Ricolinostat (ACY-1215)

製品コードS8001 別名:Rocilinostat

Ricolinostat (ACY-1215) 化学構造

分子量(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.

サイズ 価格(税別)  
JPY 31540.00
JPY 18260.00
JPY 28220.00
JPY 94620.00

カスタマーフィードバック(4)

  • (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, 36(24):3450-3463. Ricolinostat (ACY-1215) purchased from Selleck.

    Western blot analysis of PARP, C-caspase-3, total MET and phosphorylated MET (p-MET) in NuDUL-1 and Toledo cells treated as metioned. GAPDH served as a loading control. NC=negative control.

    J Pathol, 2018, 246(2):141-153. 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.

製品安全説明書

HDAC阻害剤の選択性比較

生物活性

製品説明 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.
特性 Induced less cytotoxicity in PHA-stimulated PBMCs from 4 healthy donors compared with the pan-HDAC inhibitor SAHA.
ターゲット
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
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RPMI8226 NIPuNIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvPTmlKSzVyPUG0OlghyrFiM{GwJI5O MXuyOlQ1OzB5OB?=
A-172 NE\FU5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIKycVgyOMLibl2= MkX5NlQwPDhiaB?= MkG2bY5pcWKrdIOgZ4VtdCCpcn;3eIghfGmvZTDk[ZBmdmSnboTsfS=> NIq0UpIzPjF3MEO0NC=>
U87MG MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHy3SI0yOMLibl2= MVOyOE81QCCq M1y0WolvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NHXnNYozPjF3MEO0NC=>
Hbl-1 NE[0bpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljPOFghcA>? NHfPUIlKSzVyPUGuOkDPxE1? MUOyOlEyPjJ5MB?=
OCI-Ly10 M322Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfpe2U1QCCq MkLNTWM2OD1yLkmg{txO Mn\TNlYyOTZ{N{C=
Riva MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrXOFghcA>? M134T2lEPTB;Mj6yJO69VQ>? MojhNlYyOTZ{N{C=
Su-DHL2 NXrPNlJ{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUS3d3lxPDhiaB?= MY\JR|UxRTNwMzFOwG0> NF2xZ5IzPjFzNkK3NC=>
OCI-Ly1 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUm0PEBp NH;3OZVKSzVyPUKuOEDPxE1? MW[yOlEyPjJ5MB?=
OCI-Ly7 NFvVZo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWC0PEBp NWX2PVRGUUN3ME2xMlIh|ryP Mkm4NlYyOTZ{N{C=
Su-DHL4 NFX2ZVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3v5XVQ5KGh? MUnJR|UxRTRwNzFOwG0> NWHKcHBGOjZzMU[yO|A>
Su-DHL6 NX7V[VVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFPnVmU1QCCq NFXwWnRKSzVyPUOuNkDPxE1? NUfQOm9YOjZzMU[yO|A>
Hbl-2 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnFXow1QCCq MYPJR|UxRTFwOTFOwG0> M2[0ZlI3OTF4Mkew
Jeko-1 NGHvN2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLqfVR5PDhiaB?= MnXPTWM2OD1zLkWg{txO M3y5VFI3OTF4Mkew
Jvm-2 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG[wSGc1QCCq NUTzcYNyUUN3ME20MlAh|ryP NH;heGszPjFzNkK3NC=>
Rec-1  NWrvT3lpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWO0PEBp NE[yWVBKSzVyPUKuN{DPxE1? MoXXNlYyOTZ{N{C=
CCL-119 MlfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnWxOFghcA>? NU\pOmQ{UUN3ME2xMlch|ryP MWSyOlEyPjJ5MB?=
H9 M1HEXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXu0PEBp M3LndGlEPTB;MT6yJO69VQ>? M{TUOFI3OTF4Mkew
HH MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVG0PEBp M4DWSmlEPTB;Mj61JO69VQ>? NVTiUmQ6OjZzMU[yO|A>
Sup-T1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV63bWZRPDhiaB?= MkHOTWM2OD1zLk[g{txO MVuyOlEyPjJ5MB?=
MM.1S NFTYNo1HfW6ldHnvckBCe3OjeR?= MkHkNE02|ryP MWC2JIg> MmLObY5kemWjc3XzJIFk\XS7bHH0[YQh|rFvdIXieYxqdg>? M13S[FIzOjZ{N{[w
MM.1S NV;xUGRRTnWwY4Tpc44hSXO|YYm= MXywMlI2NzIQvF2= NV7STlBFOThiaB?= M{TtOYlv[3KnYYPld{Bi[2W2eXzheIVlKM7zLYT1ZpVtcW5? NXr1W4ptOjJ{NkK3OlA>
MM.1R M2PIemZ2dmO2aX;uJGF{e2G7 MnPmNE4zPS9zzszN M4jFfVE5KGh? M2S1[Ilv[3KnYYPld{Bi[2W2eXzheIVlKM7zLYT1ZpVtcW5? NHzZbpozOjJ4Mke2NC=>
RPMI8226  NXHpUmp4TnWwY4Tpc44hSXO|YYm= MkSzNE4zPS9zzszN NIjIdGcyQCCq NEPXN3FqdmO{ZXHz[ZMh[WOndInsZZRm\CEQsT30eYJ2dGmw NHTr[lczOjJ4Mke2NC=>
MM.1S NX73RYdCS2WubDDWbYFjcWyrdImgRZN{[Xl? NHTuV|gxNTkQvF2= NFXGWlI1QCCq NUjxeW5O\GWlcnXhd4V{KE2PLXPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MYSyNlI3Ojd4MB?=
OPM1 NXvUS4VQS2WubDDWbYFjcWyrdImgRZN{[Xl? NHTWb5QxNTkQvF2= M4TE[lQ5KGh? MYXk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MkjjNlIzPjJ5NkC=
RPMI NHLBNINE\WyuIG\pZYJqdGm2eTDBd5NigQ>? Mn\NNE05|ryP Mmj2OFghcA>? NWDZblhM\GWlcnXhd4V{KE2PLXPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz Ml\NNlIzPjJ5NkC=
MM.1R MXzD[YxtKF[rYXLpcIl1gSCDc4PhfS=> M3S5[|AuQM7:TR?= M{\0UlQ5KGh? NYLyUIFj\GWlcnXhd4V{KE2PLXPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MUmyNlI3Ojd4MB?=
LR5 NXLRcGo6S2WubDDWbYFjcWyrdImgRZN{[Xl? NUHSVHA3OC16zszN NXLueFZRPDhiaB?= MWTk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MorNNlIzPjJ5NkC=
OPM2 NIm1W3pE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NW\wcHpPOC16zszN MVW0PEBp M{O2ZYRm[3KnYYPld{BOVS2lZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MWOyNlI3Ojd4MB?=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

