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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMBC-11 trisodium saltCat. No.: HY-107093ACAS No.: 387877-45-4分式: CHNNaOP分量: 577.15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 H2O : 125 mg/mL (216.58 mM; Need ultrasonic)

2、Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.7327 mL 8.6633 mL 17.3265 mL5 mM 0.3465 mL 1.7327 mL 3.4653 mL10 mM 0.1733 mL 0.8663 mL 1.7327 mL請根據(jù)產(chǎn)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 MBC-11 trisodium salt線的、靶向雙膦酸酯與抗代謝物阿糖胞苷 (Ara-C) 共價結(jié)合的偶聯(lián)物。具有治療腫瘤性病 (TIBD) 的潛。體外研究MBC

3、-11 shows similar activity profiles and significantly inhibits growth of all three cell lines between 10-8 and10-4 M. MBC-11 decreases KAS-6/1 cell growth from approximately 56% at 10-8 M to 6% at 10-5 M 1Cell Proliferation Assay 11/2 Master of Small Molecules 您邊的抑制劑師www.MedChemECell Line: Human mul

4、tiple myeloma cell lines (KAS-6/1, DP-6, KP-6).Concentration: Between 10-8 and 10-4 M.Incubation Time: 48 hours.Result: Significantly inhibited multiple myeloma cell proliferation of each cell line at the majorityof the tested concentrations.體內(nèi)研究 MBC-11 (0.04 g/day, s.c.) has a lower incidence of bo

5、ne metastases of 40% compared to those treated withPBS (90%) or 0.04 g/day zoledronate (100%). MBC-11 also significantly decreases bone tumor burdencompared to PBS- or zoledronate-treated mice 1.Weight gained in mice treated with up to 500 g/day of MBC-11 is similar to the PBS treated group 1.These

6、results demonstrate that MBC-11 decreases bone tumor burden, maintains bone structure, and mayincrease overall survival, warranting further investigation as a treatment for tumor-induced bone disease(TIBD) 1.Animal Model: Approximately four-week old female Balb/c mice inoculated (s.c. injection into

7、 theirmammary fatpads) with 500,000 4T1/luc cells at day 0 (breast tumor model) 1.Dosage: 0.04, 0.4, or 4.0 g/day.Administration: S.C. daily from day 7 to 21.Result: 47% of 17 mice treated with MBC-11 had detectable bone metastases.REFERENCES1. Reinholz MM, et al. A promising approach for treatment of tumor-induced bone diseases: utilizing bisphosphonate derivatives ofnucleoside antimetabolites. Bone. 2010 Jul;47(1):12-22.McePdfHeightCaution: Product has not been fully validated for medical applications.For rese

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