2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis
  4. Ricolinostat

Ricolinostat  (Synonyms: ACY-1215; Rocilinostat)

目录号: HY-16026 纯度: 99.83%
COA 产品使用指南

摩尔计算器

Ricolinostat (ACY-1215) 是一种有效，选择性的 HDAC6 抑制剂，IC50 为 5 nM。ACY-1215 也可抑制 HDAC1，HDAC2 和 HDAC3，IC50 分别为 58，48 和 51 nM。

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Ricolinostat Chemical Structure

Ricolinostat Chemical Structure

CAS No. : 1316214-52-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥715
In-stock
1 mg ￥261
In-stock
5 mg ￥650
In-stock
10 mg ￥990
In-stock
50 mg ￥2800
In-stock
100 mg ￥4850
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Ricolinostat 相关抗体

Top Publications Citing Use of Products

    Ricolinostat purchased from MCE. Usage Cited in: Biomed Pharmacother. 2019 Jan;109:2464-2471.  [Abstract]

    The expression of IL-1β and IL-6 in human primary chondrocytes and C28/I2 cells is tested by western blot analysis with the treatment of IL-1β, DMSO and ACY-1215.

    Ricolinostat purchased from MCE. Usage Cited in: Biomed Pharmacother. 2019 Jan;109:2464-2471.  [Abstract]

    The expression of MMP-1, MMP-13 and COL2 A1 in C28/I2 cells is tested by western blot analysis with the treatment of IL-1β, DMSO and ACY-1215.

    Ricolinostat purchased from MCE. Usage Cited in: Oncogene. 2018 Nov;37(45):5952-5966.  [Abstract]

    Mouse CAFs are treated with increasing concentrations of ACY1215 for 24 h. Western blot analysis of tubulin, histone H3, histone H4, acetylated tubulin, acetylated histone H3, and acetylated histone H4.

    Ricolinostat purchased from MCE. Usage Cited in: Oncol Rep. 2017 Feb;37(2):1270-1276.  [Abstract]

    A375 cells are treated with indicated concentrations of ACY-1215. After 72 h, Western blotting assay are utilized to detect apoptosis.

    Ricolinostat purchased from MCE. Usage Cited in: Cancer Lett. 2016 Aug 28;379(1):134-142.  [Abstract]

    Inhibition of HDAC6 by HDAC6-selective inhibitors impairs the proliferation of glioblastoma cells. U87 and U251 cells are treated with HDAC6 selective inhibitors and the cells are harvested for subsequent western blot analysis.

    Ricolinostat purchased from MCE. Usage Cited in: Med Oncol. 2016 May;33(5):50.  [Abstract]

    H460 cells are treated with 0.5 μM Aorafenib and indicated concentration of HDAC6 inhibitors, CAY10603 (CAY, 0.05 μM) or ACY1215 (ACY,1 μM). The cleavage of PARP and caspase 3 also increased after cotreatment.

    查看 HDAC 亚型特异性产品:

    查看所有亚型
    HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively.

    IC50 & Target

    HDAC6

    4.7 nM (IC50)

    HDAC2

    48 nM (IC50)

    HDAC3

    51 nM (IC50)

    HDAC1

    58 nM (IC50)

    HDAC8

    100 nM (IC50)

    HDAC7

    1400 nM (IC50)

    HDAC5

    5000 nM (IC50)

    HDAC4

    7000 nM (IC50)

    体外研究
    (In Vitro)

    Ricolinostat (ACY-1215) has slight activity against HDAC8 (IC50=0.1 μM), and has minimal activity (IC50>1 μM) against HDAC4, HDAC5, HDAC7, HDAC9, HDAC11, Sirtuin1, and Sirtuin2. The effect of Ricolinostat (ACY-1215) on multiple myeloma (MM) cell viability is determined with MTT assays using MM cell lines. Exposure of MM cell lines for 48 hours results in dose-dependent decreased viability, with IC50 values ranging from 2-8μM. Ricolinostat (ACY-1215) demonstrates significant activity in the MM PS-341-resistant cell line (ANBL-6.BR), demonstrating the ability of Ricolinostat (ACY-1215) to overcome PS-341 resistance[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Ricolinostat 相关抗体:
    体内研究
    (In Vivo)

    Mice treated with Ricolinostat (ACY-1215), PS-341, or Ricolinostat plus PS-341 show a significant delay in tumor growth (P=0.01, P=0.006, and P<0.0001, respectively). Combined treatment with Ricolinostat and PS-341 shows significant suppression of tumor growth and significantly prolonged overall survival (OS) compare with the control group (17 days in the control vs 40 days in the combination-treated group, P<0.0001) and the Ricolinostat (ACY-1215)-treated group (22 days in the PS-341 group vs 40 days in the combination-treated group, P<0.0001). Weight loss in the combination-treated group is between 4% and 12% compare with the same-day control group values during treatment, with complete recovery after the last injection. As is observed in the plasmacytoma model, a significant therapeutic advantage is found by combining Ricolinostat with PS-341 compare with either agent alone[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    433.50

    Formula

    C24H27N5O3
    CAS 号
    性状

    固体

    颜色

    White to pink

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, stored under nitrogen

    *In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 50 mg/mL (115.34 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.3068 mL 11.5340 mL 23.0681 mL
    5 mM 0.4614 mL 2.3068 mL 4.6136 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (stored under nitrogen)。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.77 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.77 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。

    *In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.83%

    COA (188 KB) LCMS (262 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [1]

    The effect of Ricolinostat with or without PS-341 on the viability of MM cell lines, patient MM cells, and PBMCs is assessed by measuring MTT dye absorbance. 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 Ricolinostat (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 (2-3×104 cells/well) are incubated in 96-well culture plates with medium and different concentrations of Ricolinostat (ACY-1215), PS-341, and/or recombinant IL-6 (10 ng/mL) or IGF-1 (50 ng/mL) for 24 hours at 37°C, and tritiated thymidine incorporation is measured[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    To evaluate the in vivo anti-MM activity of Ricolinostat, male SCID mice are inoculated subcutaneously with 5×106 MM.1S cells in 100 μL of serum-free RPMI 1640 medium. When tumors are measurable, mice are treated IP with Ricolinostat 50 mg/kg dissolved in 10% DMSO in 5% dextrose in water consecutively for 5 days a week for 3 weeks; PS-341 0.5 mg/kg dissolved in 0.9% saline solution biweekly (IV) for 3 consecutive weeks; or combination with the same dosing regimen used for the individual agents. The control group receive the carrier alone at the same schedule as the combination group. Tumor size is measured every other day in 2 dimensions using calipers, and tumor volume is calculated with the formula: V=0.5(a×b2) where a is the long diameter of the tumor and b is the short diameter of the tumor. Mice are killed when the tumor reaches 2 cm3 or is ulcerated. Survival and tumor growth are evaluated from the first day of treatment until death.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Ricolinostat 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 1 year; -20°C, 6 months (stored under nitrogen)。-80°C储存时，请在1年内使用， -20°C储存时，请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3068 mL 11.5340 mL 23.0681 mL 57.6701 mL
    5 mM 0.4614 mL 2.3068 mL 4.6136 mL 11.5340 mL
    10 mM 0.2307 mL 1.1534 mL 2.3068 mL 5.7670 mL
    15 mM 0.1538 mL 0.7689 mL 1.5379 mL 3.8447 mL
    20 mM 0.1153 mL 0.5767 mL 1.1534 mL 2.8835 mL
    25 mM 0.0923 mL 0.4614 mL 0.9227 mL 2.3068 mL
    30 mM 0.0769 mL 0.3845 mL 0.7689 mL 1.9223 mL
    40 mM 0.0577 mL 0.2884 mL 0.5767 mL 1.4418 mL
    50 mM 0.0461 mL 0.2307 mL 0.4614 mL 1.1534 mL
    60 mM 0.0384 mL 0.1922 mL 0.3845 mL 0.9612 mL
    80 mM 0.0288 mL 0.1442 mL 0.2884 mL 0.7209 mL
    100 mM 0.0231 mL 0.1153 mL 0.2307 mL 0.5767 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Ricolinostat1316214-52-4ACY-1215 RocilinostatACY1215ACY 1215HDACApoptosisHistone deacetylasesInhibitorinhibitorinhibit

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