1. Cell Cycle/DNA Damage
    Antibody-drug Conjugate/ADC Related
  2. Telomerase
    ADC Cytotoxin
  3. Telomestatin

Telomestatin 

目录号: HY-15225
产品使用指南

Telomestatin 是一种非常有效的端粒酶 (telomerase) 抑制剂,可从 Streptomyces anulatus 3533-SV4 中分离得到。Telomestatin 选择性地促进分子内 G-quadruplexes 的形成,特别是人类端粒序列 d[T2AG3]4 的形成。Telomestatin 是一种 ADC 细胞毒素,可用于癌症研究。

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Telomestatin Chemical Structure

Telomestatin Chemical Structure

CAS No. : 265114-54-3

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Description

Telomestatin is a very potent telomerase inhibitor and can be isolated from Streptomyces anulatus 3533-SV4. Telomestatin selectively facilitates the formation of intramolecular G-quadruplexes, in particular, that produced from the human telomeric sequence d[T2AG3]4. Telomestatin is an ADC cytotoxin and can be used for cancer research[1].

IC50 & Target

Traditional Cytotoxic Agents

 

In Vitro

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, 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[1].
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[2].
Telomestatin (2-5 μM; short-time or long trem) has less effect on normal diploid human fibroblasts and ALT-positive cells[2].
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[2].
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[2].

In Vivo

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[2].

Animal Model: Mice model with U937 xenografts[2]
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.
Molecular Weight

582.50

Formula

C₂₆H₁₄N₈O₇S

CAS No.

265114-54-3

SMILES

CC1=C(N=C(C2=C(C)OC([C@@]3([H])N=C(C4=COC(C5=COC6=N5)=N4)SC3)=N2)O1)C7=NC(C8=NC(C9=NC6=CO9)=CO8)=CO7

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

TelomestatinTelomeraseADC CytotoxintelomeraseG-quadruplexesADC cytotoxinU937 cellstelomeric sequencecancerADCInhibitorinhibitorinhibit

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产品名称:
Telomestatin
目录号:
HY-15225
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