中文名 | SPI 112 |
英文名 | SPI 112 |
别名 | 化合物SPI 112 (Z)-3-(2-(5-(N-(4-氟苄基)氨磺酰基)-2-氧代二氢吲哚-3-亚基)肼基)苯甲酸 |
英文别名 | SPI112 SPI 112 SPI-112 (Z)-3-(2-(5-(N-(4-Fluorobenzyl)sulfamoyl)-2-oxoindolin-3-ylidene)hydrazinyl)benzoic acid Benzoic acid, 3-[(2Z)-2-[5-[[[(4-fluorophenyl)methyl]amino]sulfonyl]-1,2-dihydro-2-oxo-3H-indol-3-ylidene]hydrazinyl]- |
CAS | 1051387-90-6 |
化学式 | C22H17FN4O5S |
分子量 | 468.46 |
密度 | 1.52±0.1 g/cm3(Predicted) |
熔点 | >300 °C |
溶解度 | 溶于DMSO |
酸度系数 | 4.15±0.10(Predicted) |
存储条件 | -20℃ |
体外研究 | SPI-112 has a polar -NO 2 or a negatively charged -COOH group and has no detectable cellular activity, suggesting that SPI-112 is not cell permeable. In surface plasmon resonance (SPR) binding assay, SPI-112 displays a 1:1 stoichiometric binding kinetics to SHP2 with a kinetic constant K D of 1.30 µM. Enzyme kinetic data obtained with SPI-112 are best fitted with the competitive inhibition model (K i of 0.8 µM), suggesting that SPI-112 interacts with the catalytic site of SHP2. |
参考资料 展开查看 | 1: Inhibition of cellular Shp2 activity by a methyl ester analog of SPI-112.Chen L, Pernazza D, Scott LM, Lawrence HR, Ren Y, Luo Y, Wu X, Sung SS, Guida WC, Sebti SM, Lawrence NJ, Wu J. Biochem Pharmacol. 2010 Sep 15;80(6):801-10. doi: 10.1016/j.bcp.2010.05.019. Epub 2010 May 25.PMID: 20510203 Free PMC ArticleSimilar articles |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.135 ml | 10.673 ml | 21.347 ml |
5 mM | 0.427 ml | 2.135 ml | 4.269 ml |
10 mM | 0.213 ml | 1.067 ml | 2.135 ml |
5 mM | 0.043 ml | 0.213 ml | 0.427 ml |
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