NSC-87877
目录号 : KM18717 CAS No. : 56990-57-9 纯度 : ≥98%

NSC-87877 是一种有效的Shp2 和Shp1 蛋白质酪氨酸磷酸酶抑制剂,IC50 值分别为0.318 μM 和0.355 μM。NSC-87877还抑制双特异性磷酸酶26 (DUSP26)。

规格 价格 是否有货 数量
5mg
In-stock
10mg
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25mg
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50mg
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100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

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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).

体外研究

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.

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

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

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.
分子式
C19H13N3O7S2
分子量
459.45
CAS号
56990-57-9
运输条件

Room temperature in continental US; may vary elsewhere.

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)

溶解性数据
In Vitro: 

DMSO : 25 mg/mL (54.41 mM; ultrasonic and warming and heat to 60°C)

配制储备液
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
*

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 (sealed storage, away from moisture)。-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: ≥ 2.08 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 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。

  • 2.

    请依序添加每种溶剂: 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。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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