MT-DADMe-ImmA-Methylthio-DADMe-Immucillin-A-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMT-DADMe-ImmACat. No.: HY-101496CAS No.: 653592-04-2Synonyms: Methylthio-DADMe-Immucillin A; MTDIA分式: CHNOS分量: 293.39作靶點: Others作通路: Others儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 33

2、.33 mg/mL (113.60 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.4084 mL 17.0422 mL 34.0843 mL5 mM 0.6817 mL 3.4084 mL 6.8169 mL10 mM 0.3408 mL 1.7042 mL 3.4084 mL請根據(jù)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。BIOLOGICAL ACTIVITY物活性 MT-DADMe-ImmA5-甲硫基腺苷磷

3、酸化酶的抑制劑 (MTAP)，Ki值為90 pM。IC50 & Target Ki: 90 pM (MTAP) 1體外研究Treatment of cultured cells with MT-DADMe-ImmA and MTA inhibit MTAP, increase cellular MTA1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEconcentrations, decrease polyamines, and induce apoptosis in FaDu and Cal27, two head and necksquamo

4、us cell carcinoma cell lines. The same treatment does not induce apoptosis in normal humanfibroblast cell lines (CRL2522 and GM02037) or in MCF7, a breast cancer cell line with an MTAP genedeletion. MT-DADMe-ImmA alone does not induce apoptosis in any cell line, implicating MTA as the activeagent 2.

5、體內研究 The t1/2 for onset of inhibition is 50 min with complete inhibition by 250 min. MTAP activity slowly returns,giving a biological half-life for the action of oral MT-DADMe-ImmA of 6.3 days. The time-dependent growth ofFaDu tumors in immunodeficient mice is suppressed by oral or intraperitoneal t

6、reatment with MT-DADMe-ImmA 2.PROTOCOLCell Assay 2 Cell viability is evaluated using the Alamar Blue assay. Cells are seeded onto 96-well plates at a density of104 cells/well and incubated with increasing concentrations of MT-DADMe-ImmA (100 pM to 100 M) for 4days at fixed MTA concentrations (0, 5,

7、10, and 20 M). IC50 is determined with the assay data 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Tumors were established in mice for 5 days prior to oral or intraperitoneal treatments with MT-DADMe-Administration 1 ImmA. Mice are tre

8、ated with oral dose of 21 mg/kg or an intraperitoneal dose of 5 mg/kg/day MT-DADMe-ImmA 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Evans GB, et al. Second generation transition state analogue inhibitors of human 5-methylthioadenosine phosphorylase. J Med Chem.2005 Jul 14;48(14):4679-89.2. Basu I, et al. A transition state analogue of 5-methylthioadenosine phosphorylase induces apoptosis in head and neck cancers. J BiolChem. 2007 Jul 20;282(29):21477-86.McePdfHeightCaution: Product has not been fully validated for medical a