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EDO-S101
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EDO-S101图片
CAS NO:1236199-60-2
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
Tinostamustine
产品介绍
EDO-S101 (Tinostamustine) 是HDAC的广谱抑制剂;抑制HDAC1HDAC2HDAC3IC50值分别为 6 nM,9 nM,9 nM 和 25 nM。
生物活性

EDO-S101 (Tinostamustine) is a panHDACinhibitor; inhibitsHDAC6,HDAC1,HDAC2andHDAC3withIC50values 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)

EDOS101 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. EDO-S101 triggers apoptosis and shows strong antitumor activity in HL60 and Daudi cells. Initialin vitroexperiments 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].

体内研究
(In Vivo)

Intracellular HDAC inhibition of EDO-S101, 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 EDO-S101 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 EDO-S101[1].

Clinical Trial
分子量

415.36

性状

Solid

Formula

C19H28Cl2N4O2

CAS 号

1236199-60-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL(240.76 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.4076 mL12.0378 mL24.0755 mL
5 mM0.4815 mL2.4076 mL4.8151 mL
10 mM0.2408 mL1.2038 mL2.4076 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

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

  • 1.

    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); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (6.02 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
*以上所有助溶剂都可在本网站选购。