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(6)

  • (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.

  • Effect of 9 h treatment with bortezomib (Bort, 5 nM) alone or in combination with C1A (2 µM) or ACY-1215 (ACY, 2 µM) on caspase-3/7 activity in OPM-2 cells.

    Br J Cancer, 2018, 119(10):1278-1287. 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.

  • WB analysis of PARP and acetylated-α-tubulin in CRC cells following treatment with ACY-1215 for 24h.

    Mol Cancer Ther, 2018, 17(6):1280-1290. 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 NFO1dlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXzTWM2OD1zNE[4JOKyKDNzMDDuUS=> M2fuR|I3PDR|MEe4
A-172 NYHEOoRCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXqxNOKhdk1? NGqyVVAzPC92ODDo M4PVUYlvcGmkaYTzJINmdGxiZ4Lve5RpKHSrbXWg[IVx\W6mZX70cJk> NWfkSVI3OjZzNUCzOFA>
U87MG Mn71S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIO2V5kyOMLibl2= NYS0cI1QOjRxNEigbC=> NIDPZ5RqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NWG4eZJpOjZzNUCzOFA>
Hbl-1 MnHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rvTFQ5KGh? NILjS|dKSzVyPUGuOkDPxE1? NE\iVIIzPjFzNkK3NC=>
OCI-Ly10 Mmf3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3BdIpUPDhiaB?= MmnzTWM2OD1yLkmg{txO MlnDNlYyOTZ{N{C=
Riva M{nhSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nDXFQ5KGh? M{P0eWlEPTB;Mj6yJO69VQ>? M1z3WVI3OTF4Mkew
Su-DHL2 MkG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjHOFghcA>? NYjIbnVPUUN3ME2zMlMh|ryP M1LVeFI3OTF4Mkew
OCI-Ly1 NYPSWXJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXxPWQ1QCCq MV;JR|UxRTJwNDFOwG0> NWn4O5REOjZzMU[yO|A>
OCI-Ly7 M4XPS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33UfVQ5KGh? NHHZWVlKSzVyPUGuNkDPxE1? NWXvV4l2OjZzMU[yO|A>
Su-DHL4 M4HJV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEKzN5E1QCCq MnqzTWM2OD12Lkeg{txO NG\SNZMzPjFzNkK3NC=>
Su-DHL6 NIPZTZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HzdVQ5KGh? MVHJR|UxRTNwMjFOwG0> Mm[2NlYyOTZ{N{C=
Hbl-2 M3zaTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV:0PEBp NHzkXGtKSzVyPUGuPUDPxE1? MXWyOlEyPjJ5MB?=
Jeko-1 M2fWc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofUOFghcA>? MX;JR|UxRTFwNTFOwG0> NIXsPJMzPjFzNkK3NC=>
Jvm-2 NW\QVZBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnjXXU1QCCq NIPrVFJKSzVyPUSuNEDPxE1? MoP3NlYyOTZ{N{C=
Rec-1  NFHvS49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETu[m41QCCq MW\JR|UxRTJwMzFOwG0> NHqxPXMzPjFzNkK3NC=>
CCL-119 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;oZplOPDhiaB?= M4LkOGlEPTB;MT63JO69VQ>? MXeyOlEyPjJ5MB?=
H9 NXr6b3dNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LNe|Q5KGh? NEDtWGZKSzVyPUGuNkDPxE1? M2HIV|I3OTF4Mkew
HH NUHsd3d1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH:3e3A1QCCq MYXJR|UxRTJwNTFOwG0> NGTQUoszPjFzNkK3NC=>
Sup-T1 NXLpbWZbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTNRnBkPDhiaB?= M4TyOWlEPTB;MT62JO69VQ>? M13obVI3OTF4Mkew
MM.1S NEDsdlZHfW6ldHnvckBCe3OjeR?= NGHPOoUxNTYQvF2= M{LsUlYhcA>? M1[xW4lv[3KnYYPld{Bi[2W2eXzheIVlKM7zLYT1ZpVtcW5? NVjS[ZhHOjJ{NkK3OlA>
MM.1S NH;wbZVHfW6ldHnvckBCe3OjeR?= MXKwMlI2NzIQvF2= M{PETlE5KGh? MXfpcoNz\WG|ZYOgZYNmfHmuYYTl[EDPuS22dXL1cIlv NWLsVI1kOjJ{NkK3OlA>
MM.1R M2C0NmZ2dmO2aX;uJGF{e2G7 MorBNE4zPS9zzszN NVrYemg{OThiaB?= M{mzSYlv[3KnYYPld{Bi[2W2eXzheIVlKM7zLYT1ZpVtcW5? M3LDd|IzOjZ{N{[w
RPMI8226  M{H0R2Z2dmO2aX;uJGF{e2G7 M2rNfVAvOjVxMd88US=> MkfBNVghcA>? MX7pcoNz\WG|ZYOgZYNmfHmuYYTl[EDPuS22dXL1cIlv NYWwR4Z7OjJ{NkK3OlA>
MM.1S MlLWR4VtdCCYaXHibYxqfHliQYPzZZk> MYewMVjPxE1? M2G5bVQ5KGh? MVHk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M3TqNVIzOjZ{N{[w
OPM1 M2Hu[WNmdGxiVnnhZoltcXS7IFHzd4F6 MYmwMVjPxE1? NVX2fIdbPDhiaB?= MkLR[IVkemWjc3XzJG1ONWOnbHygeoli[mmuaYT5JIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NX\6e4c{OjJ{NkK3OlA>
RPMI M{jLdGNmdGxiVnnhZoltcXS7IFHzd4F6 NY\ZTIt{OC16zszN MVW0PEBp M{fMSIRm[3KnYYPld{BOVS2lZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mnq0NlIzPjJ5NkC=
MM.1R NYrDfGZGS2WubDDWbYFjcWyrdImgRZN{[Xl? MkHiNE05|ryP NHPYXWE1QCCq MWjk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= MlvtNlIzPjJ5NkC=
LR5 MVvD[YxtKF[rYXLpcIl1gSCDc4PhfS=> NXjYTFZrOC16zszN NHHl[YI1QCCq MWjk[YNz\WG|ZYOgUW0u[2WubDD2bYFjcWyrdImgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= Ml3hNlIzPjJ5NkC=
OPM2 M{C0[WNmdGxiVnnhZoltcXS7IFHzd4F6 MYiwMVjPxE1? MnvrOFghcA>? NFvMZ2pl\WO{ZXHz[ZMhVU1vY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MYqyNlI3Ojd4MB?=

