1. Cell Cycle/DNA Damage
  2. Telomerase
  3. Telomerase-IN-8

Telomerase-IN-8 是一种口服活性的 telomerase 抑制剂,IC50 值为 0.98 μM。Telomerase-IN-8 对多种肿瘤细胞系 (包括 PC3、Bcap-37、MGC-803 和 HepG2) 表现出显著的抗增殖活性。Telomerase-IN-8 在 S180 肉瘤或 HepG2 肝癌异种移植小鼠中展现出显著的抗肿瘤功效。Telomerase-IN-8 可用于端粒酶靶向抗癌研究。

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Telomerase-IN-8

Telomerase-IN-8 Chemical Structure

CAS No. : 1884341-01-8

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Telomerase-IN-8 is an orally active telomerase inhibitor, with an IC50 value of 0.98 μM. Telomerase-IN-8 exhibits potent antiproliferative activity against multiple tumor cell lines, including PC3, Bcap-37, MGC-803 and HepG2. Telomerase-IN-8 demonstrates potent antitumor efficacy in S180 sarcoma or HepG2 hepatoma xenograft mice. Telomerase-IN-8 can be used for the study of telomerase-targeted anticancer[1].

体外研究
(In Vitro)

Telomerase-IN-8 (Compound 13i) (48 h) 对 PC3、Bcap-37、MGC-803 和 HepG2 肿瘤细胞显示出强效抗增殖活性,IC50 值分别为 4.87 μM、3.37 μM、2.96 μM 和 2.45 μM[1]
Telomerase-IN-8 (48 h) 对人正常 GES-1 和 L-02 细胞显示出低毒性,IC50 值分别为 1.64 mM 和 1.62 mM[1]
Telomerase-IN-8 在 MGC-803 细胞提取物中对人端粒酶修饰 TRAP 实验显示出强效抑制活性,IC50 值为 0.98 μM[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Telomerase-IN-8 (Compound 13i) (60 mg/kg,口服,每日一次,连续 10 天) 在 S180 肉瘤或 HepG2 肝癌异种移植昆明小鼠中表现出显著的抗肿瘤功效[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: S180 sarcoma cells or HepG2 hepatoma cells (2 × 106 cells in 0.2 mL sterile normal saline, prepared from 7-day-old tumor ascites) were subcutaneously implanted into the right front armpit of Kunming mice [1]
Dosage: 60 mg/kg
Administration: p.o., once daily, 10 consecutive days
Result: Achieved tumor growth inhibition (TGI) rates of 48.9% and 46.1% in S180 sarcoma-bearing and HepG2 hepatoma-bearing Kunming mice .
Showed no significant changes in body weight.
分子量

459.58

Formula

C28H33N3O3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Telomerase-IN-8
目录号:
HY-204056
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