Ricolinostat (ACY-1215)

For research use only. Not for use in humans.

目录号:S8001 别名: Rocilinostat

Ricolinostat (ACY-1215)  Chemical Structure

CAS No. 1316214-52-4

Ricolinostat (ACY-1215, Rocilinostat) 是一种选择性HDAC6抑制剂,无细胞试验中IC50为5 nM,作用于HDAC6比作用于HDAC1/2/3(I型HDACs)选择性高10倍以上,对HDAC8具有微弱的作用活性,对HDAC4/5/7/9/11, Sirtuin1和Sirtuin2具有最小的作用活性。Ricolinostat (ACY-1215) 可抑制细胞增殖并促进凋亡。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1566.47 现货
RMB 900.21 现货
RMB 4664.38 现货
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客户使用Selleck生产的Ricolinostat (ACY-1215) 发表文献42篇:

产品安全说明书

HDAC抑制剂选择性比较

生物活性

产品描述 Ricolinostat (ACY-1215, Rocilinostat) 是一种选择性HDAC6抑制剂,无细胞试验中IC50为5 nM,作用于HDAC6比作用于HDAC1/2/3(I型HDACs)选择性高10倍以上,对HDAC8具有微弱的作用活性,对HDAC4/5/7/9/11, Sirtuin1和Sirtuin2具有最小的作用活性。Ricolinostat (ACY-1215) 可抑制细胞增殖并促进凋亡。Phase 2。
特性 ACY-1215作用于4名健康捐献者的PHA刺激的PBMCs,与pan-HDAC抑制剂SAHA相比,具有更低的细胞毒性。
靶点
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
体外研究