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
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
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
NCT02661815 Active not recruiting Ovarian Cancer|Fallopian Tube Cancer|Primary Peritoneal Carcinoma Dana-Farber Cancer Institute|Celgene Corporation June 15 2016 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.

HDACシグナル伝達経路

HDAC Inhibitors with Unique Features

相関HDAC製品

Tags: Ricolinostat (ACY-1215) を買う | Ricolinostat (ACY-1215) ic50 | Ricolinostat (ACY-1215) 供給者 | Ricolinostat (ACY-1215) を購入する | Ricolinostat (ACY-1215) 費用 | Ricolinostat (ACY-1215) 生産者 | オーダーRicolinostat (ACY-1215) | Ricolinostat (ACY-1215) 化学構造 | Ricolinostat (ACY-1215) 分子量 | Ricolinostat (ACY-1215) 代理店
×

大阪市内で「G20サミット」が開催されることに伴い、大阪府内で大規模な交通規制が行われる影響で、6月26日(水)から7月1日(月)までの間、下記地域へ出荷が行えなくなります。
対象地域
大阪府(全域)、兵庫県(芦屋市、尼崎市、伊丹市、西宮市)
上記地域より西の地域につきましては納期の遅延が予想されます。
また、国際便も遅延が予想されているため国内在庫がない製品の納期が一週間程度遅れる可能性がございます。
ご不便をおかけいたしますが、宜しくお願い申し上げます。

×
細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID