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265114-54-3

中文名稱 TELOMESTATIN
英文名稱 telomestatin
CAS 265114-54-3
分子式 C26H14N8O7S
分子量 582.504
MOL 文件 265114-54-3.mol
265114-54-3 結(jié)構(gòu)式 265114-54-3 結(jié)構(gòu)式

基本信息

中文別名
替莫美他汀
化合物 T28942
英文別名
GM 95
SOT 095
telomestatin
(R)-Telomestatin
YVSQVYZBDXIXCC-INIZCTEOSA-N
3,7,11,15,19,23,27-Heptaoxa-31-thia-33,34,35,36,37,38,39,40-octaazanonacyclo[28.2.1.12,5.16,9.110,13.114,17.118,21.122,25.126,29]tetraconta-2(40),4,6(39),8,10(38),12,14(37),16,18(36),20,22(35),24,26(34),28,30(33)-pentadecaene, 4,8-dimethyl-, (1R)-

物理化學(xué)性質(zhì)

密度2.01±0.1 g/cm3(Predicted)
酸度系數(shù)(pKa)0.31±0.20(Predicted)

常見問題列表

生物活性
Telomestatin 是一種非常有效的端粒酶 (telomerase) 抑制劑,可從 Streptomyces anulatus?3533-SV4 中分離得到。Telomestatin 選擇性地促進(jìn)分子內(nèi) G-quadruplexes 的形成,特別是人類端粒序列 d[T2AG3]4 的形成。Telomestatin 是一種 ADC 細(xì)胞毒素,可用于癌癥研究。
靶點(diǎn)

Traditional Cytotoxic Agents

體外研究

Telomestatin (0-50 μM) promotes or stabilizes the formation of the intramolecular G-quadruplex. At the DNA concentrations of 0.005 and 0.2 μM, EC 50 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 (2-10?μM) effects the expression of DN-hTERT on telomerase activity and telomere length, at 10?μM,the expression of DN-hTERT shows a significant reduction of telomerase activity. Additionally, at 2?μM?, 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 (5?μM; short-time 3 days) exposure has no affect the viability of normal human fibroblasts BJ or IMR-90; however, 5?μM?of telomestatin reduces the viability of GM847 cells.Telomestatin (2 μM; 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.

體內(nèi)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?mm 3 compared with telomestatin treated with a mean tumor volume of 291?mm 3 .Exhibited no adverse effects (body weight loss, clinical signs or survival).Reduced U937 cells in bone marrow and recovered the normal hematopoiesis in mice.
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