产品说明书

Teniposide

Print
Chemical Structure| 29767-20-2 同义名 : 替尼泊甙 ;VM26;NSC 122819;PTG.;Vehem. Abbreviations: EPT;CCRIS 2058. Brand name: Vumon;HSDB 6546
CAS号 : 29767-20-2
货号 : A102576
分子式 : C32H32O13S
纯度 : 98%
分子量 : 656.654
MDL号 : MFCD00866516
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(45.69 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 8 mg/mL clear

PO 0.5% CMC-Na 45 mg/mL suspension

生物活性
靶点

  • Topo II
描述 Type II topoisomerases are ubiquitous enzymes in all branches of life that can alter DNA superhelicity and unlink double-stranded DNA segments during processes such as replication and transcription. In cells, type II topoisomerases are particularly useful for their ability to disentangle newly-replicated sister chromosomes[3]. Teniposide is a topoisomerase II inhibitor. Teniposide (VM-26, 0.15-45 mg/L) inhibits the proliferation of Tca8113 cells in a dose-dependent manner, with an IC50 of 0.35 mg/L. Teniposide (5 mg/L) induces apoptosis of Tca8113 cells. Teniposide (5.0 mg/L) causes cell arrested at G2/M phase in Tca8113 cells[4].Teniposide (0.5 mg/kg, i.p.) significantly increases micronucleated polychromatic erythrocyte (MNPCE) frequencies, which is directly related to bone marrow toxicity as significant suppression of bone marrow is noted. Teniposide (24 mg/kg, i.p.) markedly decreases the frequencies of BrdU-labelled sperm. Teniposide (12, 24 mg/kg, i.p.) also dramatically induces disomic sperm in the germ cell of male mice[5]. Teniposide is active on primary cultured glioma cells from patients, when the level of miR-181b is high in the cells, with an IC50 of 1.3 ± 0.34 μg/mL. Cells treated with teniposide with low MDM2 have decreased viability compared with control cells, and the IC50 decreases from 5.86 ± 0.36 μg/mL to 2.90 ± 0.35 μg/mL upon MDM2 suppression. Teniposide also inhibits the viability of glioma cell with high level of miR-181b, through mediation of MDM2[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00198991 Adult Acute Lymphocytic Leukem... 展开 >>ia 收起 << Phase 4 Unknown - Germany ... 展开 >> University of Frankfurt, Medical Dept. II Recruiting Frankfurt, Germany, 60590 Contact: Dieter Hoelzer, MD,PhD    ++49(0)69 6301 5194    hoelzer@em.uni-frankfurt.de    Contact: Nicola Goekbuget, MD    ++49(0)69 6301 6365    goekbuget@em.uni-frankfurt.de    Principal Investigator: Dieter Hoelzer, MD,PhD          Sub-Investigator: Nicola Goekbuget, MD 收起 <<
NCT02086942 Multiple Myeloma Phase 2 Recruiting August 2017 China, Jiangsu ... 展开 >> Jinling Hospital Recruiting Nanjing, Jiangsu, China, 210002 Contact: zhai yo ping, doctor    13951947646    ypzhai@medmail.com.cn 收起 <<
NCT00199004 Adult Acute Lymphocytic Leukem... 展开 >>ia 收起 << Phase 4 Completed - Germany ... 展开 >> University Hospital of Frankfurt, Medical Dept. II Frankfurt, Germany, 60590 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.52mL

0.30mL

0.15mL

7.61mL

1.52mL

0.76mL

15.23mL

3.05mL

1.52mL
参考文献

[1]Rappa G, Lorico A, et al. Potentiation by novobiocin of the cytotoxic activity of etoposide (VP-16) and teniposide (VM-26). Int J Cancer. 1992 Jul 9;51(5):780-7.

[2]Richter A, Strausfeld U, et al. Effects of VM26 (teniposide), a specific inhibitor of type II DNA topoisomerase, on SV40 DNA replication in vivo. Nucleic Acids Res. 1987 Apr 24;15(8):3455-68.

[3] Joyce H Lee, James M Berger. Cell Cycle-Dependent Control and Roles of DNA Topoisomerase II. Genes (Basel). 2019 Oct 30;10(11):859.

[4] Li J, et al. Topoisomerase II trapping agent teniposide induces apoptosis and G2/M or S phase arrest of oral squamous cell carcinoma. World J Surg Oncol. 2006 Jul 6;4:41.

[5] Attia SM, et al. Molecular cytogenetic evaluation of the aneugenic effects of teniposide in somatic and germinal cells of male mice. Mutagenesis. 2012 Jan;27(1):31-9.

[6] Sun YC, et al. MiR-181b sensitizes glioma cells to teniposide by targeting MDM2. BMC Cancer. 2014 Aug 25;14:611.