SPI-112

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SPI-112  纯度: 97.06%

SPI-112 是一种有效的，选择性和竞争性的 SHP2 (PTPN11) 抑制剂，对 SHP2，蛋白酪氨酸磷酸酶 (PTP) 和 PTP1B 的 IC50 分别为 1 μM，18.3 μM 和 14.5 μM。

SPI-112

SPI-112 Chemical Structure

CAS No. : 1051387-90-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥550 In-stock
10 mg ￥500 In-stock
25 mg ￥1000 In-stock
50 mg ￥1800 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

SPI-112 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Phosphatase Inhibitor Library
  • Anti-Obesity Compound Library

生物活性

SPI-112 is a potent, selective and competitive SHP2 (PTPN11) inhibitor with IC50s of 1 μM, 18.3 μM and 14.5 μM for SHP2, protein tyrosine phosphatase (PTP) and PTP1B, respectively[1][2].

IC50 & Target

IC50: 1 μM (SHP2), 18.3 μM (PTP) and 14.5 μM (PTP1B)[2]
体外研究
(In Vitro)

SPI-112 has a polar -NO2 or a negatively charged -COOH group and has no detectable cellular activity, suggesting that SPI-112 is not cell permeable[1].
In surface plasmon resonance (SPR) binding assay, SPI-112 displays a 1:1 stoichiometric binding kinetics to SHP2 with a kinetic constant KD of 1.30 µM. Enzyme kinetic data obtained with SPI-112 are best fitted with the competitive inhibition model (Ki of 0.8 µM), suggesting that SPI-112 interacts with the catalytic site of SHP2[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.
分子量

468.46

Formula

C22H17FN4O5S
CAS 号

1051387-90-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (106.73 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1347 mL 10.6733 mL 21.3465 mL
5 mM 0.4269 mL 2.1347 mL 4.2693 mL
10 mM 0.2135 mL 1.0673 mL 2.1347 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 (protect from light)。-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。
参考文献

  • [1]. Chen L, et al. Inhibition of cellular Shp2 activity by a methyl ester analog of SPI-112. Biochem Pharmacol. 2010 Sep 15;80(6):801-10.

    [2]. Lawrence HR, et al. Inhibitors of Src homology-2 domain containing protein tyrosine phosphatase-2 (Shp2) based on oxindole scaffolds. J Med Chem. 2008 Aug 28;51(16):4948-56.

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