TH588,98.56%

产品编号:Bellancom-12814| CAS NO:1609960-31-7| 分子式:C13H12Cl2N4| 分子量:295.17

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-12814
750.00 杭州 北京(现货)
Bellancom-12814
1400.00 杭州 北京(现货)
Bellancom-12814
2520.00 杭州 北京(现货)
Bellancom-12814
4550.00 杭州 北京(现货)

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TH588

产品介绍 TH588 是 MTH1 (NUDT1) 高效选择性抑制剂,IC50 值 5 nM。
生物活性

TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).

体外研究

TH588 (2-10μM; 7-10 days) selectively and effectively kills U2OS, HeLa, MDA-MB-231, MCF-7, SW480, and SW620 cells with IC50s of 1.38, 0.83, 1.03, 1.08, 1.72, 0.8 μM.

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

Cell Viability Assay

Cell Line: U2OS, HeLa, MDA-MB-231, MCF-7, SW480, SW620, VH10, HDFn cells
Concentration: 2, 4, 6, 8, 10 μM
Incubation Time: 7-10 days
Result: Selectively and effectively killed U2OS, HeLa, MDA-MB-231, MCF-7, SW480, and SW620 cells with IC50s of 1.38, 0.83, 1.03, 1.08, 1.72, 0.8 μM, but was less toxic to several primary or immortalized cells.
体内研究
(In Vivo)

TH588 (30 mg/kg; s.c.; once daily for 35 days) reduces tumour growth in SW480 xenograft cancer model.

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

Animal Model: 5-6 weeks female SCID mice (SW480 xenograft cancer model)
Dosage: 30 mg/kg
Administration: Subcutaneous injection; once daily for 35 days
Result: Reduced tumour growth in SW480 xenograft cancer model.
体内研究

TH588 (30 mg/kg; s.c.; once daily for 35 days) reduces tumour growth in SW480 xenograft cancer model.

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

Animal Model: 5-6 weeks female SCID mice (SW480 xenograft cancer model)
Dosage: 30 mg/kg
Administration: Subcutaneous injection; once daily for 35 days
Result: Reduced tumour growth in SW480 xenograft cancer model.
体内研究

TH588 (30 mg/kg; s.c.; once daily for 35 days) reduces tumour growth in SW480 xenograft cancer model.

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

Animal Model: 5-6 weeks female SCID mice (SW480 xenograft cancer model)
Dosage: 30 mg/kg
Administration: Subcutaneous injection; once daily for 35 days
Result: Reduced tumour growth in SW480 xenograft cancer model.
性状Solid
溶解性数据
In Vitro: 

DMSO : 16 mg/mL (54.21 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.3879 mL 16.9394 mL 33.8788 mL
5 mM 0.6776 mL 3.3879 mL 6.7758 mL
10 mM 0.3388 mL 1.6939 mL 3.3879 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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 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 (8.47 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.47 mM,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;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
  • 2.

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

    Solubility: ≥ 2.5 mg/mL (8.47 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.47 mM,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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.47 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.47 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    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玉米油中,混合均匀。

*以上所有助溶剂都可在 西域 网站选购。
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 6 months
-20°C 1 month
参考文献

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