同义名 :	-
	CAS号 :	1051387-90-6
	货号 :	A708911
	分子式 :	C22H17FN4O5S
	纯度 :	99%+
	分子量 :	468.46
	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 :	-
	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.