SPI-112

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Chemical Structure| 1051387-90-6 同义名 : -
CAS号 : 1051387-90-6
货号 : A708911
分子式 : C22H17FN4O5S
纯度 : 99%+
分子量 : 468.458
MDL号 : MFCD31620831
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(106.73 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The protein tyrosine phosphatase (PTP) Shp2 (PTPN11) is an attractive target for anticancer drug discovery because it mediates growth factor signaling and its gain-of-function mutants are causally linked to leukemias[3]. SPI-112 is a cell-impermeable and selective inhibitor of Shp2 with an IC50 value of 1 µM in cell-free assays[4]. In SPR binding assay, SPI-112 displayed a 1:1 stoichiometric binding kinetics to Shp2 with a kinetic constant (KD) of 1.30±0.14 µM and the association and dissociation rates of Ka=2.24×104/Ms and KD=0.029/s. Shp2 PTP activity and function were inhibited in cells treated with SPI-112Me, a prodrug of SPI-112, indicating that SPI-112Me is a cell-active Shp2 PTP inhibitor[3].
作用机制 SPI-112 bound to Shp2 by surface plasmon resonance (SPR)[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.67mL

2.13mL

1.07mL

21.35mL

4.27mL

2.13mL
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.

[3]Chen L, Pernazza D, Scott LM, Lawrence HR, Ren Y, Luo Y, Wu X, Sung SS, Guida WC, Sebti SM, Lawrence NJ, Wu J. Inhibition of cellular Shp2 activity by a methyl ester analog of SPI-112. Biochem Pharmacol. 2010 Sep 15;80(6):801-10.

[4]Lawrence HR, Pireddu R, Chen L, Luo Y, Sung SS, Szymanski AM, Yip ML, Guida WC, Sebti SM, Wu J, Lawrence NJ. 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.