生物活性分子抑制剂ZZW-115 hydrochloride

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ZZW-115 hydrochloride  纯度: 98.00%

ZZW-115 hydrochloride 是一种有效的 NUPR1 抑制剂,Kd 为 2.1 μM,通过坏死和凋亡 (apoptosis) 诱导肿瘤细胞死亡。具有抗癌活性。

ZZW-115 hydrochloride

ZZW-115 hydrochloride Chemical Structure

CAS No. : 10122-45-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥4420 In-stock
5 mg ¥3500 In-stock
10 mg ¥5800 In-stock
50 mg   询价  
100 mg   询价  

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ZZW-115 hydrochloride 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Targeted Diversity Library

生物活性

ZZW-115 hydrochloride is a potent NUPR1 inhibitor, with a Kd of 2.1 μM. ZZW-115 hydrochloride induces tumor cell death by necroptosis and apoptosis. Anticancer activity[1][2].

体外研究
(In Vitro)

ZZW-115 hydrochloride (0.1-33 μM; 72 hours) is efficient in killing cancer cells, with an IC50 in the range of 0.84 μM (ANOR) to 4.93 μM (HN14)[1].
ZZW-115 hydrochloride (0-100 μM; 24-72 hours) is efficient to kill these tumor cells with an IC50 in the range of 0.42 μM (Hep2G cells) to 7.75 μM (SaOS-2 cells)[1].
ZZW-115 hydrochloride induces pancreatic cell death by necrosis and apoptosis. ZZW-115 hydrochloride treatment induces a decrease in ATP production and induces a ROS overproduction[1].
LDH release is significantly higher in ZZW-115 hydrochloride-treated cells (MiaPaCa-2, 02-063, LIPC, Foie8b, and HN14 cells) than in control cells in a concentration-dependent manner. Similarly, caspase 3/7 activity is also greater in ZZW-115 hydrochloride-treated cells. These experiments demonstrated that ZZW-115 hydrochloride exerted both pronecrotic and proapoptotic effects[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: ANOR cells, MiaPaCa-2, 02-063, 01008, LIPC, 02136, HN01,01046, AOIPC, Foie8b, HN14 cells
Concentration: 0.1- 33 μM
Incubation Time: 72 hours
Result: Was efficient in killing cancer cells, with an IC50 in the range of 0.84 μM (ANOR) to 4.93 μM (HN14).

Cell Proliferation Assay[1]

Cell Line: U87, A375, U2OS, SaOS-2, HT29, SK-CO-1, LS174T, H1299 and H358, HepG2, PC3, THP-1, Daudi, Jurkat and MDA-MB-231 cells
Concentration: 0-100 μM
Incubation Time: 24 or 72 hours
Result: Was efficient to kill these tumor cells with an IC50 in the range of 0.42 μM (Hep2G cells) to 7.75 μM (SaOS-2 cells).

体内研究
(In Vivo)

ZZW-115 hydrochloride (0.5-5 mg/kg; injection; daily for 30 days) inhibits the growth of pancreatic xenografted tumors[1].
ZZW-115 hydrochloride (5 mg/kg for 30 days; immunocompetent C57BL/6 mice were orthotopically implanted with Panc02 cells) treatment shows the tumor size is almost unmeasurable in some cases[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NMRI-Foxn1nu/Foxn1nu mice (nude mice) xenografted with MiaPaCa-2 cells [1]
Dosage: 5, 2.5, 1.0, or 0.5 mg/kg
Administration: Injection; daily for 30 days
Result: When the mice were injected with 5 mg/kg ZZW-115 hydrochloride, the tumors stopped growing a few days after treatment and their size decreased progressively, almost disappearing at the end of the treatment.

分子量

573.97

Formula

C24H34Cl3F3N4S

CAS 号

10122-45-9

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, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL (145.18 mM; Need ultrasonic)

H2O : 60 mg/mL (104.54 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7423 mL 8.7113 mL 17.4225 mL
5 mM 0.3485 mL 1.7423 mL 3.4845 mL
10 mM 0.1742 mL 0.8711 mL 1.7423 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 (stored under nitrogen)。-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: ≥ 6.25 mg/mL (10.89 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (10.89 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 62.5 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: ≥ 6.25 mg/mL (10.89 mM); Clear solution

    此方案可获得 ≥ 6.25 mg/mL (10.89 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 62.5 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
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Santofimia-Castaño P, et al. Ligand-based design identifies a potent NUPR1 inhibitor exerting anticancer activity via necroptosis. J Clin Invest. 2019;129(6):2500-2513. Published 2019 Mar 28.

    [2]. Santofimia-Castaño P, et al. Targeting the Stress-Induced Protein NUPR1 to Treat Pancreatic Adenocarcinoma. Cells. 2019;8(11):1453. Published 2019 Nov 17.

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