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

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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 M4GyV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIriUVNKSzVyPUG0OlghyrFiM{GwJI5O NGP0bGUzPjR2M{C3PC=>
A-172 NXzpc4JjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUexNOKhdk1? M3zhVlI1NzR6IHi= Mn;NbY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> MnjnNlYyPTB|NEC=
U87MG M2PEb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYmxNOKhdk1? M1PrZVI1NzR6IHi= NHX3Wm5qdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NGnUV2YzPjF3MEO0NC=>
Hbl-1 MoXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XGTVQ5KGh? MVLJR|UxRTFwNjFOwG0> MWeyOlEyPjJ5MB?=
OCI-Ly10 MmfUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XqeVQ5KGh? MkDjTWM2OD1yLkmg{txO NVjjOWJLOjZzMU[yO|A>
Riva M{TLcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPlenBlPDhiaB?= MVzJR|UxRTJwMjFOwG0> NXPUPXNsOjZzMU[yO|A>
Su-DHL2 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrodG01QCCq M3PPVGlEPTB;Mz6zJO69VQ>? M1rjfFI3OTF4Mkew
OCI-Ly1 NHnwNYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYW0PEBp M4jIbGlEPTB;Mj60JO69VQ>? MnH5NlYyOTZ{N{C=
OCI-Ly7 NWLRNFRGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGCxOYk1QCCq M1O0TmlEPTB;MT6yJO69VQ>? MmnDNlYyOTZ{N{C=
Su-DHL4 MlXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHSxcJA1QCCq NF7uUZJKSzVyPUSuO{DPxE1? NVzPbnVzOjZzMU[yO|A>
Su-DHL6 MnnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfLOFghcA>? MmfsTWM2OD1|LkKg{txO M2jvWVI3OTF4Mkew
Hbl-2 Mo\zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33PVFQ5KGh? MXfJR|UxRTFwOTFOwG0> NXLyeIFuOjZzMU[yO|A>
Jeko-1 MkfkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MliyOFghcA>? Mlj1TWM2OD1zLkWg{txO NV:0T5BCOjZzMU[yO|A>
Jvm-2 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHy0NpI1QCCq M3TGcWlEPTB;ND6wJO69VQ>? NXzzVG54OjZzMU[yO|A>
Rec-1  MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYO0PEBp NGDqeXlKSzVyPUKuN{DPxE1? Ml\zNlYyOTZ{N{C=
CCL-119 NHrEbo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG[1fmc1QCCq NHjXcoFKSzVyPUGuO{DPxE1? NF\ueZAzPjFzNkK3NC=>
H9 M2LWNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nkUFQ5KGh? NVrwd3Z4UUN3ME2xMlIh|ryP NUjIVoF1OjZzMU[yO|A>
HH MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYq0PEBp M1vobWlEPTB;Mj61JO69VQ>? MnHlNlYyOTZ{N{C=
Sup-T1 NYOxWI5JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWP0eHc2PDhiaB?= M2qzd2lEPTB;MT62JO69VQ>? NEDiRZEzPjFzNkK3NC=>
MM.1S NXXrNnBnTnWwY4Tpc44hSXO|YYm= M4fRVFAuPc7:TR?= NHHNO483KGh? MX3pcoNz\WG|ZYOgZYNmfHmuYYTl[EDPuS22dXL1cIlv M2jXNVIzOjZ{N{[w
MM.1S NHLKXI1HfW6ldHnvckBCe3OjeR?= NIHRW2ExNjJ3L{JOwG0> M1P0NFE5KGh? MWHpcoNz\WG|ZYOgZYNmfHmuYYTl[EDPuS22dXL1cIlv NVS3WZV6OjJ{NkK3OlA>
MM.1R NYizOJVtTnWwY4Tpc44hSXO|YYm= M2OxclAvOjVxMd88US=> Mn:3NVghcA>? MmD6bY5kemWjc3XzJIFk\XS7bHH0[YQh|rFvdIXieYxqdg>? Mnq4NlIzPjJ5NkC=
RPMI8226  NVjXe2d{TnWwY4Tpc44hSXO|YYm= NH3qZ4kxNjJ3L{JOwG0> M4LhXVE5KGh? NGiyT2xqdmO{ZXHz[ZMh[WOndInsZZRm\CEQsT30eYJ2dGmw MoHiNlIzPjJ5NkC=
MM.1S NIPHeoFE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MmXiNE05|ryP M2HtbFQ5KGh? MVvk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MUWyNlI3Ojd4MB?=
OPM1 MmruR4VtdCCYaXHibYxqfHliQYPzZZk> NUDSc491OC16zszN MkmwOFghcA>? MofU[IVkemWjc3XzJG1ONWOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NF3LS20zOjJ4Mke2NC=>
RPMI MXTD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NHq1OmIxNTkQvF2= MVu0PEBp MXrk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NXTHU3VPOjJ{NkK3OlA>
MM.1R NHG0PVhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NGHYb|QxNTkQvF2= M1PrZVQ5KGh? M2T4SYRm[3KnYYPld{BOVS2lZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MUeyNlI3Ojd4MB?=
LR5 NXX1cJJjS2WubDDWbYFjcWyrdImgRZN{[Xl? NUOwUGxwOC16zszN NXO3XmFkPDhiaB?= MkHz[IVkemWjc3XzJG1ONWOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy MlLHNlIzPjJ5NkC=
OPM2 M1zwRmNmdGxiVnnhZoltcXS7IFHzd4F6 NIn0XXkxNTkQvF2= NWrBdmY3PDhiaB?= Mnza[IVkemWjc3XzJG1ONWOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy M{PQUFIzOjZ{N{[w

... 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 N/A

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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