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Teniposide/替尼泊苷 {[allProObj[0].p_purity_real_show]}

货号:A102576 同义名: 替尼泊甙 / VM26; NSC 122819

Teniposide是Podophyllotoxin的衍生物,可以与DNA拓扑异构酶II相互作用,用于癌症的研究。

Teniposide/替尼泊苷 化学结构 CAS号:29767-20-2
Teniposide/替尼泊苷 化学结构
CAS号:29767-20-2
Teniposide/替尼泊苷 3D分子结构
CAS号:29767-20-2
Teniposide/替尼泊苷 化学结构 CAS号:29767-20-2
Teniposide/替尼泊苷 3D分子结构 CAS号:29767-20-2
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Teniposide/替尼泊苷 纯度/质量文件 产品仅供科研

货号:A102576 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Topo I Topo II Topo IV Topoisomerase 其他靶点 纯度
Ellagic acid 98%
β-Lapachone 99%+
(s)-10-hydroxycamptothecin 98+%
Camptothecin ++

Topo I, IC50: 0.68 μM

98%
Betulinic acid ++

Eukaryotic topoisomerase I, IC50: 5 μM

98%
Topotecan ++++

Topo I (MCF-7 Luc cells), IC50: 13 nM

Topo I (DU-145 Luc cells), IC50: 2 nM

98%
Irinotecan HCl Trihydrate 98%
SN-38 98%
Levofloxacin hydrate 98%
Dexrazoxane 99%+
Ofloxacin 98+%
Enoxacin 99%+
Flumequine +

Topo II, IC50: 15 μM

98%
Levofloxacin 97%
Etoposide 98%
Pefloxacin mesylate dihydrate 99.5%
Marbofloxacin 98+%
Voreloxin HCl 98%
Mitoxantrone 2HCl PKC 98%
Nalidixic acid 98%
Doxorubicin 97%
Novobiocin sodium 95%
Amonafide 99%+
Pirarubicin 98%+
Idarubicin HCl +++

Topo II (MCF-7 cells), IC50: 3.3 ng/mL

99%+
Genistein EGFR 98%
Teniposide 98%
Moxifloxacin 98%
Ciprofloxacin 98%
Clinafloxacin 99%
Gatifloxacin 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

98%
Epirubicin HCl 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Teniposide/替尼泊苷 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].

Teniposide/替尼泊苷 细胞实验

Cell Line
Concentration Treated Time Description References
MDA-MB-231 500 nM 24 hours To assess the effect of Teniposide on cell viability, results showed minimal impact on cell viability at low concentrations. Cell Death Dis. 2024 May 8;15(5):322.
Glioblastoma stem-like cells (GSCs) 0.5 µM 24 hours To evaluate the cytotoxic effect of Teniposide on GSCs under normoxic and hypoxic conditions. Results showed that Teniposide decreased GSC viability under normoxia but no changes were observed under hypoxia, indicating hypoxia enhances chemoresistance of GSCs to Teniposide. Int J Mol Sci. 2022 Aug 12;23(16):9022.
MDA-MB-231-1833 500 nM 5 days To evaluate the effect of Teniposide on 3D growth morphology, results showed Teniposide significantly reduced invasive growth morphology. Cell Death Dis. 2024 May 8;15(5):322.

Teniposide/替尼泊苷 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice CT26 tumor model Intraperitoneal injection 10 mg/kg Once on day 6 and once on day 7 To evaluate the inhibitory effect of Teniposide on tumor growth and its impact on immune cell infiltration in the tumor microenvironment. Results showed that Teniposide significantly inhibited tumor growth and increased the number and activity of tumor-infiltrating CD8+ T cells. J Clin Invest. 2019 Aug 13;129(11):4850-4862
C57BL/6J mice Hepa1-6 liver orthotopic tumor model Intraperitoneal injection 10 mg/kg Twice, interval not specified Evaluate the effect of HBO combined with teniposide treatment on the efficacy of PD-1 antibody. Results showed that HBO significantly enhanced teniposide-induced cGAS-STING-dependent tumor type I interferon and NF-κB signaling, both of which contributed to the activation of dendritic cells and subsequent cytotoxic T cells. J Immunother Cancer. 2022 Aug;10(8):e004006
Nude mice Breast cancer lung metastasis model Tail vein injection 500 nM Single injection, observed for 21 days To assess the effect of Teniposide on breast cancer lung metastasis, results showed Teniposide significantly reduced the formation of lung metastatic colonies. Cell Death Dis. 2024 May 8;15(5):322.

Teniposide/替尼泊苷 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 <<

Teniposide/替尼泊苷 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.

Teniposide/替尼泊苷 实验方案

计算器
存储液制备 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

Teniposide/替尼泊苷 技术信息

CAS号29767-20-2
分子式C32H32O13S
分子量 656.65
SMILES Code O=C1OC[C@]2([H])[C@H](O[C@H]3[C@@H]([C@H]([C@@H]([C@@H](CO4)O3)O[C@@H]4C5=CC=CS5)O)O)C6=C(C=C7OCOC7=C6)[C@@H](C8=CC(OC)=C(O)C(OC)=C8)[C@]21[H]
MDL No. MFCD00866516
别名 替尼泊甙 ;VM26; NSC 122819; HSDB 6546
运输蓝冰
InChI Key NRUKOCRGYNPUPR-QBPJDGROSA-N
Pubchem ID 452548
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
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