1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETPI-1Cat. No.: HY-100463CAS No.: 79756-69-7分式: CHClO分量: 253.08作靶點: Phosphatase作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 50 mg/mL (197.57 mM; Need ultraso

2、nic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.9513 mL 19.7566 mL 39.5132 mL5 mM 0.7903 mL 3.9513 mL 7.9026 mL10 mM 0.3951 mL 1.9757 mL 3.9513 mL請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內實驗 請根據您的實驗動物和給藥式選擇適當的溶解案，配制前請先配制澄清的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的作液，建議您現現配，當天使；澄清的儲備液可以根據儲存條件，適當保存；

3、以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (9.88 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (9.88 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (9.88 mM); Clear

4、solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 TPI-1是SHP-1的抑制劑；抑制重 組SHP-1的IC50值為40 nM。IC50 & Target IC50: 40 nM (recombinant SHP-1) 1體外研究 SHP-1 has been implicated as a potential cancer therapeutic target. TPI-1 is effective starting at 10 ng/mL inincreasing SHP-1 ph

5、ospho-substrates pLck-pY394. TPI-1 selectively increases SHP-1 phospho-substrates(pLck-pY394, pZap70 and pSlp76) in Jurkat T cells but has little effects on pERK1/2 or pLck-pY505. TPI-1induces mouse splenic-IFN+ cells and induces IFN+ cells in human peripheral blood 1.體內研究 TPI-1 inhibits the growth

6、of B16 melanoma tumors in mice at a tolerated oral dose in a T cell-dependentmanner but has little effects on B16 cell growth in culture. TPI-1 thus also increases pLck-pY394 and IFN+cells in mice. TPI-1 also inhibits B16 tumor growth and prolongs tumor mice survival as a tolerated s.c. agent1.PROTO

7、COLAnimal Mice: For in vivo induction of pLck-pY394 and IFN+ cells in mice, C57BL/6J mice are treated with PBS orAdministration 1 TPI-1 (1 or 3 mg/kg, s.c.) for 4 days. Spleens are harvested one hour post-treatment on day 4 and processedinto splenocytes, which are used for assessing pLck-pY394 level

8、s by SDS/Western blotting and forquantification of IFN+ cells by ELISPOT assays. Mice are also treated with TPI-1 (10 mg/kg, daily, s.c.) toevaluate the toxicity of the compounds in vivo 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Kundu S, et al. Novel SHP-1 inhibitors tyrosine phosphatase inhibitor-1 and analogs with preclinical anti-tumor activities as tolerated oralagents. J Immunol. 2010 Jun 1;184(11):6529-36.McePdfHeightCaution: Product has not been fully validated for medical app