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.
細胞試験:

[1]

+ 展開
  • 細胞株: MM cell lines, patient MM cells, and PBMCs
  • 濃度: ~8 μM
  • 反応時間: 48 hours
  • 実験の流れ:

    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.


    (参考用のみ)
動物試験:

[1]

+ 展開
  • 動物モデル: MM xenograft SCID mouse model
  • 製剤: 10% DMSO in 5% dextrose in water
  • 投薬量: 50 mg/kg
  • 投与方法: ip
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 86 mg/mL (198.38 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+ddH2O
混合させたのち直ちに使用することを推奨します。
5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 433.5
化学式

C24H27N5O3

CAS No. 1316214-52-4
保管
in solvent
別名 Rocilinostat

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03176472 Not yet recruiting Diabetic Neuropathic Pain Regenacy Pharmaceuticals LLC October 2018 Phase 2
NCT02856568 Withdrawn Non-Resectable Cholangiocarcinoma|Recurrent Cholangiocarcinoma|Stage III Extrahepatic Bile Duct Cancer|Stage III Intrahepatic Cholangiocarcinoma|Stage IIIA Hilar Cholangiocarcinoma|Stage IIIB Hilar Cholangiocarcinoma|Stage IVA Extrahepatic Bile Duct Cancer|Stage IVA Hilar Cholangiocarcinoma|Stage IVA Intrahepatic Cholangiocarcinoma|Stage IVB Extrahepatic Bile Duct Cancer|Stage IVB Hilar Cholangiocarcinoma|Stage IVB Intrahepatic Cholangiocarcinoma|Unresectable Extrahepatic Bile Duct Carcinoma Mayo Clinic|National Cancer Institute (NCI) May 1 2017 Phase 1
NCT02661815 Active not recruiting Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Carcinoma Dana-Farber Cancer Institute|Celgene Corporation June 15 2016 Phase 1
NCT02787369 Active not 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|National Cancer Institute (NCI)|Columbia University February 2016 Phase 1
NCT02189343 Active not recruiting Multiple Myeloma Celgene September 15 2014 Phase 1

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

    What would you suggest to obtain a clear solution?

  • 回答:

    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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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID