1. Cell Cycle/DNA Damage Epigenetics
  2. HDAC
  3. Tinostamustine

Tinostamustine  (Synonyms: EDO-S101; NL-101)

目录号: HY-101780 纯度: 99.42%
COA 产品使用指南

Tinostamustine (EDO-S101) 是 HDAC 的广谱抑制剂;抑制 HDAC1HDAC2HDAC3IC50 值分别为 6 nM,9 nM,9 nM 和 25 nM。

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Tinostamustine Chemical Structure

Tinostamustine Chemical Structure

CAS No. : 1236199-60-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2420
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1 mg ¥880
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5 mg ¥2200
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10 mg ¥3200
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25 mg ¥5450
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50 mg ¥7650
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100 mg   询价  
200 mg   询价  

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tinostamustine (EDO-S101) is a pan HDAC inhibitor; inhibits HDAC6, HDAC1, HDAC2 and HDAC3 with IC50 values of 6 nM, 9 nM, 9 nM and 25 nM, respectively[1].

IC50 & Target[1]

HDAC6

6 nM (IC50)

HDAC1

9 nM (IC50)

HDAC2

9 nM (IC50)

HDAC3

25 nM (IC50)

HDAC10

72 nM (IC50)

HDAC8

107 nM (IC50)

体外研究
(In Vitro)

Tinostamustine inhibits HDAC activity in rat peripheral blood mononuclear cells (PBMCs) in a cellular assay by approximately 90% one hour after dosing with 10mg/kg i.v. HDAC inhibition in PBMCs could not be increased with higher doses up to 50mg/kg. Tinostamustine triggers apoptosis and shows strong antitumor activity in HL60 and Daudi cells. Initial in vitro experiments in HL60 cells shows an activation of the intrinsic pathway of apoptosis with cleavage of caspases 3, 9 and PARP and a marked reduction of anti-apoptotic proteins XIAP and Mcl-1[1].

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

体内研究
(In Vivo)

Intracellular HDAC inhibition of Tinostamustine, which occurs rapidly after dosing is at maximum activity already at the lowest dose of 10mg/kg and lasts for about 12-16 hours. Exposure to Tinostamustine causes a strong DNA repair response evidenced by activation of pH2AX and p53 in tumors taken from mice bearing subcutaneous human Burkitt’s lymphoma. Tumors of BL rapidly shrink or are completely eradicated after i.v. administration of Tinostamustine[1].

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

Clinical Trial
分子量

415.36

Formula

C19H28Cl2N4O2

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (240.76 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4076 mL 12.0378 mL 24.0755 mL
5 mM 0.4815 mL 2.4076 mL 4.8151 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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

In Vivo:

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 (6.02 mM); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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。
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

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)。
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
参考文献
Kinase Assay
[1]

Tinostamustine is dissolved in DMSO and added to the assay buffer solution. Tinostamustine dilutions of 5 μL of each dilution is added to 50 μL of the reaction mixture including the Fluor de Lys substrate and all of the enzymatic reactions are conducted in duplicate at 37°C for 30 minutes. After enzymatic reactions, 50 μL of 2xHDAC developer is added to each well and fluorescence intensity is measured[1].

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

Animal Administration
[1]

Rats: The duration of HDAC inhibition is assessed in 12 female rats after receiving a single dose of either vehicle or Tinostamustine (25mg/kg). Blood samples from EDO-S101 treated rats are collected 1hr, 3hr, 6hr, 16hr and 24hr post dosing (n=2 per time point). Blood sample from vehicle treated rats (n=2) are collected 24hr post dosing[1].

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

参考文献

Tinostamustine 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4076 mL 12.0378 mL 24.0755 mL 60.1888 mL
5 mM 0.4815 mL 2.4076 mL 4.8151 mL 12.0378 mL
10 mM 0.2408 mL 1.2038 mL 2.4076 mL 6.0189 mL
15 mM 0.1605 mL 0.8025 mL 1.6050 mL 4.0126 mL
20 mM 0.1204 mL 0.6019 mL 1.2038 mL 3.0094 mL
25 mM 0.0963 mL 0.4815 mL 0.9630 mL 2.4076 mL
30 mM 0.0803 mL 0.4013 mL 0.8025 mL 2.0063 mL
40 mM 0.0602 mL 0.3009 mL 0.6019 mL 1.5047 mL
50 mM 0.0482 mL 0.2408 mL 0.4815 mL 1.2038 mL
60 mM 0.0401 mL 0.2006 mL 0.4013 mL 1.0031 mL
80 mM 0.0301 mL 0.1505 mL 0.3009 mL 0.7524 mL
100 mM 0.0241 mL 0.1204 mL 0.2408 mL 0.6019 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.

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产品名称:
Tinostamustine
目录号:
HY-101780
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