ACY-1215是一种异羟肟酸类衍生物。ACY-1215作用于HDAC1, HDAC2, 和 HDAC3 (I型 HDACs)效果分别低12,10, 和 11倍。ACY-1215最低活性作用于(IC50>1μM) HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1,和 Sirtuin2,对HDAC8(IC50=0.1μM)具有轻微的作用活性。ACY-1215作用于T细胞毒性的IC50值为2.5μM。ACY-1215作用于骨髓(BM)环境,克服BMSCs和细胞因子赋予的肿瘤细胞生长和存活。ACY-1215与Bortezomib联用,诱导协同抗MM活性。ACY-1215在非常低的剂量时,诱导强有力的α-tubulin乙酰化,只有在较高剂量时,触发组蛋白H3和H4组蛋白赖氨酸的乙酰化,证实其对HDAC6活性的特定抑制效果。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RPMI8226 M3\jd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUG5XYRNUUN3ME2xOFY5KMLzIEOxNEBvVQ>? NVHNTGhzOjZ2NEOwO|g>
A-172 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUSxV3Q5OTEEoH7N NWe0VINnOjRxNEigbC=> NIHCOVlqdmirYnn0d{Bk\WyuIHfyc5d1cCC2aX3lJIRmeGWwZHXueIx6 NGPZOGozPjF3MEO0NC=>
U87MG M2j5e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HCRlExyqCwTR?= MkG5NlQwPDhiaB?= NWPvXGs4cW6qaXLpeJMh[2WubDDndo94fGhidHnt[UBl\XCnbnTlcpRtgQ>? MYOyOlE2ODN2MB?=
Hbl-1 NXTZSIp5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnz1OFghcA>? MXzJR|UxRTFwNjFOwG0> NFr5cnAzPjFzNkK3NC=>
OCI-Ly10 MoHrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jkPVQ5KGh? MUPJR|UxRTBwOTFOwG0> MWOyOlEyPjJ5MB?=
Riva NHzq[GJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLNOFghcA>? NX[2VXBuUUN3ME2yMlIh|ryP MVuyOlEyPjJ5MB?=
Su-DHL2 MofLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYC0PEBp MVfJR|UxRTNwMzFOwG0> MnnYNlYyOTZ{N{C=
OCI-Ly1 M3;6dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfRcpFnPDhiaB?= M1zCXGlEPTB;Mj60JO69VQ>? NXz1NWdnOjZzMU[yO|A>
OCI-Ly7 MlvxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPzUFdYPDhiaB?= MUPJR|UxRTFwMjFOwG0> MY[yOlEyPjJ5MB?=
Su-DHL4 NGjmUGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITSOGs1QCCq MnvJTWM2OD12Lkeg{txO MkTuNlYyOTZ{N{C=
Su-DHL6 NEHHeXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;oOFghcA>? NVLKTIJOUUN3ME2zMlIh|ryP M122[FI3OTF4Mkew
Hbl-2 NFPIe|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTlcIVFPDhiaB?= M3PyVWlEPTB;MT65JO69VQ>? NICzZnczPjFzNkK3NC=>
Jeko-1 Mn3KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHRSJRnPDhiaB?= MojaTWM2OD1zLkWg{txO MX6yOlEyPjJ5MB?=
Jvm-2 M3zMZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFHMVHc1QCCq M3fjSWlEPTB;ND6wJO69VQ>? MnvTNlYyOTZ{N{C=
Rec-1  M2P0cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTEXoU1QCCq M4jhV2lEPTB;Mj6zJO69VQ>? MV6yOlEyPjJ5MB?=
CCL-119 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX20PEBp M4OxXWlEPTB;MT63JO69VQ>? MlrDNlYyOTZ{N{C=
H9 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUG0PEBp M4j5bWlEPTB;MT6yJO69VQ>? MW[yOlEyPjJ5MB?=
HH NEDSNIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVX6V|dQPDhiaB?= MX7JR|UxRTJwNTFOwG0> M3P0ZVI3OTF4Mkew
Sup-T1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX20PEBp MkTUTWM2OD1zLk[g{txO NY\GWIlMOjZzMU[yO|A>
MM.1S MWPGeY5kfGmxbjDBd5NigQ>? NXi2bYxlOC13zszN MkjSOkBp NV7OXlFScW6lcnXhd4V{KGGlZYT5cIF1\WRizsGteJVjfWyrbh?= NELQNoczOjJ4Mke2NC=>
MM.1S NYHDZoxMTnWwY4Tpc44hSXO|YYm= MlPuNE4zPS9zzszN MVOxPEBp NEHpc5BqdmO{ZXHz[ZMh[WOndInsZZRm\CEQsT30eYJ2dGmw MV6yNlI3Ojd4MB?=
MM.1R M33CXWZ2dmO2aX;uJGF{e2G7 MVSwMlI2NzIQvF2= M3vhXFE5KGh? MYfpcoNz\WG|ZYOgZYNmfHmuYYTl[EDPuS22dXL1cIlv MY[yNlI3Ojd4MB?=
RPMI8226  MYHGeY5kfGmxbjDBd5NigQ>? MV2wMlI2NzIQvF2= NEnVXZkyQCCq NFPNbIhqdmO{ZXHz[ZMh[WOndInsZZRm\CEQsT30eYJ2dGmw M3rJWVIzOjZ{N{[w
MM.1S MnHvR4VtdCCYaXHibYxqfHliQYPzZZk> NYPnR2RGOC16zszN MlrwOFghcA>? NFL1TZdl\WO{ZXHz[ZMhVU1vY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MnzyNlIzPjJ5NkC=
OPM1 NWPGc5NPS2WubDDWbYFjcWyrdImgRZN{[Xl? MoG5NE05|ryP MlX5OFghcA>? M2HmcoRm[3KnYYPld{BOVS2lZXzsJJZq[WKrbHn0fUBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> M1:yXlIzOjZ{N{[w
RPMI NX3oVXNuS2WubDDWbYFjcWyrdImgRZN{[Xl? MnjyNE05|ryP MY[0PEBp NF\iW4Rl\WO{ZXHz[ZMhVU1vY3XscEB3cWGkaXzpeJkhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NX;0PY43OjJ{NkK3OlA>
MM.1R NHXpb2JE\WyuIG\pZYJqdGm2eTDBd5NigQ>? NFW4ZosxNTkQvF2= MUC0PEBp NUO2WYR5\GWlcnXhd4V{KE2PLXPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NHnZWngzOjJ4Mke2NC=>
LR5 M3:4Z2NmdGxiVnnhZoltcXS7IFHzd4F6 MXqwMVjPxE1? MXO0PEBp NXLoWnNN\GWlcnXhd4V{KE2PLXPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NU[wNVljOjJ{NkK3OlA>
OPM2 NHXRNXhE\WyuIG\pZYJqdGm2eTDBd5NigQ>? MXywMVjPxE1? MXS0PEBp NVPYTlJT\GWlcnXhd4V{KE2PLXPlcIwhfmmjYnnsbZR6KGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M3Hab|IzOjZ{N{[w

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Ac-α-tubulin / Ac-Histone H4 ; 

PubMed: 31015208     


Ricolinostat promotes the accumulation of acetylated (Ac) α-tubulin. MM cells were treated with the indicated concentrations of ricolinostat for 24 hours. Protein expression was measured by immunoblotting. 

