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NSC 87877
目录号: PC10110 纯度: ≥98%
CAS No. :56990-57-9
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中文名称
NSC 87877
英文名称
NSC 87877
英文别名
5-Quinolinesulfonicacid, 8-hydroxy-7-[2-(6-sulfo-2-naphthalenyl)diazenyl]-;NSC 87877;(7E)-8-oxo-7-[(6-sulfonaphthalen-2-yl)hydrazinylidene]quinoline-5-sulfonic acid;5-Quinolinesulfonic acid, 8-hydroxy-7-(6-sulfo-2-naphthylazo)-;8-Hydroxy-7-(6-sulfo-naphthalen-2-ylazo)-quinoline-5-sulfonic acid;8-Hydroxy-7-[(6-sulfo-2-naphthyl)azo]-5-quinolinesulfonicacid;AC1NURFB;CCG-37311;NCIStruc1_001562;NCIStruc2_001738;NSC-87877;NSC87877;8-HYDROXY-7-[(6-SULFO-2-NAPHTHYL)AZO]-5-QUINOLINESULFONIC ACID;8-oxo-7-[(6-sulfo-2-naphthalenyl)hydrazinylidene]-5-quinolinesulfonic acid;NCGC00013917;MLS006010814;8-hydroxy-7-((6-sulfo-2-naphthyl)diazenyl)-5-quinolinesulfonic acid;(E)-8-hydroxy-7-((6-sulfonaphthalen-2-yl)diazenyl)quinoline-5-sulfonic acid;8-hydroxy-7-(2-(6-sulfonaphthalen-2-yl)hydrazinyl)quinoline-5-sulfonic acid;http:////www.amadischem.com/proen/519279/;Not available
Cas No.
56990-57-9
分子式
C19H13N3O7S2
分子量
459.45
包装储存

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

NSC-87877 is a potent inhibitor of Shp2 and Shp1 protein tyrosine phosphatases (SH-PTP2 and SH-PTP1), with IC50 values of 0.318 μM, 0.355 μM shp2 and shp1, respectively. NSC-87877 also inhibits dual-specificity phosphatase 26 (DUSP26).

性状

Solid

IC50 & Target[1][2]

IC50: 0.318 μM (shp2), 0.355 μM (shp1).

体外研究(In Vitro)

NSC-87877 (0-0.5 μM, 5 days) inhibits DUSP26 function in NB cell lines.
NSC-87877 (0-0.5 μM, 5 days) results in increased p53 phosphorylation (Ser37 and Ser46) and activation.

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

Cell Viability Assay

Cell Line: p53 wild-type neuroblastoma (NB) cell lines.
Concentration: 0, 0.25, 0.5 μM.
Incubation Time: 5 dsys.
Result: Resulted in increased p53 phosphorylation (Ser37 and Ser46) and activation, increased activation of downstream p38 effector proteins (heat shock protein 27 (HSP27) and MAP kinase-activated protein kinase 2 (MAPKAPK2)) and poly ADP ribose polymerase/caspase-3 cleavage.
Inhibited DUSP26 function in NB cell lines.
Resulted in apoptosis in many cell lines at varying IC50 levels of 1.84 μM (IMR32), 6.35 μM (SK-N-SH), 8.69 μM (NB-19), 12.6 μM (SMS-KCN), 15.7 μM (SH-SY5Y), 15.8 μM (JF) and 19.0 μM (CHLA-225), respectively.
体内研究(In Vivo)

NSC-87877 (30?mg/kg, IP once daily for 15 days) possesses excellent anti- neuroblastoma activity.

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

Animal Model: Intrarenal neuroblastoma (NB) tumor mouse model in female nude mice.
Dosage: 30?mg/kg.
Administration: IP once daily for 15 days.
Result: Significantly inhibited NB tumor growth.
运输条件

Room temperature or refrigerated transportation.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献
溶解度数据
体外研究: 

H2O : 23.81 mg/mL (51.82 mM; ultrasonic and warming and heat to 60°C)

DMSO : 16.67 mg/mL (36.28 mM; ultrasonic and warming and heat to 60°C)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1765 mL 10.8826 mL 21.7652 mL
5 mM 0.4353 mL 2.1765 mL 4.3530 mL
10 mM 0.2177 mL 1.0883 mL 2.1765 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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 (sealed storage, away from moisture)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

    建议依照次序添加每种溶剂: PBS

    Solubility: 3.33 mg/mL (7.25 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.53 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (3.63 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.63 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 16.7 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 ddH?O 中,得到澄清透明的生理盐水溶液
*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

The molarity calculator equation
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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