ4Mke2NC=>
RPMI8226  MlTDSpVv[3Srb36gRZN{[Xl? NFewTmIxNjJ3L{JOwG0> NYX4NotQOThiaB?= NIewUXVqdmO{ZXHz[ZMh[WOndInsZZRm\CEQsT30eYJ2dGmw M3jwVVIzOjZ{N{[w
MM.1S MlrpR4VtdCCYaXHibYxqfHliQYPzZZk> NV3MZWl[OC16zszN NFHUd|Y1QCCq MUXk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NFK5[JczOjJ4Mke2NC=>
OPM1 NH;NUJFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFTTcHYxNTkQvF2= M2\FO|Q5KGh? MVTk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MWmyNlI3Ojd4MB?=
RPMI NUDLc2pDS2WubDDWbYFjcWyrdImgRZN{[Xl? NVrlNmxIOC16zszN M4LZZlQ5KGh? MWjk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M1f0XlIzOjZ{N{[w
MM.1R MXnD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXzIcm97OC16zszN NXPqZVV2PDhiaB?= M1HlWYRm[3KnYYPld{BOVS2lZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M3vRSVIzOjZ{N{[w
LR5 M3jWUmNmdGxiVnnhZoltcXS7IFHzd4F6 NWG5RYVoOC16zszN NFX6fpU1QCCq MXzk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MlTLNlIzPjJ5NkC=
OPM2 NF;vTo1E\WyuIG\pZYJqdGm2eTDBd5NigQ>? M4LQU|AuQM7:TR?= MWS0PEBp M1LEfoRm[3KnYYPld{BOVS2lZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NH3NVmozOjJ4Mke2NC=>

... 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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+30% PEG 300+ddH2O 5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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