Survivin / P21 / CDC2 / p53 / p-p53(S392) / Cyclin A2 / Cyclin B1; 

PubMed: 30050135     


Western blot analysis of G2/M phase cell cycle regulatory-proteins for 48 h

Bax / Bim / Bcl2 / Cleaved caspase-3 / Cleaved caspase-9 / Cleaved PARP; 

PubMed: 30050135     


Western blot analysis of apoptosis regulatory-proteins for 48 h

PI3K(p85) / AKT / p-AKT(S473) / PRAS40 / Rag C / mTOR / p-mTOR / ERK / p-ERK; 

PubMed: 30050135     


ACY-1215 treatment inhibited PI3K/AKT/mTOR and ERK signaling protein levels in ESCC EC109 and TE-1 cell lines for 48 h.

Ac-β-catenin(K49) / p-β-catenin / β-catenin; 

PubMed: 25546293     


Time-course immunoblot analysis of human NPCs treated with an HDAC6 inhibitor. Human NPCs were treated with HDAC6 inhibitor ACY-1215 at 5 μM for the times points indicated and the lysates immunoblotted with antibodies against β-catenin, Ac-Lys49-β-catenin, phos-Ser45 and phos-Ser33, Ser37, and Thr41. β-actin is using shown as loading control.

31015208 30050135 25546293
Immunofluorescence
β-tubulin / β-catenin; 

PubMed: 25546293     


Immunofluorescence staining for β-catenin treated with HDAC6 inhibitor in human NPCs. Cells were treated with 5 μM ACY-1215 or DMSO for 18 h and imaged with anti-β-catenin antibody (green), anti-β-tubulin antibody (red), and Hoechst 33342 (blue). Scale bar, 20 μm.  Quantification of β-catenin levels at the membrane represent two independent experiments with three fields of view each at 20× magnification. Error bars indicate standard deviation. ** and **** denote significance at p < 0.01 and p < 0.0001, respectively (unpaired t test).

25546293
Growth inhibition assay
Cell viability; 

PubMed: 31015208     


Ricolinostat decreases MM cell viability. A panel of MM cell lines was treated with the indicated concentrations of ricolinostat for 72 hours. Cell viability was measured by MTT assay.

31015208
体内研究 ACY-1215与Bortezomib 联用,作用于两个浆细胞瘤模型和弥散性MM模型,抑制肿瘤生长,并延长生存,没有显著的不利影响。比单独使用具有更显著的抗MM 活性。ACY-1215易被肿瘤组织吸收。此外,药物不会在肿瘤组织中累积,处理24小时后,血液细胞和肿瘤组织的乙酰化的α-tubulin平行下降。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:

[1]

- 合并

HDAC 酶促实验:

ACY-1215在实验 Buffer [50 mM HEPES, pH 7.4, 100 mM KCl, 0.001% Tween-20, 0.05% BSA, 和20 μM三羧甲基磷酸(TCEP)] 中溶解,然后稀释到终浓度的6倍。HDAC酶在实验Buffer中稀释到终浓度的1.5倍,与ACY-1215预温育10分钟,然后加入底物。通过滴定曲线测定,用于每种酶的FTS(HDAC1,HDAC2,HDAC3和HDAC6)和MAZ-1675(HDAC4,HDAC5,HDAC7,HDAC8,和HDAC9)量等于米氏常数(Km)。使用0.3μM 测序等级胰蛋白酶将FTS或MAZ-1675在实验 Buffer中稀释到终浓度的6倍。底物/胰蛋白酶混合物添加到酶/化合物混合物中,实验板震荡60秒,然后置于SpectraMax M5酶标仪上。监测酶促反应中的7-氨基-4-甲氧基香豆素在30分钟内的释放,肽底物中赖氨酸侧链的脱乙酰化,计算反应的线性速率。
细胞实验:

[1]

- 合并
  • Cell lines: MM cell lines, patient MM cells, and PBMCs
  • Concentrations: ~8 μM
  • Incubation Time: 48 hours
  • Method:

    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.


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: MM移植瘤SCID小鼠模型
  • Dosages: 50 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 86 mg/mL (198.38 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 433.5
化学式

C24H27N5O3

CAS号 1316214-52-4
储存条件 粉状
溶于溶剂
别名 Rocilinostat

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

技术支持

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操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 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 Signaling Pathway Map

HDAC Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID