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Telomestatin  ≥95%

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产品描述：基本信息 产品编号： T10664  产品名称： Telomestatin CAS: 265114-54-3   储存条件 粉末 -20℃ 四年     分子式： C26H14N8O7S 溶于液体     分子量 582.50     化学名：  (R)-Telomestatin Solubility (25°C)：   体外:   DMSO   Water   Ethanol   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   生物活性 产品描述 一种非常有效的端粒酶抑制剂，可从 Streptomyces anulatus 3533-SV4 中分离得到。 靶点 Traditional Cytotoxic Agents 体外研究 Telomestatin (0-50μM) promotes or stabilizes the formation of the intramolecular G-quadruplex. At the DNA concentrations of 0.005 and 0.2 µM, EC50 values of 0.03 µM and 0.53 µM telomestatin are found. In a parallel experiment with the mutated oligonucleotide d[T2AGAG]4, there is no conversion of the mutated sequence to a G-quadruplex structure by telomestatin. Telomestatin (2-10μM) effects the expression of DN-hTERT on telomerase activity and telomere length, at 10μM，the expression of DN-hTERT shows a significant reduction of telomerase activity. Additionally, at 2μM , the terminal restriction fragment (TRF) length of U937 cells shortens progressively from 9.5 to 3.8 kb at population doubling (PD) 20 in U937 cells . Telomestatin (2-5 μM; short-time or long trem) has less effect on normal diploid human fibroblasts and ALT-positive cells. Telomestatin (5μM; short-time 3 days) exposure has no affect the viability of normal human fibroblasts BJ or IMR-90; however, 5μM of telomestatin reduces the viability of GM847 cells. Telomestatin (2μM; long-term 10-50 days) does not significantly change the proliferation rate or viability to that of control cells in BJ or IMR-90 cells and also does not change the proliferation of GM847 cells 体内研究 Telomestatin (intraperitoneal injection; 3-15 mg/kg; two times a week; 4 weeks) decreases tumor telomerase activity and inhibits the growth of U937 xenografts. Systemic administrations of 3 mg/kg or 9 mg/kg or 15 mg/kg of telomestatin decreases tumor telomerase activity by 60.2%, 74% and 92.5% compared to control, respectively.   Animal Model: Mice model with U937 xenografts Dosage: 3-15 mg/kg Administration: Intraperitoneal injection; 3-15 mg/kg; two times a week; 4 weeks Result: Treated with PBS for 21 days had a mean tumor volume of 1395 mm3 compared with telomestatin treated with a mean tumor volume of 291 mm3.Exhibited no adverse effects (body weight loss, clinical signs or survival).Reduced U937 cells in bone marrow and recovered the normal hematopoiesis in mice.
保存条件：-20℃

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