Rocilinostat (ACY-1215)

Catalog No.S8001

Rocilinostat (ACY-1215) Chemical Structure

Molecular Weight(MW): 433.5

Rocilinostat (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.. Rocilinostat (ACY-1215) purchased from Selleck.

Purity & Quality Control

Choose Selective HDAC Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Rocilinostat (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 NHK0XYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTF2NkigxtEhOzFyIH7N NYXPdG41OjZ2NEOwO|g>
A-172 M2e1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;oNVDDqG6P MX2yOE81QCCq MXrpcohq[mm2czDj[YxtKGe{b4f0bEB1cW2nIHTldIVv\GWwdHz5 MUSyOlE2ODN2MB?=
U87MG M1zaemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXuxNOKhdk1? NFT0RWkzPC92ODDo MlrLbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NXLPbFN3OjZzNUCzOFA>
Hbl-1 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWq0PEBp MmD2TWM2OD1zLk[g{txO Moj4NlYyOTZ{N{C=
OCI-Ly10 MoG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWW0PEBp NFPjWGRKSzVyPUCuPUDPxE1? NWTGWZRoOjZzMU[yO|A>
Riva NWjL[|J7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rCcVQ5KGh? NYHjZlB{UUN3ME2yMlIh|ryP M2PqcFI3OTF4Mkew
Su-DHL2 NIDLc25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnjOFghcA>? NUHWXmY{UUN3ME2zMlMh|ryP NYqzWXJHOjZzMU[yO|A>
OCI-Ly1 NY\McW86T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTwU2h4PDhiaB?= NUHTOGxGUUN3ME2yMlQh|ryP NHn1cGMzPjFzNkK3NC=>
OCI-Ly7 M1nvb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLYOFghcA>? Mn3uTWM2OD1zLkKg{txO MoXmNlYyOTZ{N{C=
Su-DHL4 M4XWcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVy0PEBp Mn3ETWM2OD12Lkeg{txO MkW5NlYyOTZ{N{C=
Su-DHL6 M3\BOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLJc21oPDhiaB?= M1XxNmlEPTB;Mz6yJO69VQ>? M1;3VVI3OTF4Mkew
Hbl-2 MofPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV60PEBp NUP3O4RRUUN3ME2xMlkh|ryP NIfTSWUzPjFzNkK3NC=>
Jeko-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVj6NYp3PDhiaB?= MUfJR|UxRTFwNTFOwG0> NG\IeFIzPjFzNkK3NC=>
Jvm-2 NFX6[3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnDR2NQPDhiaB?= NYTKV|lbUUN3ME20MlAh|ryP M2Po[lI3OTF4Mkew
Rec-1  M2nZS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3sNVVpPDhiaB?= M{X2SGlEPTB;Mj6zJO69VQ>? M2XJelI3OTF4Mkew
CCL-119 NUjDXVU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jPdVQ5KGh? NX\DN4dtUUN3ME2xMlch|ryP NH7uPZIzPjFzNkK3NC=>
H9 NEj5NohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\XTZRpPDhiaB?= NUj4NlNzUUN3ME2xMlIh|ryP NF;sZW4zPjFzNkK3NC=>
HH NUTydVd3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoTlOFghcA>? MljhTWM2OD1{LkWg{txO Mki5NlYyOTZ{N{C=
Sup-T1 M4rofmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1PZcFQ5KGh? NFHRUlRKSzVyPUGuOkDPxE1? NIC1[|MzPjFzNkK3NC=>
MM.1S Mnn1SpVv[3Srb36gRZN{[Xl? M3\q[FAuPc7:TR?= M1fsXVYhcA>? MoDWbY5kemWjc3XzJIFk\XS7bHH0[YQh|rFvdIXieYxqdg>? MmTDNlIzPjJ5NkC=
MM.1S MWDGeY5kfGmxbjDBd5NigQ>? MnPFNE4zPS9zzszN Ml\xNVghcA>? MXnpcoNz\WG|ZYOgZYNmfHmuYYTl[EDPuS22dXL1cIlv MVOyNlI3Ojd4MB?=
MM.1R NY\uWpdrTnWwY4Tpc44hSXO|YYm= M3jaeFAvOjVxMd88US=> NWP5Wox1OThiaB?= M{jQfolv[3KnYYPld{Bi[2W2eXzheIVlKM7zLYT1ZpVtcW5? MoTaNlIzPjJ5NkC=
RPMI8226  MX7GeY5kfGmxbjDBd5NigQ>? MojRNE4zPS9zzszN NFrvNI4yQCCq M4XQN4lv[3KnYYPld{Bi[2W2eXzheIVlKM7zLYT1ZpVtcW5? M2TJcFIzOjZ{N{[w
MM.1S MVXD[YxtKF[rYXLpcIl1gSCDc4PhfS=> Mk\mNE05|ryP M4DaWVQ5KGh? NXfKdIc6\GWlcnXhd4V{KE2PLXPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NYO1dJY5OjJ{NkK3OlA>
OPM1 NX\6c2tGS2WubDDWbYFjcWyrdImgRZN{[Xl? MViwMVjPxE1? M1rCO|Q5KGh? MX;k[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NVXGd|B1OjJ{NkK3OlA>
RPMI NFnPdnVE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXewMVjPxE1? MVy0PEBp MXHk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MWWyNlI3Ojd4MB?=
MM.1R NUT1UYdkS2WubDDWbYFjcWyrdImgRZN{[Xl? MYmwMVjPxE1? MX60PEBp M3PFZYRm[3KnYYPld{BOVS2lZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MkTtNlIzPjJ5NkC=
LR5 MmLZR4VtdCCYaXHibYxqfHliQYPzZZk> MoC4NE05|ryP NF\nd|k1QCCq MnLT[IVkemWjc3XzJG1ONWOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MWqyNlI3Ojd4MB?=
OPM2 MUjD[YxtKF[rYXLpcIl1gSCDc4PhfS=> MXewMVjPxE1? M2DQcVQ5KGh? NHXlSVRl\WO{ZXHz[ZMhVU1vY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MUiyNlI3Ojd4MB?=

... 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
+ 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 N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02787369 Not yet 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